RAAS

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S2199	Aliskiren Hemifumarate	100 mg/mL	100 mg/mL	100 mg/mL
S1657	Enalaprilat Dihydrate	<1 mg/mL	70 mg/mL	<1 mg/mL
S5067	Losartan	-1 mg/mL	84 mg/mL	-1 mg/mL
S5728	Delapril Hydrochloride	<1 mg/mL	98 mg/mL	25 mg/mL
S5712	Zofenopril calcium	<1 mg/mL	32 mg/mL	<1 mg/mL
S1506	Perindopril Erbumine	88 mg/mL	<1 mg/mL	88 mg/mL
S1793	Ramipril	<1 mg/mL	83 mg/mL	83 mg/mL
S1941	Enalapril Maleate	<1 mg/mL	99 mg/mL	4 mg/mL
S2051	Captopril	2 mg/mL	43 mg/mL	43 mg/mL
S2076	Lisinopril	20 mg/mL	<1 mg/mL	<1 mg/mL
S2081	Cilazapril Monohydrate	<1 mg/mL	87 mg/mL	87 mg/mL
S2079	Moexipril HCl	<1 mg/mL	20 mg/mL	<1 mg/mL
S2581	Quinapril HCl	95 mg/mL	18 mg/mL	95 mg/mL
S2099	Temocapril HCl	<1 mg/mL	103 mg/mL	103 mg/mL
S2109	Imidapril HCl	54 mg/mL	88 mg/mL	29 mg/mL
S7678	Sacubitril/valsartan (LCZ696)	100 mg/mL	30 mg/mL	9 mg/mL
S2095	Fosinopril Sodium	117 mg/mL	<1 mg/mL	4 mg/mL
S1578	Candesartan	<1 mg/mL	88 mg/mL	1 mg/mL
S1359	Losartan Potassium (DuP 753)	92 mg/mL	92 mg/mL	92 mg/mL
S1738	Telmisartan	<1 mg/mL	13 mg/mL	<1 mg/mL
S4975	Fimasartan	-1 mg/mL	100 mg/mL	24 mg/mL
S1507	Irbesartan	<1 mg/mL	4 mg/mL	3 mg/mL
S1894	Valsartan	<1 mg/mL	87 mg/mL	87 mg/mL
S7098	PD123319	100 mg/mL	100 mg/mL	100 mg/mL
S1604	Olmesartan Medoxomil	<1 mg/mL	89 mg/mL	<1 mg/mL
S2037	Candesartan Cilexetil	<1 mg/mL	122 mg/mL	4 mg/mL
S3057	Azilsartan Medoxomil	<1 mg/mL	114 mg/mL	<1 mg/mL
S3046	Azilsartan	<1 mg/mL	91 mg/mL	<1 mg/mL
S4102	Eprosartan Mesylate	<1 mg/mL	104 mg/mL	4 mg/mL
S2199	Aliskiren Hemifumarate	100 mg/mL	100 mg/mL	100 mg/mL
S1657	Enalaprilat Dihydrate	<1 mg/mL	70 mg/mL	<1 mg/mL
S5067	Losartan	-1 mg/mL	84 mg/mL	-1 mg/mL
S5728	Delapril Hydrochloride	<1 mg/mL	98 mg/mL	25 mg/mL
S5712	Zofenopril calcium	<1 mg/mL	32 mg/mL	<1 mg/mL
S1506	Perindopril Erbumine	88 mg/mL	<1 mg/mL	88 mg/mL
S1793	Ramipril	<1 mg/mL	83 mg/mL	83 mg/mL
S1941	Enalapril Maleate	<1 mg/mL	99 mg/mL	4 mg/mL
S2051	Captopril	2 mg/mL	43 mg/mL	43 mg/mL
S2076	Lisinopril	20 mg/mL	<1 mg/mL	<1 mg/mL
S2081	Cilazapril Monohydrate	<1 mg/mL	87 mg/mL	87 mg/mL
S2079	Moexipril HCl	<1 mg/mL	20 mg/mL	<1 mg/mL
S2581	Quinapril HCl	95 mg/mL	18 mg/mL	95 mg/mL
S2099	Temocapril HCl	<1 mg/mL	103 mg/mL	103 mg/mL
S2109	Imidapril HCl	54 mg/mL	88 mg/mL	29 mg/mL
S7678	Sacubitril/valsartan (LCZ696)	100 mg/mL	30 mg/mL	9 mg/mL
S2095	Fosinopril Sodium	117 mg/mL	<1 mg/mL	4 mg/mL

