PDE
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) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S2131 | Roflumilast | <1 mg/mL | 81 mg/mL | 15 mg/mL |
| S1431 | Sildenafil Citrate | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S1455 | Cilomilast | <1 mg/mL | 69 mg/mL | 50 mg/mL |
| S1512 | Tadalafil | <1 mg/mL | 78 mg/mL | <1 mg/mL |
| S2515 | Vardenafil HCl Trihydrate | 10 mg/mL | 100 mg/mL | 20 mg/mL |
| S5014 | Crisaborole (AN2728) | -1 mg/mL | 50 mg/mL | -1 mg/mL |
| S4837 | Ibudilast | 30 mg/mL | 46 mg/mL | 46 mg/mL |
| S1550 | Pimobendan | <1 mg/mL | 67 mg/mL | 5 mg/mL |
| S2620 | GSK256066 | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S2687 | Mardepodect (PF-2545920) | <1 mg/mL | 78 mg/mL | 78 mg/mL |
| S1430 | Rolipram | <1 mg/mL | 55 mg/mL | 55 mg/mL |
| S8034 | Apremilast (CC-10004) | <1 mg/mL | 92 mg/mL | <1 mg/mL |
| S1294 | Cilostazol | <1 mg/mL | 74 mg/mL | 6 mg/mL |
| S2484 | Milrinone | <1 mg/mL | 42 mg/mL | <1 mg/mL |
| S4019 | Avanafil | <1 mg/mL | 97 mg/mL | <1 mg/mL |
| S2127 | S- (+)-Rolipram | <1 mg/mL | 55 mg/mL | 55 mg/mL |
| S1673 | Aminophylline | 84 mg/mL | 53 mg/mL | <1 mg/mL |
| S3172 | Anagrelide HCl | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S1504 | Dyphylline | 51 mg/mL | 51 mg/mL | <1 mg/mL |
| S1895 | Dipyridamole | <1 mg/mL | 101 mg/mL | 50 mg/mL |
| S4164 | Doxofylline | 24 mg/mL | 53 mg/mL | 2 mg/mL |
| S4090 | Fenspiride HCl | 59 mg/mL | 9 mg/mL | <1 mg/mL |
| S7224 | Deltarasin | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8459 | TAK-063 | <1 mg/mL | 85 mg/mL | <1 mg/mL |
| S2291 | Diosgenin | <1 mg/mL | <1 mg/mL | 5 mg/mL |
| S2312 | Icariin | <1 mg/mL | 50 mg/mL | <1 mg/mL |
| S4683 | Sildenafil Mesylate | 100 mg/mL | 100 mg/mL | 4 mg/mL |
| S4684 | Sildenafil | 14 mg/mL | <1 mg/mL | <1 mg/mL |
| S2320 | Luteolin | <1 mg/mL | 57 mg/mL | 3 mg/mL |
| S8218 | PF-8380 | <1 mg/mL | 95 mg/mL | <1 mg/mL |
| S2368 | Theobromine | <1 mg/mL | <1 mg/mL | <1 mg/mL |
- PDE抑制剂（31）
- 新PDE产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2131 |
RoflumilastRoflumilast 是一种选择性的PDE4抑制剂，无细胞试验中IC50为0.2-4.3 nM。 |
Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6). |
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| S1431 |
Sildenafil CitrateSildenafil Citrate，一种环鸟苷酸单磷酸盐(cGMP)特异性的Ⅵ型磷酸二酯酶(PDE5)选择性抑制剂，对勃起功能障碍具有良好的耐受性和较高作用效果。 |
ADOR lung cancer cells (a July 2015 PDX model) were transfected with an empty vector plasmid or plasmids to express GRP78 and HSP27 together. Twenty-four hours after transfection cells were treated with vehicle control or with OSU-03012 (2.0mM) sildenafil (2mM) for 6 h after which cells were fixed in place and permeabilized using 0.5% Triton X100. Immuno-fluorescence was performed to detect the expression levels of Calnexin; glucosidase I; and glucosidase IIa at 10 magnification using a Hermes WiScan system.
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| S1455 |
CilomilastCilomilast是一种有效的PDE4抑制剂，IC50为110 nM，具有抗炎活性和弱的中枢神经系统活性。Phase 3。 |
LNCaP-C4 prostate cancer cells were suspended in matrigel and transplanted under the kidney capsule of male nude mice hosts. Mice were treated with vehicle-only (10% EtOH, 90% olive oil) control, cilomilast or NVP-ABE171 by gavage (n=7-11 for each respective group)The xenografts LNCaP-C4 xenografts were excised, fixed in formalin, and embedded in paraffin blocks. IHC with Ki67 (proliferation), TUNEL (apoptosis), or p21 (senescence) was performed. Representative Ki67 and TUNEL photomicrographs for cilomilast and NVP-ABE171 treatment group are shown.
