Home GPCR & G Protein Angiotensin Receptor antagonist Olmesartan Medoxomil For research use only.

Olmesartan Medoxomil

Synonyms: CS-866,RNH-6270

Olmesartan Medoxomil (CS-866,RNH-6270) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.

Olmesartan Medoxomil Chemical Structure

Olmesartan Medoxomil Chemical Structure

CAS No. 144689-63-4

Purity & Quality Control

Olmesartan Medoxomil Related Products

Biological Activity

Description Olmesartan Medoxomil (CS-866,RNH-6270) 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00185055 Completed
Healthy
Daiichi Sankyo
 November 2004 Phase 4
NCT00362960 Completed
Type 2 Diabetes Mellitus|Diabetic Nephropathy|Proteinuria|Renal Disease
Sankyo Pharma Gmbh|Daiichi Sankyo
 May 2003 Phase 3

Chemical Information & Solubility

Molecular Weight 558.59 Formula

C29H30N6O6
CAS No. 144689-63-4 SDF Download Olmesartan Medoxomil SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (159.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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