TAK875 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO: 100 mg/mL (187.40 mM);Ethanol: Insoluble

Water Solubility 

Water: Insoluble

InChI

InChI=1S/2C29H32O7S.H2O/c2*1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24;/h2*4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31);1H2/t2*23-;/m11./s1

InChIKey

OJXYMYYDAVXPIK-IWKNALKQSA-N

SMILES

S(C([H])([H])[H])(C([H])([H])C([H])([H])C([H])([H])OC1C([H])=C(C([H])([H])[H])C(=C(C([H])([H])[H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])OC1C([H])=C([H])C2=C(C=1[H])OC([H])([H])[C@@]2([H])C([H])([H])C(=O)O[H])(=O)=O.S(C([H])([H])[H])(C([H])([H])C([H])([H])C([H])([H])OC1C([H])=C(C([H])([H])[H])C(=C(C([H])([H])[H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])OC1C([H])=C([H])C2=C(C=1[H])OC([H])([H])[C@@]2([H])C([H])([H])C(=O)O[H])(=O)=O.O([H])[H]

CAS DataBase Reference

1374598-80-7

TAK875 Usage And Synthesis

Characteristics

More potent at activating hGPR40 than oleic acid

Uses

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].

Biological Activity

TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.

target

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 DOI:10.1124/jpet.111.183772
[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. DOI:10.1016/j.jaci.2017.09.053

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