RAAS
信号通路图
研究领域
抑制剂选择性比较
RAAS产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2199 |
Aliskiren HemifumarateAliskiren Hemifumarate是一种直接肾素抑制剂，IC50为1.5 nM。 |
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| S1657 |
Enalaprilat DihydrateEnalaprilat Dihydrate是一种新型血管紧张肽转化酶(ACE)抑制剂，IC50为1.2 nM。 |
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| S6468New |
TrandolaprilTrandolapril是新型的血管紧张素转化酶（ACE）抑制剂，主要在肝脏被快速水解，生成其生物活性代谢物trandolaprilat。 |
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| S1506 |
Perindopril ErbuminePerindopril Erbumine是一种有效的血管紧张素转换酶（ACE）抑制剂，IC50为1.05 nM。 |
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| S1793 |
RamiprilRamipril 是血管紧张素转换酶(ACE)抑制剂，IC50为5 nM。 |
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| S1941 |
Enalapril MaleateEnalapril Maleate是一种血管紧张素转换酶抑制剂，用于治疗高血压，糖尿病肾病以及慢性心力衰竭。 |
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| S2051 |
CaptoprilCaptopril是一种血管紧张素转换酶（ACE）抑制剂，IC50为6 nM。 |
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| S2076 |
LisinoprilLisinopril 是血管紧张素转换酶抑制剂，用于治疗高血压，充血性心脏衰竭及心脏病发作，并能防止肾和糖尿病的视网膜并发症。 |
||
| S2079 |
Moexipril HClMoexipril HCl是一种口服有效的非巯基血管紧张素转化酶（ACE）抑制剂，IC50为0.041 µM，用于治疗高血压和充血性心脏衰竭。 |
||
| S2581 |
Quinapril HClQuinapril HCl 是Quinapril的盐酸盐，是一种血管紧张素转换酶抑制剂，Ki为20 μM。 |
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| S2099 |
Temocapril HClTemocapril HCl 是Temocapril的盐酸盐形式，是一种长效的血管紧张素转换酶（ACE）抑制剂，用于治疗高血压。 |
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| S2100 |
TemocaprilTemocapril是一种长效的血管紧张素转换酶（ACE）抑制剂，用于治疗高血压。 |
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| S2109 |
Imidapril HClImidapril HCl是一种血管紧张素转换酶（ACE）抑制剂，IC50为2.6 nM，用于治疗高血压。 |
||
| S5067 |
LosartanLosartan is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement. |
||
| S5728 |
Delapril HydrochlorideDelapril Hydrochloride is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. |
||
| S5712 |
Zofenopril calciumZofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure. |
||
| S7678 |
Sacubitril/valsartan (LCZ696)Sacubitril/valsartan (LCZ696)，由valsartan和sacubitril以1：1的摩尔比组成，是一个口服生物有效，双重作用的angiotensin receptor-neprilysin inhibitor (ARNi)，用于治疗高血压和心脏衰竭。Phase 3。 |
Histological analysis staining of three groups. (a) Representative H&E-staining micrographs displaying transverse myocardial section (original magnification ×200). (b) Masson staining of three groups (original magnification ×200). Collagen content (%) of heart tissues were presented as fibrosis (***P < 0.001, n = 7 per group). (c) Cardiac section of three group mice hearts stained with WGA (original magnification ×400) (*P < 0.05, n = 7 per group). (d) The expression of Drp1 significantly increased in DOX group (***P < 0.001, n = 7 per group) and it decreased in DOX + LCZ696 group (**P < 0.01, n = 7 per group).