特异性亚型抑制剂

RAAS抑制剂（48）
新RAAS产品

产品目录	产品描述	文献引用	实验数据
S2199	Aliskiren Hemifumarate Aliskiren Hemifumarate是一种直接肾素抑制剂，IC50为1.5 nM。
S1657	Enalaprilat Dihydrate Enalaprilat Dihydrate是一种新型血管紧张肽转化酶(ACE)抑制剂，IC50为1.2 nM。
S5067^New	Losartan Losartan 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^New	Delapril Hydrochloride Delapril Hydrochloride is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.
S5712^New	Zofenopril calcium Zofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure.
S1506	Perindopril Erbumine Perindopril 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	Ramipril Ramipril 是血管紧张素转换酶(ACE)抑制剂，IC50为5 nM。
S1941	Enalapril Maleate Enalapril 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	Captopril Captopril是一种血管紧张素转换酶（ACE）抑制剂，IC50为6 nM。
S2076	Lisinopril Lisinopril 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。
S2081	Cilazapril Monohydrate Cilazapril Monohydrate 是一种血管紧张素转换酶（ACE）抑制剂，用于治疗高血压和充血性心脏衰竭。。
S2079	Moexipril HCl Moexipril 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 HCl Quinapril HCl 是Quinapril的盐酸盐，是一种血管紧张素转换酶抑制剂，K_i为20 μM。
S2099	Temocapril HCl Temocapril 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	Temocapril Temocapril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 HCl Imidapril 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。
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。	J Mol Cell Cardiol, 2017, 108:138-148	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).
S2095	Fosinopril Sodium Fosinopril 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。
S1578	Candesartan Candesartan 是angiotensin II(血管紧张素II)受体拮抗剂， IC50为0.26 nM。	Exp Biol Med, 2015, 10.1177/1535370215576312 Acta Biochim Biophys Sin, 2015, 47(7), 1–9 Sci Rep, 2015, 5:8116	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.
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。	Antiviral Res, 2015, 120:140-6 Sci Rep, 2015, 5:8116	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	Telmisartan Telmisartan 是一种血管紧张素II受体拮抗剂（ARB），用于治疗高血压。	Sci Rep, 2015, 5:8116	(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.
S4975^New	Fimasartan Fimasartan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。
S1507	Irbesartan Irbesartan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。	Antiviral Res, 2015, 120:140-6 Sci Rep, 2015, 5:8116	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	Valsartan Valsartan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。	J Nat Med, 2014, 68(3):623-9 Sci Rep, 2015, 5:8116	Effect of valsartan and cardamonin on Ang II-induced phosphorylation of p38 MAPK and ERK. Representative results of Western blot.
S7098	PD123319 PD123319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。	Exp Biol Med, 2015, 10.1177/1535370215576312 Naunyn Schmiedebergs Arch Pharmacol, 2016, 389(12):1333-1340 Acta Biochim Biophys Sin, 2015, 47(7), 1–9	Effect of PD123319 treatment on sodium current (INa). Typical recordings of INa in cells from control (a), non-PD123319 (b), and PD123319 (c). x-axis: time (ms mini-second); y-axis: current volume (pA). The voltage clamp protocol is shown in (d). e Average I-V relationships of INa density (pA/pF) as a function of step potential (mV), obtained in control (filled squares), non-PD123319 (empty squares), and PD123319 (empty circles)
S1604	Olmesartan Medoxomil Olmesartan 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。	Sci Rep, 2015, 5:8116	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.
S2037	Candesartan Cilexetil Candesartan 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。	Exp Biol Med, 2015, 10.1177/1535370215576312 Sci Rep, 2015, 5:8116	(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
S3057	Azilsartan Medoxomil Azilsartan 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。	Sci Rep, 2015, 5:8116	(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.
S3046	Azilsartan Azilsartan是angiotensin II type 1 (AT1)（血管紧张素II 1型）受体拮抗剂，IC50为2.6 nM。	Sci Rep, 2015, 5:8116	(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.
S4102	Eprosartan Mesylate Eprosartan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，K_D为0.83 nM。	Sci Rep, 2015, 5:8116 Sci Rep, 2016, 10.1038/srep25694	(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.
S2199	Aliskiren Hemifumarate Aliskiren Hemifumarate是一种直接肾素抑制剂，IC50为1.5 nM。
S1657	Enalaprilat Dihydrate Enalaprilat Dihydrate是一种新型血管紧张肽转化酶(ACE)抑制剂，IC50为1.2 nM。
S5067^New	Losartan Losartan 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^New	Delapril Hydrochloride Delapril Hydrochloride is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.
S5712^New	Zofenopril calcium Zofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure.
S1506	Perindopril Erbumine Perindopril 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	Ramipril Ramipril 是血管紧张素转换酶(ACE)抑制剂，IC50为5 nM。
S1941	Enalapril Maleate Enalapril 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	Captopril Captopril是一种血管紧张素转换酶（ACE）抑制剂，IC50为6 nM。
S2076	Lisinopril Lisinopril 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。
S2081	Cilazapril Monohydrate Cilazapril Monohydrate 是一种血管紧张素转换酶（ACE）抑制剂，用于治疗高血压和充血性心脏衰竭。。
S2079	Moexipril HCl Moexipril 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 HCl Quinapril HCl 是Quinapril的盐酸盐，是一种血管紧张素转换酶抑制剂，K_i为20 μM。
S2099	Temocapril HCl Temocapril 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	Temocapril Temocapril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 HCl Imidapril 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。
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。	J Mol Cell Cardiol, 2017, 108:138-148	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).
S2095	Fosinopril Sodium Fosinopril 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。

研究领域

产品类型

RAAS

信号通路图

研究领域

特异性亚型抑制剂