An AT1 receptor antagonist and active metabolite of olmesartan medoxomil
Related Products
Labeled Version(s)
36324Olmesartan-d6
Pro-drug Form(s)
11614Olmesartan Medoxomil
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Olmesartan

Item No. 23412

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid
CAS Number
144689-24-7
Synonyms
  • CS 088
  • RNH 6270
Molecular Formula
C24H26N6O3
Formula Weight
446.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 0.2 mg/ml
SMILES
OC(C)(C)C1=C(C(O)=O)N(CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2)C(CCC)=N1
InChi Code
InChI=1S/C24H26N6O3/c1-4-7-19-25-21(24(2,3)33)20(23(31)32)30(19)14-15-10-12-16(13-11-15)17-8-5-6-9-18(17)22-26-28-29-27-22/h5-6,8-13,33H,4,7,14H2,1-3H3,(H,31,32)(H,26,27,28,29)
InChi Key
VTRAEEWXHOVJFV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Olmesartan is a non-peptide angiotensin II receptor 1 (AT1) antagonist (IC50 = 0.0077 µM for the bovine adrenal cortex receptor) and an active metabolite of olmesartan medoxomil (Item No. 11614).1 It is formed from olmesartan medoxomil by paraoxonase 1 (PON1) in human plasma.2 Olmesartan is selective for AT1 over AT2 (IC50 = >100 µM for the bovine cerebellar receptor). It reduces contraction of isolated guinea pig aorta induced by angiotensin II (Item No. 17150; pD2 = 9.9) but not phenylephrine (Item Nos. 17205 | 18619) or potassium chloride. Olmesartan (0.01 and 0.03 mg/kg, i.v.) reduces the angiotensin II-induced pressor response in conscious normotensive rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mizuno, M., Sada, T., Ikeda, M., et al. Pharmacology of CS-866, a novel nonpeptide angiotensin II receptor antagonist. Eur. J. Pharmacol. 285(2), 181-188 (1995).

    2. Ishizuka, T., Fujimori, I., Nishida, A., et al. Paraoxonase 1 as a major bioactivating hydrolase for olmesartan medoxomil in human blood circulation: Molecular identification and contribution to plasma metabolism. Drug Metab. Dispos. 40(2), 374-380 (2012).