CAS 145733-36-4|Tasosartan

Introduction:Basic information about CAS 145733-36-4|Tasosartan, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameTasosartan
CAS Number145733-36-4Molecular Weight411.459
Density1.3±0.1 g/cm3Boiling Point759.4±70.0 °C at 760 mmHg
Molecular FormulaC23H21N7OMelting Point/
MSDS/Flash Point413.1±35.7 °C

Names

Name2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one
SynonymMore Synonyms

Tasosartan BiologicalActivity

DescriptionTasosartan is a long-acting angiotensin II (AngII) receptor antagonist.
Related CatalogSignaling Pathways >>GPCR/G Protein >>Angiotensin ReceptorResearch Areas >>Cardiovascular Disease
Target

Angiotensin II (AngII) receptor[1]

In VitroTasosartan 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 VivoAdministration 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 AdminRats[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.

Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point759.4±70.0 °C at 760 mmHg
Molecular FormulaC23H21N7O
Molecular Weight411.459
Flash Point413.1±35.7 °C
Exact Mass411.180756
PSA100.55000
LogP2.62
Vapour Pressure0.0±2.6 mmHg at 25°C
Index of Refraction1.665
InChIKeyADXGNEYLLLSOAR-UHFFFAOYSA-N
SMILESCc1nc(C)c2c(n1)N(Cc1ccc(-c3ccccc3-c3nn[nH]n3)cc1)C(=O)CC2
Storage condition2-8℃

Synonyms

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
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