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| S2095 |
Fosinopril SodiumFosinopril Sodium是一种血管紧张素转换酶（ACE）抑制剂的酯类前体药物，用于治疗高血压和某些类型的慢性心脏衰竭。 |
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| S1578 |
CandesartanCandesartan 是angiotensin II(血管紧张素II)受体拮抗剂， IC50为0.26 nM。 |
In vivo effects of candesartan and valsartan in post-MI rats overexpressing adrenal barr1. (A) Trichrome-Masson's staining in myocardial cross-sections from post-MI rats overexpressing barr1 specifically in their adrenals and treated for 7 days with either vehicle or 10 mg/kg body weight/day candesartan or 40 mg/kg body weight/day irbesartan (all via drinking water). Blue denotes collagen fibers, red denotes muscle fibers, and black represents cell nuclei. Representative images are shown from 5–6 rat hearts stained per group, along with staining in sham-operated rat hearts, in which no blue staining was detectable. (B,C) Heart mRNA levels of (B) collagen I (Col1a1) and brain natriuretic peptide (BNP) (C) in these rats at the end of the 7-day drug treatments. Values for post-MI rats receiving AdGFP in their adrenals instead of Adbarr1 (i.e. not overexpressing barr1 in their adrenals) were used as reference. *, p < 0.05, vs. Candesartan (Adbarr1), n=5 rat hearts/group. |
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| S1359 |
Losartan Potassium (DuP 753)Losartan Potassium (DuP 753)是一种血管紧张素II受体拮抗剂，与血管紧张素II竞争性结合AT1受体，IC50为20 nM。 |
Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan. |
|
| S1738 |
TelmisartanTelmisartan 是一种血管紧张素II受体拮抗剂（ARB），用于治疗高血压。 |
(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan. |
|
| S1507 |
IrbesartanIrbesartan是一种高效的特定血管紧张素II 1型(AT1)受体拮抗剂，IC50为1.3 nM。 |
Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p <0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan. |
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| S1894 |
ValsartanValsartan是一种血管紧张素II受体拮抗剂，用于治疗高血压以及充血性心力衰竭。 |
Effect of valsartan and cardamonin on Ang II-induced phosphorylation of p38 MAPK and ERK. Representative results of Western blot. |
|
| S7098 |
PD123319PD123319是一种有效的，选择性AT2血管紧张素Ⅱ受体拮抗剂， IC50为34 nM。 |
Ang II-induced MMP-2 protein expression through AT1 receptor in ex vivo cultured IAAA aortic walls (A) Ex vivo cultured aortic pieces from IAAA patients (n = 5) were incubated in the presence of different concentrations of Ang II for 48 h. (B) Ex vivo cultured aneurysmal aorta walls were pre-treated with either candesartan (10 µM, AT1R inhibitor) or PD123319 (10 µM, AT2R antagonist) for 48 h, followed by 1 µM Ang II treatment for 48 h. The group without Ang II incubation was used as control. **P < 0.01 vs. untreated control group; ##P < 0.01 vs. treated with Ang II alone. CA, candesartan; PD, PD123319. |
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| S1604 |
Olmesartan MedoxomilOlmesartan Medoxomil水解产物为Olmesartan，是一种选择性AT1亚型血管紧缩素II受体拮抗剂。 |
Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 mM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A–B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan. |
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| S2037 |
Candesartan CilexetilCandesartan Cilexetil一种特异性的，非肽类血管生成素II受体（ATR）拮抗剂，也是Candesartan的前体药物，是ATR拮抗剂，IC50为15 μg/kg。 |
(b) ASMCs were incubated with 1 µM candesartan or 10 µM PD123319 for 60 min before stimulation with 0.1 µM Ang II for 24 h in six-well plates. Western blot was used for analyses of the levels of MMP-2 expression in cell lysates. Top panel: Graphs show the relative MMP-2 protein levels normalized to GAPDH relative to control. Bottom panel: Ratio of MMP-2/GAPDH protein expression from a representative Western blot experiment. Shown are mean ± SEM of three individual experiments. **P < 0.01 vs. untreated control cells; ##P < 0.01 vs. cells treated with Ang II |
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| S3057 |
Azilsartan MedoxomilAzilsartan Medoxomil是一种有效的angiotensin II type 1 (AT1) receptor（血管紧张素II 1型受体）拮抗剂，抑制RAAS比作用于AT2选择性高10，000倍以上，用于治疗高血压。 |
(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan. |
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| S3046 |
AzilsartanAzilsartan是angiotensin II type 1 (AT1)（血管紧张素II 1型）受体拮抗剂，IC50为2.6 nM。 |
(B) Dose-response curves of each drug for acute G protein or βarr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.
