1374598-80-7

1374598-80-7 structure

Name: Fasiglifam(TAK-875)
Chemical Name: 2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid,hydrate
CAS Number: 1374598-80-7
Molecular Formula: C₂₉H₃₃O_7.5S
Molecular Weight: 533.63
Catalog: Biochemical Inhibitor Endocrinology & Hormones GPR agonist
Create Date: 2018-12-24 18:29:04
Modify Date: 2024-01-03 18:29:51
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].

Name	2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid,hydrate
Synonyms	(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

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.