Olmesartan Medoxomil, a angiotensin II receptor antagonist

Olmesartan Medoxomil is a synthetic imidazole-derived angiotensin II receptor antagonist acting as a prodrug with an antihypertensive property

Product information

CAS Number: 144689-63-4

Molecular Weight: 558.59

Formula: C29H30N6O6

Synonym:

CS-866

Olmetec

Olsertain

Azor

Benicar

Related CAS Number:

144689-24-7 (Olmesartan)

Chemical Name: (5-methyl-2-oxo-2H-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-{[2'-(1H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}-1H-imidazole-5-carboxylate

Smiles: CC1OC(=O)OC=1COC(=O)C1=C(N=C(CCC)N1CC1C=CC(=CC=1)C1=CC=CC=C1C1NN=NN=1)C(C)(C)O

InChiKey: UQGKUQLKSCSZGY-UHFFFAOYSA-N

InChi: InChI=1S/C29H30N6O6/c1-5-8-23-30-25(29(3,4)38)24(27(36)39-16-22-17(2)40-28(37)41-22)35(23)15-18-11-13-19(14-12-18)20-9-6-7-10-21(20)26-31-33-34-32-26/h6-7,9-14,38H,5,8,15-16H2,1-4H3,(H,31,32,33,34)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 89 mg/mL(159.32 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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). 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.

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. 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. 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.

References:

1. Nagib MM, et al. Toxicol Appl Pharmacol,?013, 271(1), 106-113.
2. Koike H, et al. J Hypertens Suppl,?001,?9(1), S3-14.
3. Kurikawa N, et al. Br J Pharmacol,?003, 139(6), 1085-1094.
4. Kurikawa N, et al. Br J Pharmacol, ?003, 139(6), 1085-1094.

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