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| S5581 |
OlmesartanOlmesartan is an an angiotensin 2 receptor antagonist with antihypertensive activity. |
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| S4975 |
FimasartanFimasartan是一种非肽段的angiotensin II receptor拮抗剂，与AT1受体非竞争性地结合。用于高血压和心力衰竭的治疗中。 |
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| S4102 |
Eprosartan MesylateEprosartan是一种非肽类血管紧张素Ⅱ受体拮抗剂，在大鼠血管平滑肌细胞中，[3H]-eprosartan与AT1受体结合，KD为0.83 nM。 |
(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan. |
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| P1085New |
Angiotensin II human AcetateAngiotensin II (angII)是一种八肽激素，能够影响心血管、肾脏和脑活性。它通过结合细胞膜上特定受体发挥作用。 |
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| S1284 |
Benazepril HClBenazepril HCl是一种用于治疗高血压的药物。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2199 |
Aliskiren HemifumarateAliskiren Hemifumarate是一种直接肾素抑制剂，IC50为1.5 nM。 |
||
| S1657 |
Enalaprilat DihydrateEnalaprilat Dihydrate是一种新型血管紧张肽转化酶(ACE)抑制剂，IC50为1.2 nM。 |
||
| S6468New |
TrandolaprilTrandolapril是新型的血管紧张素转化酶（ACE）抑制剂，主要在肝脏被快速水解，生成其生物活性代谢物trandolaprilat。 |
||
| S1506 |
Perindopril ErbuminePerindopril Erbumine是一种有效的血管紧张素转换酶（ACE）抑制剂，IC50为1.05 nM。 |
||
| S1793 |
RamiprilRamipril 是血管紧张素转换酶(ACE)抑制剂，IC50为5 nM。 |
||
| S1941 |
Enalapril MaleateEnalapril Maleate是一种血管紧张素转换酶抑制剂，用于治疗高血压，糖尿病肾病以及慢性心力衰竭。 |
||
| S2051 |
CaptoprilCaptopril是一种血管紧张素转换酶（ACE）抑制剂，IC50为6 nM。 |
||
| S2076 |
LisinoprilLisinopril 是血管紧张素转换酶抑制剂，用于治疗高血压，充血性心脏衰竭及心脏病发作，并能防止肾和糖尿病的视网膜并发症。 |
||
| S2079 |
Moexipril HClMoexipril HCl是一种口服有效的非巯基血管紧张素转化酶（ACE）抑制剂，IC50为0.041 µM，用于治疗高血压和充血性心脏衰竭。 |
||
| S2581 |
Quinapril HClQuinapril HCl 是Quinapril的盐酸盐，是一种血管紧张素转换酶抑制剂，Ki为20 μM。 |
||
| S2099 |
Temocapril HClTemocapril HCl 是Temocapril的盐酸盐形式，是一种长效的血管紧张素转换酶（ACE）抑制剂，用于治疗高血压。 |
||
| S2100 |
TemocaprilTemocapril是一种长效的血管紧张素转换酶（ACE）抑制剂，用于治疗高血压。 |
||
| S2109 |
Imidapril HClImidapril HCl是一种血管紧张素转换酶（ACE）抑制剂，IC50为2.6 nM，用于治疗高血压。 |
||
| S5067 |
LosartanLosartan is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement. |
||
| S5728 |
Delapril HydrochlorideDelapril Hydrochloride is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. |
||
| S5712 |
Zofenopril calciumZofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure. |
||
| S7678 |
Sacubitril/valsartan (LCZ696)Sacubitril/valsartan (LCZ696)，由valsartan和sacubitril以1：1的摩尔比组成，是一个口服生物有效，双重作用的angiotensin receptor-neprilysin inhibitor (ARNi)，用于治疗高血压和心脏衰竭。Phase 3。 |
Histological analysis staining of three groups. (a) Representative H&E-staining micrographs displaying transverse myocardial section (original magnification ×200). (b) Masson staining of three groups (original magnification ×200). Collagen content (%) of heart tissues were presented as fibrosis (***P < 0.001, n = 7 per group). (c) Cardiac section of three group mice hearts stained with WGA (original magnification ×400) (*P < 0.05, n = 7 per group). (d) The expression of Drp1 significantly increased in DOX group (***P < 0.001, n = 7 per group) and it decreased in DOX + LCZ696 group (**P < 0.01, n = 7 per group).
