Tasosartan
Basic information
- CAS
145733-36-4- Standard SMILES
Cc1nc(C)c2c(n1)N(Cc1ccc(-c3ccccc3-c3nn[nH]n3)cc1)C(=O)CC2- InChIKey
ADXGNEYLLLSOAR-UHFFFAOYSA-N- Molecular formula
- C23H21N7O
- Average molar mass
- 411.5 g/mol
- Monoisotopic mass
- 411.18075832
Overview
Tasosartan is a member of biphenyls.
Names & identifiers
- Preferred name
- Tasosartan
- IUPAC
- 2,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-one
- English name
- Tasosartan
- Molecular formula
- C23H21N7O
- Molecular weight
- 411.46
Names & synonyms
TASOSARTAN145733-36-4ANA-756WAY-ANA-756taso-sartanANA75648G92V856HDTXSID401631482,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[6,5-d]pyrimidin-7-one5,8-dihydro-2,4-dimethyl-8-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)pyrido(2,3-d)pyrimidin-7(6H)-onetasosartanum2,4-dimethyl-8-((4-(2-(2H-1,2,3,4-tetrazol-5-yl)phenyl)phenyl)methyl)-5H,6H,7H,8H-pyrido(2,3-d)pyrimidin-7-one
Show more names
VerdiaCS-160DB01349AC1Q6LAAAC1L1U5XTasosartaS1539_Selleck
2,4-dimethyl-8-((4-(2-(2H-tetrazol-5-yl)phenyl)phenyl)methyl)-5,6-dihydropyrido(6,5-d)pyrimidin-7-one2,4-dimethyl-8-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-5H,6H,7H,8H-pyrido[2,3-d]pyrimidin-7-oneRefChem:891190DTXCID3085639C09CA052,4-dimethyl-8-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-5,6-dihydropyrido[2,3-d]pyrimidin-7-oneCHEMBL4321625,8-dihydro-2,4-dimethyl-8-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]pyrido[2,3-d]pyrimidin-7(6H)-one
Database identifiers
Properties
Computed structural properties
- XLogP
- 3
- Topological polar surface area
- 101 Ų
- Hydrogen bond donors
- 1
- Hydrogen bond acceptors
- 6
- Rotatable bonds
- 4
- Heavy atoms
- 31
- Formal charge
- 0
- Complexity
- 625
Experimental & physicochemical properties
DrugsPharmaceuticals -> Listed in ZINC15
Solubility3.25e-02 g/L
Physical DescriptionSolid
Physicochemical properties
- Melting point
- 197 · 197-199°
- Boiling point
- 759.4 · 759.4±70.0 °C(Predicted)
- Density
- 1.328 · 1.328±0.06 g/cm3(Predicted)
- storage temp.
- 2 · 2-8°C
- solubility
- DMSO (Slightly), Methanol (Slightly, Sonicated)
- form
- Solid
- pka
- 4.16 · 4.16±0.10(Predicted)
- color
- White to Off-White
- FDA UNII
- 48 G92V856H · 48G92V856H
- ATC code
- 9 CA05 · C09CA05
- Symbol(GHS)
- 7 · GHS07
Safety & regulation
Safety information is for reference only and does not replace the supplier’s Safety Data Sheet (SDS), applicable regulations, or professional assessment.
Toxicology
Drug Induced Liver Injury
Drug Induced Liver Injury Rank (DILIrank 2.0)
Tasosartan
vMost-DILI-concern
8
Discontinued
DOI:10.1016/j.drudis.2016.02.015
Safety data
- Signal word
- Warning
- Symbol(GHS)
- GHS07
- Hazard statements
- H315-H319-H335
- Precautionary statements
- P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501
Chemistry & industry
Pharmacology
ATC Code
C - Cardiovascular system
QC - Cardiovascular system
Pharmacodynamics
By blocking the angiotensin II (AT1) receptor, the drug ultimately causes vasodilation, reduced secretion of vasopressin (ADH), reduced production and secretion of aldosterone, amongst other actions leading to the combined effect of a reduction of blood pressure.
Mechanism of Action
Tasosartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. AT1 receptor antagonists avoid the nonspecificity of the Ang I converting enzyme (ACE) inhibitors.
Metabolism/MetabolitesTasosartan has known human metabolites that include enoltasosartan.
MeSH Pharmacological ClassificationAgents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS.
Cellular LocationsMembrane
Applications
UsesAntihypertensive.
UsesTasosartan is an angiotensin II receptor antagonist.
Upstream & downstream products
Upstream raw materials
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Compound notes
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