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| S1512 |
TadalafilTadalafil是一种PDE-5抑制剂，无细胞试验中IC50为1.8 nM。Tadalafil对PDE5的选择性比对PDEs家族中其他成员高9000倍以上，除了PDE11。它能部分抑制PDE11。 |
(a): E. coli bacteria transformed to be resistant to ampicillin and kayamycin (AMPr KAYAr) were grown in AMPt KAYAt media and cells treated with OSU-03012 (2 μM); sildenafil (2 μM); tadalafil (2 μM), or in combination as indicated. Bacterial cell numbers were determined by assessing the protein concentration of the bacterial cell pellet 3 h, 6h and 12 h after drug exposure * P<0.05 less than corresponding vehicle value. The total protein content of each treatment condition was determined 3 h after addition of antibiotic. Portions of bacteria from each treatment condition were isolated and SDS PAGE and immuno-blotting performed to determine the expression of Dna J, Dna K, RecA and GrpE. (b): E. coli bacteria Gram stained and examined under a X100 oil immersion magnification.
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| S2515 |
Vardenafil HCl TrihydrateVardenafil HCl Trihydrate是一种新型PDE抑制剂，作用于PDE5和PDE1，IC50分别为0.7和180 nM。 |
(G) Immunoblot analysis for TAZ and Nanog in PCSC after vardenafil treatments. (H) Cytotoxicity to DDP in PCSC treated with indicated concentrations of vardenafil. **p < 0.01, *p < 0.05 versus PC3 cells, vardenafil at 0 μM, or DDP at 0 μM; ++p < 0.01, +p < 0.05 versus vardenafil at 0 μM.
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| S5014New |
Crisaborole (AN2728)Crisaborole是选择性的小分子PDE4抑制剂，具有广谱的抗炎活性。 |
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| S4837New |
IbudilastIbudilast是一种相对非选择性的phosphodiesterase抑制剂，具有抗炎和神经保护活性。 |
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| S1550 |
PimobendanPimobendan是一种磷酸二酯酶III(PDE III)选择性抑制剂，IC50为0.32 μM。 |
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| S2620 |
GSK256066GSK256066是一种选择性的PDE4B(与A-D亚型具有相等的亲和力)抑制剂，IC50为3.2 pM，比作用于PDE1/2/3/5/6选择性高380，000倍以上，作用于PDE4B比作用于PDE7选择性高2500倍以上。Phase 2。 |
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| S2687 |
Mardepodect (PF-2545920)PF-2545920是一种有效的，选择性的PDE10A抑制剂，IC50为0.37 nM，比作用于PDE选择性高1000倍以上。 |
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| S1430 |
RolipramPDE4的选择性抑制剂，rolipram，抑制免疫纯化的PDE4B和PDE4D活性，IC50分别为130 nM和240 nM。具有抗炎活性。 |
D, average percentage difference of cell growth by PDE4D inhibitors between STK11 mutant and wild-type cell lines. The sensitivity on STK11mt cell lines represents the difference of average percentage growth between STK11-mutant (NCI-H1993 and NCI-H1395) and wild-type cell lines (NCI-H82 and NCI-H524). Average percentage growth of each cell line by a PDE4D inhibitor was based on the DMSO control. Cells were treated with a 20 μmol/L of PDE4D inhibitors for 3, 7, and 10 days incubation, respectively. The cell viability was determined using CellTiter-Blue fluorescence. *, P < 0.01 and **, P < 0.05 in the difference between STK11-mutant and wild-type cell lines. All cells used in the experiment were cultured in normal conditioned RPMI medium with 10% FBS and 1% penicillin/streptavidin.