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| S2095 |
Fosinopril SodiumFosinopril Sodium是一种血管紧张素转换酶（ACE）抑制剂的酯类前体药物，用于治疗高血压和某些类型的慢性心脏衰竭。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1578 |
CandesartanCandesartan 是angiotensin II(血管紧张素II)受体拮抗剂， IC50为0.26 nM。 |
In vivo effects of candesartan and valsartan in post-MI rats overexpressing adrenal barr1. (A) Trichrome-Masson's staining in myocardial cross-sections from post-MI rats overexpressing barr1 specifically in their adrenals and treated for 7 days with either vehicle or 10 mg/kg body weight/day candesartan or 40 mg/kg body weight/day irbesartan (all via drinking water). Blue denotes collagen fibers, red denotes muscle fibers, and black represents cell nuclei. Representative images are shown from 5–6 rat hearts stained per group, along with staining in sham-operated rat hearts, in which no blue staining was detectable. (B,C) Heart mRNA levels of (B) collagen I (Col1a1) and brain natriuretic peptide (BNP) (C) in these rats at the end of the 7-day drug treatments. Values for post-MI rats receiving AdGFP in their adrenals instead of Adbarr1 (i.e. not overexpressing barr1 in their adrenals) were used as reference. *, p < 0.05, vs. Candesartan (Adbarr1), n=5 rat hearts/group. |
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| S1359 |
Losartan Potassium (DuP 753)Losartan Potassium (DuP 753)是一种血管紧张素II受体拮抗剂，与血管紧张素II竞争性结合AT1受体，IC50为20 nM。 |
Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan. |
|
| S1738 |
TelmisartanTelmisartan 是一种血管紧张素II受体拮抗剂（ARB），用于治疗高血压。 |
(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan. |
|
| S1507 |
IrbesartanIrbesartan是一种高效的特定血管紧张素II 1型(AT1)受体拮抗剂，IC50为1.3 nM。 |
Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p <0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan. |
|
| S1894 |
ValsartanValsartan是一种血管紧张素II受体拮抗剂，用于治疗高血压以及充血性心力衰竭。 |
Effect of valsartan and cardamonin on Ang II-induced phosphorylation of p38 MAPK and ERK. Representative results of Western blot. |
|
| S7098 |
PD123319PD123319是一种有效的，选择性AT2血管紧张素Ⅱ受体拮抗剂， IC50为34 nM。 |
Ang II-induced MMP-2 protein expression through AT1 receptor in ex vivo cultured IAAA aortic walls (A) Ex vivo cultured aortic pieces from IAAA patients (n = 5) were incubated in the presence of different concentrations of Ang II for 48 h. (B) Ex vivo cultured aneurysmal aorta walls were pre-treated with either candesartan (10 µM, AT1R inhibitor) or PD123319 (10 µM, AT2R antagonist) for 48 h, followed by 1 µM Ang II treatment for 48 h. The group without Ang II incubation was used as control. **P < 0.01 vs. untreated control group; ##P < 0.01 vs. treated with Ang II alone. CA, candesartan; PD, PD123319. |
|
| S1604 |
Olmesartan MedoxomilOlmesartan Medoxomil水解产物为Olmesartan，是一种选择性AT1亚型血管紧缩素II受体拮抗剂。 |
Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 mM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A–B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan. |
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| S2037 |
Candesartan CilexetilCandesartan Cilexetil一种特异性的，非肽类血管生成素II受体（ATR）拮抗剂，也是Candesartan的前体药物，是ATR拮抗剂，IC50为15 μg/kg。 |
(b) ASMCs were incubated with 1 µM candesartan or 10 µM PD123319 for 60 min before stimulation with 0.1 µM Ang II for 24 h in six-well plates. Western blot was used for analyses of the levels of MMP-2 expression in cell lysates. Top panel: Graphs show the relative MMP-2 protein levels normalized to GAPDH relative to control. Bottom panel: Ratio of MMP-2/GAPDH protein expression from a representative Western blot experiment. Shown are mean ± SEM of three individual experiments. **P < 0.01 vs. untreated control cells; ##P < 0.01 vs. cells treated with Ang II |
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| S3057 |
Azilsartan MedoxomilAzilsartan Medoxomil是一种有效的angiotensin II type 1 (AT1) receptor（血管紧张素II 1型受体）拮抗剂，抑制RAAS比作用于AT2选择性高10，000倍以上，用于治疗高血压。 |
(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan. |
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| S3046 |
AzilsartanAzilsartan是angiotensin II type 1 (AT1)（血管紧张素II 1型）受体拮抗剂，IC50为2.6 nM。 |
(B) Dose-response curves of each drug for acute G protein or βarr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.
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| S5581 |
OlmesartanOlmesartan is an an angiotensin 2 receptor antagonist with antihypertensive activity. |
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| S4975 |
FimasartanFimasartan是一种非肽段的angiotensin II receptor拮抗剂，与AT1受体非竞争性地结合。用于高血压和心力衰竭的治疗中。 |
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| S4102 |
Eprosartan MesylateEprosartan是一种非肽类血管紧张素Ⅱ受体拮抗剂，在大鼠血管平滑肌细胞中，[3H]-eprosartan与AT1受体结合，KD为0.83 nM。 |
(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| P1085New |
Angiotensin II human AcetateAngiotensin II (angII)是一种八肽激素，能够影响心血管、肾脏和脑活性。它通过结合细胞膜上特定受体发挥作用。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1284 |
Benazepril HClBenazepril HCl是一种用于治疗高血压的药物。 |
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