[CAS NO. 167305-00-2] Omapatrilat

Name: Omapatrilat
Brand: Arctom Scientific
SKU: AS196249

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PRODUCTS SPECIFICATIONS [167305-00-2]

Distributor

Catalog

AS196249

Brand

Arctom Scientific

CAS

167305-00-2

DESCRIPTION [167305-00-2]

Overview

MDL	-
Molecular Weight	408.53
Molecular Formula	C19H24N2O4S2
SMILES	O=C([C@@H]1CCC[C@](N21)([H])SCC[C@H](NC([C@@H](S)CC3=CC=CC=C3)=O)C2=O)O

For research use only. We do not sell to patients.

Summary

Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with K _i values of 0.64 and 0.45 nM, respectively.

IC50 & Target

Ki: 0.45 nM (NEP), 0.64 nM (ACE) ^[1] ; IC50: 8 nM (NEP), 5 nM (ACE) ^[2]

In Vitro

Omapatrilat exhibits high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (K _i =0.45, 25, 0.64, 250 nM) ^[1] . 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 ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : ≥ 31 mg/mL ( 75.88 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4478 mL	12.2390 mL	24.4780 mL
5 mM	0.4896 mL	2.4478 mL	4.8956 mL
10 mM	0.2448 mL	1.2239 mL	2.4478 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 4.25 mg/mL (10.40 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

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)-

7H-Pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid, octahydro-4-[(2-mercapto-1-oxo-3-phenylpropyl)amino]-5-oxo-, [4S-[4α(R*),7α,10aβ]]-

(4S,7S,10aS)-Octahydro-4-[[(2S)-2-mercapto-1-oxo-3-phenylpropyl]amino]-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid

BMS 186716

Omapatrilat

BMS 186716-01