NO-LOSARTAN A Chemical Properties

Boiling point:

818.4±75.0 °C(Predicted)

Density 

1.39±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH7.2)(1:5): .5 mg/ml

form 

A crystalline solid

pka

4.16±0.10(Predicted)

NO-LOSARTAN A Usage And Synthesis

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 K_i value 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

References

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(10 Pt 2),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(5),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).
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).

NO-LOSARTAN A(791122-48-0)Related Product Information

• Losartan Carboxaldehyde
• O-Acetyl Losartan
• Losartan potassium
• Losartan potassium
• Losartan Impurity 7
• Losartan N2-Glucuronide
• Losartan-d3 Carboxylic Acid
• LOSARTAN-D4
• N-Trityl Losartan Isomer
• Trityl losartan
• Losartan Methyl Ether
• N,O-Ditrityl Losartan
• N-Trityl Losartan IsoMer
• Losartan potassium (50 MG)
• (2-BUTYL-5-CHLORO-1H-IMIDAZOL-4-YL)METHANOL
• Losartan
• (5-CHLORO-2-ETHYL-1H-IMIDAZOL-4-YL)-METHANOL
• NO-LOSARTAN A