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TAK-875 Hemihydrate

Catalog No. T2351L CAS 1374598-80-7

Synonyms: Fasiglifam, TAK-875

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

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TAK-875 Hemihydrate, CAS 1374598-80-7

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid.
Targets&IC50	GPR40:14 nM(EC50)
In vitro	TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM. TAK-875 displays weaker affinity toward the rat GPR40 receptor with Ki of 140 nM. TAK-875 displays excellent selectivity, as TAK-875 has little agonist potency to other members of the FFA receptor family with EC50 of >10 μM. [1] TAK-875 treatment induces a concentration-dependent increase in intracellular IP production in CHO-hGPR40 with EC50 of 72 nM, more potently than that of endogenous ligand agonist oleic acid which requires much higher ligand concentrations to activate the receptor with EC50 of 29.9 μM. Neither TAK-875 nor oleic acid elicits an IP response in control CHO cells devoid of hGPR40. Consistent with the activation of the Gqα-mediated signaling pathway, TAK-875 augments glucose-dependent insulin secretion in pancreatic β cells. Prolonged stimulation of GPR40/FFA1 by TAK-875 does not cause pancreatic β Cell dysfunction or induction of apoptosis. [2]
In vivo	In a rat model of diabetes, single oral dosing of TAK-875 at 0.3-3 mg/kg reduces the blood glucose excursion and augments insulin secretion during an oral glucose tolerance test, when TAK-875 is administered 1 hour before an oral glucose challenge. [1] In type 2 diabetic N-STZ-1.5 rats, administration of TAK-875 (1-10 mg/kg p.o.) shows a clear improvement in glucose tolerance and augments insulin secretion. Additionally, TAK-875 (10 mg/kg, p.o.) significantly augments plasma insulin levels and reduces fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhances insulin secretion nor causes hypoglycemia even at 30 mg/kg. [2]

Synonyms	Fasiglifam, TAK-875
Molecular Weight	1067.27
Formula	C58H66O15S2
CAS No.	1374598-80-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 93 mg/mL (174.3 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Nobuyuki Negoro, et al. ACS Med Chem Lett, 2010, 1(6), 290-294. 2. Tsujihata Y, et al. J Pharmacol Exp Ther, 2011, 339(1), 228-237.

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Keywords

TAK-875 Hemihydrate 1374598-80-7 G蛋白偶联受体内分泌与激素 GPR TAK 875 Hemihydrate Fasiglifam TAK-875 TAK875 Hemihydrate Inhibitor inhibitor inhibit

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