L-159282

Names

[ CAS No. ]:
157263-00-8

[ Name ]:
L-159282

[Synonym ]:
mk-996
L-159282

Biological Activity

[Description]:

L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor
Research Areas >> Cardiovascular Disease

[In Vivo]

In the anesthetized chimpanzee, L-159282 (1 mg/kg, iv) produces 100% inhibition of the AII pressor response and is still active (52%) at 24 h. In aortic coarcted (high renin) rats, L-159282 (3 mg/kg, p.o.) reduces blood pressure to normotensive (< 120 mm Hg) levels without reflex tachycardia. This dose of L-159282 reduces blood pressure to approximately the same level as both losartan (3 mg/kg, p.o.) and enalapril (3 mg/kg, p.o.) in this model[1].

[References]

[1]. Kivlighn SD, et al. In vivo pharmacology of a novel AT1 selective angiotensin II receptor antagonist, MK-996. Am J Hypertens. 1995 Jan;8(1):58-66.


[Related Small Molecules]

Angiotensin II acetate salt | AVE 0991 | A 779 | Tranilast | PD123319 di(trifluoroacetate) | Telmisartan | Angiotensin II Receptor Ligand | Sacubitril/valsartan (LCZ696) | EMA401 | Fimasartan | (Val5)-Angiotensin II | RE 201 | C-Type Natriuretic Peptide (32-53) (human, porcine, rat) acetate salt

Chemical & Physical Properties

[ Density]:
1.27g/cm3

[ Molecular Formula ]:
C30H28N4O3S

[ Molecular Weight ]:
524.63300

[ Exact Mass ]:
524.18800

[ PSA ]:
105.82000

[ LogP ]:
7.10010

[ Index of Refraction ]:
1.654

[ Storage condition ]:
2-8℃


Related Compounds