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Fasiglifam(TAK-875)

Names

[ CAS No. ]:
1374598-80-7

[ Name ]:
Fasiglifam(TAK-875)

[Synonym ]:
(3S)-6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy) biphenyl-3-yl)methoxy)-2,3-dihydro-l-benzofuran-3-yl)acetic acid hemihydrate
(3S)-6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy) biphenyl-3-yl)methoxy)-2,3-dihydro-l-benzofuran-3-yl)acetic acid hydrate
Fasiglifam hemihydrate
UNII-8LDT91CH8A
3-Benzofuranacetic acid,6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)(1,1'-biphenyl)-3-yl)methoxy)-2,3-dihydro-,hydrate (2:1),(3S)
TAK875

Biological Activity

[Description]:

Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPR40
Research Areas >> Metabolic Disease

[Target]

EC50: 72 nM (GPR40)[1]


[References]

[1]. Tsujihata Y,et al. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.J Pharmacol Exp  

[2]. Yoshiyuki Tsujihata, et al. TAK-875, an Orally Available GPR40/FFA1 Agonist Enhances Glucose-Dependent Insulin Secretion and Improves Both Postprandial and Fasting Hyperglycemia in Type 2 Diabetic Rats. JPET July 13, 2011

[3]. Nagatake T, et al. 17,18-EpETE-GPR40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques. J Allergy Clin Immunol. 2017 Dec 26. pii: S0091-6749(17)32949-4.  

Chemical & Physical Properties

[ Molecular Formula ]:
C29H33O7.5S

[ Molecular Weight ]:
533.63

[ Exact Mass ]:
1066.38000

[ PSA ]:
224.25000

[ LogP ]:
12.72450

[ Storage condition ]:
-20℃

Related Compounds