Tasosartan

Names

[ Name ]:
Tasosartan

[Synonym ]:
2,4-dimethyl-8-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one
ANA-756
2,4-Dimethyl-8-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one
Pyrido[2,3-d]pyrimidin-7(6H)-one, 5,8-dihydro-2,4-dimethyl-8-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
2,4-Dimethyl-8-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one
2,4-dimethyl-5,6,8-trihydro-8-[[2'-(1H-tetrazol-5-yl)[1,1-biphenyl]-4-yl]methyl]-7H-pyrido[2,3-d]pyrimidin-7-one
2,4-dimethyl-8-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one
8-[2'-(1H-tetrazol-5-yl)-biphenyl-4-yl-methyl]-2,4-dimethyl-5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one
Tasosartan (USAN/INN)
WAY-ANA-756
S1539_Selleck
Verdia
tasosartan

Biological Activity

[Description]:

Tasosartan is a long-acting angiotensin II (AngII) receptor antagonist.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Research Areas >> Cardiovascular Disease

[Target]

Angiotensin II (AngII) receptor[1]

[In Vitro]

Tasosartan is an orally active nonpeptide AngII antagonist that has demonstrates specific and selective AT1 receptor antagonistic activity in vitro. IC50 for inhibition of specific binding of 125I-AngII to rat adrenal membrane in the absence of proteins in binding buffer is 1.2±0.6 nM[1].

[In Vivo]

Administration of Tasosartan at doses of 1.0 and 3.0 mg/kg (iv) significantly (p<0.05) attenuates the pressor response to angiotensin-II in rats[2].

[Animal admin]

Rats[2] Pressor response to angiotensin-II administration in four groups of rats (n=3-5 each, weighing 343±8 g). Each rat is subjected to four separate bolus injections of angiotensin-II following the introduction of either the vehicle or graded doses of Tasosartan (0.3, 1.0, or 3.0 mg/kg, iv)[2].

[References]

[1]. Maillard MP, et al. Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54.

[2]. Elokdah HM, et al. Novel human metabolites of the angiotensin-II antagonist Tasosartan and their pharmacological effects. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1967-71.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
759.4±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₁N₇O

[ Molecular Weight ]:
411.459

[ Flash Point ]:
413.1±35.7 °C

[ Exact Mass ]:
411.180756

[ PSA ]:
100.55000

[ LogP ]:
2.62

[ Vapour Pressure ]:
0.0±2.6 mmHg at 25°C

[ Index of Refraction ]:
1.665

[ Storage condition ]:
2-8℃

Tasosartan

Names

Biological Activity

Chemical & Physical Properties

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream