OMAPATRILAT
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- CAS号:
- 167305-00-2
- 英文名:
- OMAPATRILAT
- 英文别名:
- VANLEV;OMAPATRILAT;BMS 186716-01;OMAPATRILAT/VANLEV;Omapatrilat (BMS-186716);Omapatrilat >=98% (HPLC);7H-Pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid, octahydro-4-[[(2S)-2-mercapto-1-oxo-3-phenylpropyl]amino]-5-oxo-, (4S,7S,10aS)-
- 中文名:
- OMAPATRILAT
- 中文别名:
- 奥马曲拉;化合物 T16385;化合物 OMAPATRILAT;(4S,7S,10AS)-4-((S)-2-巯基-3-苯基丙酰氨基)-5-氧代八氢-2H-吡啶并[2,1-B] [1,3]硫杂氮杂-7-甲酸
- CBNumber:
- CB1695018
- 分子式:
- C19H24N2O4S2
- 分子量:
- 408.53
- MOL File:
- 167305-00-2.mol
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OMAPATRILAT化学性质
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熔点:
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218-220°
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比旋光度:
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D -78.9° (c = 0.46 in DMF)
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沸点:
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724.2±60.0 °C(Predicted)
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密度:
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1.37±0.1 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2-8°C
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溶解度:
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DMSO: 30 mg/ml
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形态:
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A crystalline solid
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酸度系数(pKa):
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3.44±0.40(Predicted)
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颜色:
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White to gray
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OMAPATRILAT性质、用途与生产工艺
Omapatrilat是金属蛋白酶ACE和NEP的双重抑制剂，Ki值分别为0.64和0.45 nM。
Ki: 0.45 nM (NEP), 0.64 nM (ACE);
IC50: 8 nM (NEP), 5 nM (ACE)
Omapatrilat exhibits high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (K
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=0.45, 25, 0.64, 250 nM) .
In vitro
autoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A show omapatril at (10 mg/kg) causes rapid and potent inhibition of renal NEP and ACE, respectively, for 24 h.
Omapatrilat demonstrates excellent blood pressure lowering in a variety of animal models characterized by various levels of plasma renin activity and significantly potentiates urinary sodium, ANP, and cGMP excretion in a cynomolgus monkey assay. Omapatrilat decreases mean arterial pressure (MAP) approximately 40 mmHg below baseline from 10 to 24 h. Oral administration of omapatrilat at 100 μM/kg once daily results in a 38 mmHg decrease in systolic blood pressure at day three as compared to vehicle . Omapatrilat is widely used in experimental protocols related to hypertension and heart failure. Chronic oral administration of omapatrilat reduces aortic leakiness and atheroma formation with enhanced endothelial independent vasorelaxation to ANP. Omapatrilat causes significant inhibition of plasma ACE and increased plasma renin activity in rats.
OMAPATRILAT
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/11/08 | HY-18208 | OMAPATRILAT
Omapatrilat | 167305-00-2 | 5mg | 820元 |
| 2024/11/08 | HY-18208 | OMAPATRILAT
Omapatrilat | 167305-00-2 | 10mM * 1mLin DMSO | 902元 |
167305-00-2, OMAPATRILAT 相关搜索:
- 抑制剂
- 16730-00-2
- 化合物 OMAPATRILAT
- 化合物 T16385
- (4S,7S,10AS)-4-((S)-2-巯基-3-苯基丙酰氨基)-5-氧代八氢-2H-吡啶并[2,1-B] [1,3]硫杂氮杂-7-甲酸
- 奥马曲拉
- 167305-00-2
- Omapatrilat (BMS-186716)
- Omapatrilat >=98% (HPLC)
- 7H-Pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid, octahydro-4-[[(2S)-2-mercapto-1-oxo-3-phenylpropyl]amino]-5-oxo-, (4S,7S,10aS)-
- BMS 186716-01
- OMAPATRILAT/VANLEV
- VANLEV
- OMAPATRILAT