Catalog No.S2637

TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.

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TAK-875 Chemical Structure

TAK-875 Chemical Structure
Molecular Weight: 533.63

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Product Description

Biological Activity

Description TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
Targets GPR40 [1]
(CHO cells expressing human GPR40)
IC50 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]
Features More potent at activating hGPR40 than oleic acid.

Protocol(Only for Reference)

Kinase Assay: [1]

Ca influx activity of CHO cells expressing human GPR40 (FLIPR assay) CHO cells stably expressing human GPR40 are plated and incubated overnight in 5% CO2 at 37 °C. Then, cells are incubated in loading buffer (recording medium containing 2.5 μg/mL fluorescent calcium indicator Fluo 4-AM, 2.5 mM probenecid and 0.1% fatty acid-free BSA) for 60 minutes at 37 ºC. Various concentrations of TAK-875 are added into the cells and increase of the intracellular Ca2+ concentration after addition is monitored by FLIPR Tsystem for 90 seconds. EC50 value of TAK-875 is obtained with Prism 5 software.

Animal Study: [1]

Animal Models Female Wistar fatty rats subjected to oral glucose tolerance test
Formulation Formulated in 0.5% methylcellulose
Dosages ~3 mg/kg
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[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.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT01834274 Terminated Diabetes Mellitus, Type 2 Takeda June 2013 Phase 3
NCT01829464 Terminated Diabetes Takeda May 2013 Phase 3
NCT01829477 Terminated Diabetes Mellitus, Type 2 Takeda April 2013 Phase 3
NCT01647542 Terminated Type 2 Diabetes Mellitus Takeda October 2012 Phase 3
NCT01609582 Terminated Type 2 Diabetes|Cardiovascular Disease Takeda June 2012 Phase 3

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Chemical Information

Download TAK-875 SDF
Molecular Weight (MW) 533.63


CAS No. 1374598-80-7
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (187.39 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% CMC+0.25% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name [(3S)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphe-nyl-3-yl}meth-oxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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