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Omapatrilat

Catalog No. T16385   CAS 167305-00-2
Synonyms: BMS-186716

Omapatrilat is a metalloprotease ACE and NEP dual inhibitor (Ki: 0.64 and 0.45 nM, respectively).

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Omapatrilat Chemical Structure
Omapatrilat, CAS 167305-00-2
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2 mg 5 days $ 61.00
100 mg 6-8 weeks $ 996.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Omapatrilat is a metalloprotease ACE and NEP dual inhibitor (Ki: 0.64 and 0.45 nM, respectively).
Targets&IC50 ACE:0.64 nM(ki), NEP:(ki)0.45 nM
In vitro In vitro autoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A display omapatril at (10 mg/kg) induces rapid and effective inhibition of renal NEP and ACE, respectively, for 24 h. Omapatrilat displays 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) [1][4].
In vivo Omapatrilat is widely used in experimental protocols related to hypertension and heart failure. Omapatrilat reduces mean arterial pressure (MAP) approximately 40 mmHg below baseline from 10 to 24 h. Omapatrilat shows 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 (p.o.; 100 μM/kg; once daily) causes a 38 mmHg decrease in systolic blood pressure at day three as compared to the vehicle [2]. Omapatrilat(Chronic oral administration) decreases aortic leakiness and atheroma formation with enhanced endothelial independent vasorelaxation to ANP[3]. Omapatrilat leads to significant inhibition of plasma ACE and increased plasma renin activity in rats[4].
Synonyms BMS-186716
Molecular Weight 408.53
Formula C19H24N2O4S2
CAS No. 167305-00-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL (75.88 mM)

TargetMolReferences and Literature

1. Fryer RM, et al. Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy ofenzymes associated with bradykinin-mediated angioedema.Br J Pharmacol. 2008 Mar;153(5):947-55. 2. Robl JA, et al. Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics asinhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7. 3. Ichiki T, et al. Endothelial permeability in vitro and in vivo: protective actions of ANP and omapatrilat in experimental atherosclerosis. Peptides. 2013 Oct;48:21-6. 4. Burrell LM, et al. Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6.

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Keywords

Omapatrilat 167305-00-2 Endocrinology/Hormones RAAS BMS 186716 BMS186716 BMS-186716 inhibitor inhibit

 

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