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| S8034 |
Apremilast (CC-10004)Apremilast (CC-10004)是一种口服生物有效的PDE4和TNF-α抑制剂，IC50分别为74 nM和77 nM。 |
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| S1294 |
CilostazolCilostazol是一种环核苷酸磷酸二酯酶3型(PDE3)抑制剂，IC50为0.2 μM，也抑制腺苷酸的摄取。 |
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| S2484 |
MilrinoneMilrinone是一种有效的，选择性的磷酸二酯酶-3抑制剂，抑制FIII PDE，IC50为0.42 μM。 |
Viability of H9c2 cells incubated with MRN-HSA-NPs (black bars) compared with MRN-Lactate (grey bars) at different MRN concentrations, at (a) 4 hours, (b) 24 hours and (c) 48 hours. The graph shows a representative result of mean±SD (n=3). ****P<0.0001, ***P<0.001, **P<0.01 and *P<0.05 were considered significant based on Sidak’s posthoc analysis. |
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| S4019 |
AvanafilAvanafil是一种高度选择性PDE5抑制剂，IC50为1nM. |
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| S2127 |
S- (+)-RolipramS- (+)-Rolipram抑制人体单核细胞环AMP特异性的PDE4，IC50为0.75 μM，作用于中枢神经系统，具有消炎和抗抑郁活性，比其R-对映体作用效果稍弱。 |
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| S1673 |
AminophyllineAminophylline是一种竞争性的，非选择性的磷酸二酯酶抑制剂，IC50为0.12 mM，也是非选择性的腺苷受体拮抗剂。 |
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| S3172 |
Anagrelide HClAnagrelide HCl是一种治疗原发性血小板增多症的药物。是一种口服的imidazoquinazoline药剂，具有抗环腺苷酸磷酸二酯酶的活性并且在人和动物中都能抑制血小板聚集。Anagrelide通过抑制巨核细胞成熟为血小板来起作用。 |
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| S1504 |
DyphyllineDyphylline是一种黄嘌呤衍生物，具有扩张支气管和血管的作用。 |
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| S1895 |
DipyridamoleDipyridamole是一种磷酸二酯酶抑制剂，通过红细胞和血管内皮细胞，抑制腺苷的摄取和代谢。 |
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| S4164 |
DoxofyllineDoxofylline是一种磷酸二酯酶抑制剂，是黄嘌呤衍生物，用于治疗哮喘。 |
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| S4090 |
Fenspiride HClFenspiride是一种支气管扩张剂，具有抗炎特性，作用于人离体的支气管，抑制磷酸二酯酶4和磷酸二酯酶3活性，logIC50值分别为4.16和3.44。 |
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| S7224 |
DeltarasinDeltarasin是一种小分子抑制剂，抑制KRAS-PDEδ相互作用，其结合到纯PDEδ的Kd值为38 nM。 |
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| S8459 |
TAK-063TAK-063是新型的、选择性的PDE10A抑制剂，IC50为0.30 nM。 |
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| S2291 |
DiosgeninDiosgenin 是一种类固醇皂甙元，为半合成孕激素的前体，在早期与口服避孕药一起使用。 |
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| S2312 |
IcariinIcariin是一种cGMP特异性的PDE5抑制剂，IC50为0.432 μM，作用于PDE5比作用于PDE4选择性高167倍。 |
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| S4683 |
Sildenafil MesylateSildenafil Mesylate是Sildenafil的甲磺酸盐形式，Sildenafil是Phosphodiesterase 5的抑制剂。 |
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| S4684 |
SildenafilSildenafil是Phosphodiesterase 5抑制剂，其IC50为5.22 nM。 |
mRNA and protein expression levels of Id‑1 following treatment with 5 μM sildenafil for 24 h. (A) Relative mRNA expression levels of Id‑1 in the HemECs were significantly decreased by 44.2%, according to the 2‑ΔΔCq method (***P=0.0006 vs. control). (B) Western blotting revealed that the protein expression levels of Id‑1 markedly decreased following treatment with sildenafil when compared with the negative control. The TCA 8113 cell line was used as a positive control. HemECs, hemangioma endothelial cells; SIL, sildenafil; ID‑1, inhibitor of differentiation 1.
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| S2320 |
LuteolinLuteolin是一种非选择性的PDE抑制剂，作用于PDE1-5，Ki分别为15.0 μM， 6.4 μM， 13.9 μM， 11.1 μM和9.5 μM。Phase 2. |
Bioactive compounds inhibit recombinant HDAC activity. Recombinant HDACs were incubated with flavonoid Luteolin (C) for 2 h prior to the addition of cell permeable HDAC substrates. Luteolin inhibited activity of most classes I, IIa, and IIb HDAC isoforms. |
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| S8218 |
PF-8380PF-8380是一种有效的自毒素抑制剂，在体外酶活性实验中测得IC50为2.8 nM。 |
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| S2368 |
TheobromineTheobromine 是黄嘌呤生物碱，作为一种支气管扩张剂，血管扩张剂。 |
