OMAPATRILAT
OMAPATRILAT Basic information
- Product Name:
- OMAPATRILAT
- Synonyms:
-
- OMAPATRILAT
- VANLEV
- OMAPATRILAT/VANLEV
- BMS 186716-01
- 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)-
- Omapatrilat >=98% (HPLC)
- Omapatrilat (BMS-186716)
- CAS:
- 167305-00-2
- MF:
- C19H24N2O4S2
- MW:
- 408.53
- Mol File:
- 167305-00-2.mol
OMAPATRILAT Chemical Properties
- Melting point:
- 218-220°
- alpha
- D -78.9° (c = 0.46 in DMF)
- Boiling point:
- 724.2±60.0 °C(Predicted)
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- DMSO: 30 mg/ml
- form
- A crystalline solid
- pka
- 3.44±0.40(Predicted)
- color
- White to gray
OMAPATRILAT Usage And Synthesis
Uses
Treatment of hypertension and congestive heart failure (neutral endopeptidase and angiotensin converting enzyme inhibitor).
Definition
ChEBI: Omapatrilat is a dipeptide.
in vivo
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 [2]. 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[3]. Omapatrilat causes significant inhibition of plasma ACE and increased plasma renin activity in rats[4].
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