A4082-25mg | Olmesartan medoxomil [144689-63-4] Biotrend

Background

Olmesartan medoxomil, the medoxomil ester of olmesartan, is novel and oral antagonist of angiotensin II TYPE-1 receptor (AT₁ receptor) with an inhibition constant IC₅₀ of 33 nmol/L. Through oral administration, olmesartan medoxomil is rapidly absorbed by the gastrointestinal tract converting to its active metabolite olmesartan, whose inhibition constant IC₅₀ towards AT₁ receptor is 8 nmol/L. The esterification of olmesartan with medoxomil moiety is just to improve its water solubility (from 4.5% to 28.6%). Olmesartan medoxomil is used for the treatment of hypertension, in which olmesartan dose-dependently reduces the blood pressure through arterial vasodilation and reducing sodium retention.

Reference

HR Brunner. The new oral angiotensin II antagonist olmesartan medoxomil: a concise overview. Journal of Human Hypertension (2002) 16 (Suppl 2), S13-S16

Shailesh T. Prajapati, Hitesh H. Bulchandani, Dashrath M. Patel, Suresh K. Dumaniya and Chhaganbhai N. Patel. Formulation and evaluation of liquisolid compacts for olmesartan medoxomil. Journal of Drug Delivery 2013.

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	558.6
Cas No.	144689-63-4
Formula	C₂₉H₃₀N₆O₆
Synonyms	Benicar, Benevas, Olvance
Solubility	≥21.1 mg/mL in DMSO; insoluble in H2O; ≥4.6 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name	(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
SDF	Download SDF
Canonical SMILES	CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)OCC5=C(OC(=O)O5)C)C(C)(C)O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.