| Bioactivity | Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM. | ||||||||||||
| Target | IC50: 66.2 μM (angiotensin II receptor) | ||||||||||||
| Invitro | Inhibition of Arachidonic acid (AA) metabolism by angiotensin II receptor blockers (ARBs) is detected in a concentration-dependent manner with IC50 of Olmesartan (66.2 μM)[1]. Olmesartan medoxomil (OLM) is a potent and selective angiotensin AT1 receptor blocker[2]. | ||||||||||||
| In Vivo | The efficacy of Olmesartan (20 mg/kg) studied in db/db diabetic mice for a period of 12 weeks starting from week 10 to 12 of age. The db/db mice have 11.7 fold increased albuminuria in comparison to control mice at week 22 to 24 of age. Twelve weeks Olmesartan administration significantly reduces albuminuria in db/db mice by 77% as compared with placebo treated db/db mice. The albumin/creatinine ratio (ACR) is increased in db/db mice in comparison to control mice by 7.1 fold and Olmesartan treatment significantly decreases ACR by 59% in db/db mice[3]. | ||||||||||||
| Name | Olmesartan medoxomil | ||||||||||||
| CAS | 144689-63-4 | ||||||||||||
| Formula | C29H30N6O6 | ||||||||||||
| Molar Mass | 558.59 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Senda A, et al. Effects of Angiotensin II Receptor Blockers on Metabolism of Arachidonic Acid via CYP2C8. Biol Pharm Bull. 2015;38(12):1975-9. [2]. Shah S, et al. Simultaneous Quantitative Analysis of Olmesartan Medoxomil and Amlodipine Besylate in Plasma by High-performance Liquid Chromatography Technique. J Young Pharm. 2012 Apr;4(2):88-94. [3]. Gu J, et al. Olmesartan Prevents Microalbuminuria in db/db Diabetic Mice Through Inhibition of Angiotensin II/p38/SIRT1-Induced Podocyte Apoptosis. Kidney Blood Press Res. 2016 Nov 21;41(6):848-864. |