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Home   »   Product Pathways  »  GPR40  »  TAK-875

Products are for research use only. Not for human use. We do not sell to patients.

CS-0282 TAK-875

(Fasiglifam;TAK 875;TAK875)
Structure Price and Availability of    TAK-875
United States
Size Price Stock
2mg $90 In-stock Inquiry
5mg $120 In-stock
10mg $220 In-stock
50mg $500 In-stock
100mg $855 In-stock
200mg $1300 In-stock
500 mg Get quote
1 g Get quote
 Distributor In Japan:  フナコシ株式会社    電話番号:81-3-5684-1620   
Inquiry for price and availability only. Please place your order via our email or fax.
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  • Data Sheet
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TAK-875  M.Wt:  524.63
TAK-875  Formula: C29H32O7S
TAK-875  Solubility: DMSO: ≥ 158 mg/mL
TAK-875  Purity: >98%
TAK-875  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 1000413-72-8

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TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM. IC50 Value: 0.072 μM(EC50) Target: GPR40 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. 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. in vivo: 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.

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