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Olmesartan

Cat. No. M3265
Olmesartan Structure
Synonym:

Benicar, Olmetec

Size Price Availability Quantity
25mg USD 50  USD50 In stock
50mg USD 80  USD80 In stock
100mg USD 125  USD125 In stock
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Quality Control & Documentation
Biological Activity

Olmesartan is an angiotensin II receptor antagonist with an IC50 of 7.7 nM. It is used to treat high blood pressure. Olmesartan works by blocking the binding of angiotensin II to the AT1 receptors in vascular muscle; it is therefore independent of angiotensin II synthesis pathways, unlike ACE inhibitors. By blocking binding rather than synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion. As a result of this blockage, olmesartan reduces vasoconstriction and the secretion of aldosterone. This lowers blood pressure by producing vasodilation, and decreasing peripheral resistance.

Chemical Information
Molecular Weight 446.5
Formula C24H26N6O3
CAS Number 144689-24-7
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Long Zou, et al. Olmesartan-associated Enteropathy

[2] V Zimmer, et al. Gastrointestinal: The duodenum on and off olmesartan

[3] Yong Huo, et al. Efficacy and safety of sacubitril/valsartan compared with olmesartan in Asian patients with essential hypertension: A randomized, double-blind, 8-week study

[4] Abdulrahman A Al-Majed, et al. Olmesartan

[5] Hermann Haller, et al. Olmesartan for the delay or prevention of microalbuminuria in type 2 diabetes

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Keywords: Olmesartan, Benicar, Olmetec supplier, Angiotensin Receptor, inhibitors, activators


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