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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

NO-Losartan A

Cayman Chemical Item Number 10006456

(CAS 791122-48-0)

NO-Losartan A (CAS 791122-48-0)

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Description

Angiotensin II is a hormone that plays an important role in regulating blood pressure.1 Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1) receptor.2 Losartan is a mammalian AT1 receptor antagonist with a Ki of 5-20 nM.3 In humans, losartan effectively controls hypertension while protecting renal function.4 Nitric oxide (NO) causes vasodilation and also inhibits platelet and neutrophil aggregation in the endothelium.5,6 NO-losartan A possesses similar anti-hypertensive effects to losartan, with the addition of the vasodilating effects of NO release.7

1 Ortiz, M.C., Sanabria, E., Manriquez, M.C., et al. Role of endothelin and isoprostanes in slow pressor responses to angiotensin II. Hypertension 37(2) 505-511 (2001).

2 Schiffrin, E.L. Beyond blood pressure: The endothelium and atherosclerosis progression. Am J Hypertens 15 115S-122S (2002).

3 Ji, H., Leung, M., Zhang, Y., et al. Differential 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. J Biol Chem 269(24) 16533-16536 (1994).

4 Caruso, D., D'Avino, M., Acampora, C., et al. Effects 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 44 520-524 (2004).

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

6 Loscalzo, J., and Welch, G. Nitric oxide and its role in the cardiovascular system. Prog Cardiovasc Dis 38 87-103 (1995 Sep 1).

7 Breschi, M.C., Calderone, V., Digiacomo, M., et al. NO-sartans: A new class of pharmacodynamic hybrids as cardiovascular drugs. J Med Chem 47 5597-5600 (2004).

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 602.0
Formulation A crystalline solid
Purity >97%
Stability 2 years
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES
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CCCCc1nc(Cl)​c(COC(=O)​c2cccc(CO[N]​(=O)​O)​c2)​n1Cc1ccc(cc1)​c1ccccc1c1nnn[nH]​1

Background Reading

Breschi, M.C., Calderone, V., Digiacomo, M., et al. NO-sartans: A new class of pharmacodynamic hybrids as cardiovascular drugs. J Med Chem 47 5597-5600 (2004).

Loscalzo, J., and Welch, G. Nitric oxide and its role in the cardiovascular system. Prog Cardiovasc Dis 38 87-103 (1995 Sep 1).

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

Caruso, D., D'Avino, M., Acampora, C., et al. Effects 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 44 520-524 (2004).

Ortiz, M.C., Sanabria, E., Manriquez, M.C., et al. Role of endothelin and isoprostanes in slow pressor responses to angiotensin II. Hypertension 37(2) 505-511 (2001).

Ji, H., Leung, M., Zhang, Y., et al. Differential 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. J Biol Chem 269(24) 16533-16536 (1994).

Schiffrin, E.L. Beyond blood pressure: The endothelium and atherosclerosis progression. Am J Hypertens 15 115S-122S (2002).

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Size Price Quantity Subtotal
1 mg $14.00 $0.00
5 mg $63.00 $0.00
10 mg $112.00 $0.00
50 mg $490.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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