Olmesartan Medoxomil

Catalog No.S1604 Synonyms: CS-866

For research use only.

Olmesartan Medoxomil (CS-866) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.

Olmesartan Medoxomil Chemical Structure

CAS No. 144689-63-4

Selleck's Olmesartan Medoxomil has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Angiotensin Receptor Inhibitors

Biological Activity

Description Olmesartan Medoxomil (CS-866) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.
Targets
AT1 receptor [1]
In vitro

Olmesartan Medoxomil significantly reduces liver hydroxyproline content, the mRNA expression of collagen alpha1(I) and alpha-smooth muscle actin (alpha-SMA), and plasma levels of transforming growth factor-beta1 (TGF-beta1). [1] Olmesartan Medoxomil is a pro-drug containing an ester moiety that, after oral administration, is rapidly cleaved to release the active form Olmesartan (RNH-6270). Olmesartan is a highly potent, competitive and selective All AT1 receptor antagonist with almost no antagonistic activity on AT2 and AT4 receptors. [2]

In vivo Olmesartan produces a rapid and long-lasting inhibition of All-induced pressor responses in conscious rats. Oralolmesartan medoxomil also inhibits All-pressor response but onset of the action is slower compared with intravenous administration. Olmesartan Medoxomil exhibits dose-dependent antihypertensive effects in several rat and dog models, with the most marked effects seen in high plasma renin models, when compared with normal or low renin types. Olmesartan medoxomil exhibits, beside antihypertensive effects, beneficial effects in animal models of various types of nephrosis and heart failure, and anti-atherogenic effects in hyperlipidaemic animals. [2] Olmesartan Medoxomil dose-dependently ameliorates the colonic histopathological and biochemical injuries in rats, an effect that is comparable or even better than that of the standard Sulfasalazine. [3] Olmesartan medoxomil significantly reduces the induction of hypoxic cor pulmonale not only on echocardiographical observations but also in brain natriuretic peptide (BNP) in chronic hypoxic rats, TGF-beta and endothelin gene expressions in molecular studies. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 89 mg/mL
(159.32 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 558.59
Formula

C29H30N6O6

CAS No. 144689-63-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)OCC5=C(OC(=O)O5)C)C(C)(C)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00185055 Completed Drug: Olmesartan medoxomil|Drug: Irbesartan|Drug: Valsartan Healthy Daiichi Sankyo Inc. November 2004 Phase 4
NCT00362960 Completed Drug: Olmesartan medoxomil|Drug: Losartan Type 2 Diabetes Mellitus|Diabetic Nephropathy|Proteinuria|Renal Disease Sankyo Pharma Gmbh|Daiichi Sankyo Inc. May 2003 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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