2. Metabolic Enzyme/Protease
  3. Angiotensin-converting Enzyme (ACE)
  4. Omapatrilat

Omapatrilat  (Synonyms: BMS-186716)

Cat. No.: HY-18208 Purity: 99.88%
COA Handling Instructions

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

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

Omapatrilat Chemical Structure

Omapatrilat Chemical Structure

CAS No. : 167305-00-2

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Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 109 In-stock
Solid
5 mg USD 99 In-stock
10 mg USD 172 In-stock
25 mg USD 370 In-stock
50 mg USD 686 In-stock
100 mg USD 1241 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki 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 (Ki=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.
Molecular Weight

408.53

Appearance

Solid

Formula

C19H24N2O4S2
CAS No.
SMILES

O=C([[email protected]@H]1CCC[[email protected]](N21)([H])SCC[[email protected]](NC([[email protected]@H](S)CC3=CC=CC=C3)=O)C2=O)O
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.
Purity & Documentation
References
Kinase Assay
[1]

Omapatrilat is dissolved in 100% DMSO at 10 mM and diluted to 1% DMSO. NEP, NEP2, ACE and APP assays are performed at pH 7.4. The reaction buffer for NEP and NEP2 contained 50 mM HEPES, 140 mM NaCl, 10 mM KCl, 0.01% BSA. The buffer for ACE contained 100 mM Tris-HCl, 50 mM NaCl, 10 μM ZnCl2, and the buffer for APP contained 100 mM HEPES and 0.01% BSA. Assays are performed in 100 μL volume in black 96-well round-bottom plates at room temperature. Reactions are continuously monitored with excitation and emission wavelengths appropriate for each respective substrate. Enzyme velocity is determined from the linear part of the reaction[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3][4]

Rats: Sprague Dawley rats are weighed and then gavaged with vehicle (5% arabic gum) or omapatrilat (0.1, 1, 10 mg/kg) (n 5 6 rats/group). Rats are killed by decapitation at 1 h after gavage. Trunk blood is collected into prechilled tubes containing EDTA/aprotinin for the measurement of PRA and into prechilled heparin tubes for the measurement ofplasma ACE[4].

Rabbits: Omapatrilat is dissolved in drinking water. Rabbits are divided into 2 groups with 1% cholesterol diet, placebo-treated group and omapatrilat-treated group, and administrated (12 mg/Kg/day omapatrilat) once daily for 8 weeks. To demonstrate the acute effect of omapatrilat, urine is collected after omapatrilat or placebo administration for 24 hours at day 1, and urine volume, cGMP and ANP levels are assessed[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Omapatrilat167305-00-2BMS-186716BMS186716BMS 186716Angiotensin-converting Enzyme (ACE)Inhibitorinhibitorinhibit

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