TAK875 free base · Synonyms: Fasiglifam

Fasiglifam is a potent, selective and orally bioavailable GPR40 agonist.

For research use only. Not for human or veterinary use.

Target Free Fatty Acid Receptor

Research area Metabolic Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

TAK875 structure

CAS No.: 1000413-72-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 420.00	BP-01824-250mg	In stock	Get quote
500 mg	USD 620.00	BP-01824-500mg	In stock	Get quote
1 g	USD 920.00	BP-01824-1g	In stock	Get quote
5 g	Inquire	BP-01824-5g	In stock	Inquire

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Description

Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

Biological activity

In Vitro Fasiglifam (TAK-875) (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. Fasiglifam (TAK-875) (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells. Fasiglifam (TAK-875) (3-30 μM) concentration-dependently augments [Ca2+]i. In the presence of 10 mM glucose, TAK-875 (0.001-10 μM) dose-dependently stimulats insulin secretion from INS-1 833/15 cells. In Vivo Fasiglifam (TAK-875) (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. Fasiglifam (TAK-875) (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. Fasiglifam (TAK-875) at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, Fasiglifam (TAK-875) does not significantly alter insulin secretion in SD rats with normal fasting glucose levels.

Identifiers

SMILES: CC1=CC(OCCCS(C)(=O)=O)=CC(C)=C1C1=CC=CC(COC2=CC=C3[C@H](CC(O)=O)COC3=C2)=C1
InChIKey: BZCALJIHZVNMGJ-HSZRJFAPSA-N

Specifications

MW (average): 524.6250
Formula: C₂₉H₃₂O₇S
CAS No.: 1000413-72-8
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

[4]. Urano Y, et al. Comparative hepatic transcriptome analyses revealed possible pathogenic mechanisms of fasiglifam (TAK-875)-induced acute liver injury in mice. Chem Biol Interact. 2018 Sep 20;296:185-197.

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