Omapatrilat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

金属蛋白酶 ACE 和 NEP 的有效双重抑制剂，Ki 分别为 0.64 nM 和 0.45 nM。

A potent, dual inhibitor of the metalloproteases ACE and NEP with Ki of 0.64 nM and 0.45 nM, respectively; shows moderate activity against APP, and low activity against ECE1; causes significant inhibition of plasma ACE and increases plasma renin activity, reduces blood pressure in spontaneously hypertensive rats; orally active.Hypertension Discontinued.

Omapatrilat exhibits high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (Ki=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.

BMS-186716

Metabolic Enzyme/Protease

ACE

ACE

Cardiovascular Disease

Hypertension

167305-00-2

408.5349

C19H24N2O4S2

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C([C@@H]1CCC[C@](N21)([H])SCC[C@H](NC([C@@H](S)CC3=CC=CC=C3)=O)C2=O)O

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)-

(-20℃)

With Ice Pack

≥ 2 years