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Omapatrilat

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Catalog No. T16385Cas No. 167305-00-2
Alias BMS-186716

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

Omapatrilat

Omapatrilat

😃Good
Catalog No. T16385Alias BMS-186716Cas No. 167305-00-2
Omapatrilat is a metalloprotease ACE and NEP dual inhibitor (Ki: 0.64 and 0.45 nM, respectively).
Pack SizePriceAvailabilityQuantity
2 mg57 €5 days
100 mg946 €6-8 weeks
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Product Introduction

Bioactivity
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].
AliasBMS-186716
Chemical Properties
Molecular Weight408.53
FormulaC19H24N2O4S2
Cas No.167305-00-2
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 31 mg/mL (75.88 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4478 mL12.2390 mL24.4780 mL122.3900 mL
5 mM0.4896 mL2.4478 mL4.8956 mL24.4780 mL
10 mM0.2448 mL1.2239 mL2.4478 mL12.2390 mL
20 mM0.1224 mL0.6120 mL1.2239 mL6.1195 mL
50 mM0.0490 mL0.2448 mL0.4896 mL2.4478 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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