For research use only.
Catalog No.S1604 Synonyms: CS-866
CAS No. 144689-63-4
Olmesartan Medoxomil (CS-866) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.
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Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 mM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A–B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan.
Sci Rep, 2015, 5:8116.. Olmesartan Medoxomil purchased from Selleck.
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|Description||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 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. |
|In vitro||DMSO||89 mg/mL (159.32 mM)|
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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|
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