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Cat. No. M2054
TAK-875 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 140 In stock
10mg USD 240 In stock
50mg USD 550 In stock
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Quality Control
Biological Activity

TAK-875 is a novel, orally available, selective GPR40 agonist. TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM. TAK-875 enhanced glucose-induced insulin secretion in a glucose-dependent manner in both human and rat islets. In rat insulinoma INS-1 833/15 cells, TAK-875 increased intracellular inositol monophosphate and calcium concentration, consistent with activation of the Gqα signaling pathway. In addition, TAK-875 (10 mg/kg, p.o.) significantly augmented plasma insulin levels and reduced fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhanced insulin secretion nor caused hypoglycemia even at 30 mg/kg. TAK-875 improves both postprandial and fasting hyperglycemia with a low risk of hypoglycemia and no evidence of β cell toxicity. TAK-875 significantly improved glycaemic control in patients with type 2 diabetes with minimum risk of hypoglycaemia.

Customer Product Validations & Biological Datas
Source Br J Pharmacol (2013). Figure 3. TAK-875
Method oral
Cell Lines ZL rats
Concentrations 3 mg/kg
Incubation Time 120 min
Results TAK-875 significantly enhanced insulin secretion before a glucose load (P ≤ 0.01) and tended to augment it at 10 min after glucose load, while metformin showed a trend towards reduce insulin release at 10 min
Cell Experiment
Cell lines INS-1 832/13 cells
Preparation method Measurement of Caspase 3/7 Activity. INS-1 832/13 cells were suspended in RPMI medium containing 11 mM glucose and the supplements described above. These cells were seeded at a density of 2 × 104 cells/well in a 96-well black plate coated with poly-D-lysine (BD BioCoat), and 1% BSA and 0.1% DMSO alone (control), palmitic acid (62.5, 125, 250, 500, and 1000 μM), oleic acid (62.5, 125, 250, 500, and 1000 μM), or TAK-875 (6.25, 12.5, 25, 50, and 100 μM) was added to the plate with 1% BSA and 0.1% DMSO, followed by culture for 72 h. After the culture, caspase 3/7 activity was measured with the Apo-one homogeneous caspase 3/7 assay (Promega, Madison, WI) according to the manufacturer's instructions. Fluorescence intensity was measured at an excitation of 485 nm and an emission at 535 nm.
Concentrations 6.25, 12.5, 25, 50, and 100 μM
Incubation time 72 h
Animal Experiment
Animal models Oral Glucose Tolerance Test and Effects on Fasting Normoglycemia and Hyperglycemia with N-STZ-1.5 rats
Formulation 0.5% methylcellulose
Dosages 10 and 30 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 533.63
Formula C29H32O7S.1/2H2O
CAS Number 1374598-80-7
Purity 99.43%
Solubility DMSO 100 mg/mL
Storage at -20°C

The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets.
Yashiro H, et al. J Pharmacol Exp Ther. 2012 Feb;340(2):483-9. PMID: 22106100.

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.
Tsujihata Y, et al. J Pharmacol Exp Ther. 2011 Oct;339(1):228-37. PMID: 21752941.

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Keywords: TAK-875 supplier, GPR, inhibitors

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