product name Olmesartan Medoxomil
Description: Olmesartan Medoxomil (also known as CS-866) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure. It also inhibits the negative regulatory feedback on renin secretion. The result of receptor inhibition is vasodilation and a reduction in peripheral resistance. Olmesartan Medoxomil significantly reduces liver hydroxyproline content, and TGF-beta1.
References: Br J Pharmacol. 2003 Jul;139(6):1085-94; J Hypertens Suppl. 2001 Jun;19(1):S3-14.
558.59
Formula
C29H30N6O6
CAS No.
144689-63-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (159.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CS-866
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| References | Br J Pharmacol. 2003 Jul;139(6):1085-94; J Hypertens Suppl. 2001 Jun;19(1):S3-14; Toxicol Appl Pharmacol. 2013 Aug 15;271(1):106-13. |
