A potent AT1 receptor antagonist linked to an NO-donor
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NO-Losartan A

Item No. 10006456

Technical Information
Formal Name
[2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazol-5-yl] methyl ester
CAS Number
791122-48-0
Molecular Formula
C30H28ClN7O5
Formula Weight
Purity
≥97%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH7.2)(1:5): .5 mg/ml
SMILES
CCCCc1nc(Cl)c(COC(=O)c2cccc(CO[N](=O)O)c2)n1Cc1ccc(cc1)c1ccccc1c1nnn[nH]1
InChi Code
InChI=1S/C30H28ClN7O5/c1-2-3-11-27-32-28(31)26(19-42-30(39)23-8-6-7-21(16-23)18-43-38(40)41)37(27)17-20-12-14-22(15-13-20)24-9-4-5-10-25(24)29-33-35-36-34-29/h4-10,12-16H,2-3,11,17-19H2,1H3,(H,33,34,35,36)
InChi Key
MWJCPZGVGOVWQZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Losartan is a mammalian AT1 receptor antagonist with a Ki value of 5-20 nM.1 In humans, losartan effectively controls hypertension while protecting renal function.2 Nitric oxide (NO) causes vasodilation and also inhibits platelet and neutrophil aggregation in the endothelium.3,4 NO-losartan A possesses similar anti-hypertensive effects to losartan, with the addition of the vasodilating effects of NO release.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ji, H., Leung, M., Zhang, Y., et alDifferential structural requirements for specific binding of nonpeptide and peptide antagonists to the AT1 angiotensin receptor. Identification of amino acid residues that determine binding of the antihypertensive drug losartan. The Journal of Biological Chemisty 269(24), 16533-16536 (1994).

    2. Caruso, D., D'Avino, M., Acampora, C., et alEffects of losartan and chlorthalidone on blood pressure and renal vascular resistance index in non-diabetic patients with essential hypertension and normal renal functions. J. Cardiovasc. Pharmacol. 44(5), 520-524 (2004).

    3. Moncada, S., and Higgs, A. The L-arginine-nitric oxide pathway. N. Engl. J. Med. 329, 2002-2012 (1993).

    4. Loscalzo, J., and Welch, G. Nitric oxide and its role in the cardiovascular system. Prog. Cardiovasc. Dis. 38, 87-103 (1995).

    5. Breschi, M.C., Calderone, V., Digiacomo, M., et alNO-sartans: A new class of pharmacodynamic hybrids as cardiovascular drugs. J. Med. Chem. 47, 5597-5600 (2004).