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Fasiglifam

Catalog No. T2351 CAS 1000413-72-8

Synonyms: TAK875

Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.

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Fasiglifam, CAS 1000413-72-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 164.00
25 mg	In stock	$ 298.00
50 mg	In stock	$ 494.00
100 mg	In stock	$ 597.00
200 mg	In stock	$ 864.00
1 mL * 10 mM (in DMSO)	In stock	$ 126.00

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Purity: 99.82%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.
Targets&IC50	FFA1/GPR40:72 nM.(EC50)
In vitro	TAK-875 (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM.?TAK-875 (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells[1]. 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[2].
In vivo	Administered orally, TAK-875 at a dose of 10 mg/kg enhances plasma insulin levels in ZDF rats. At a higher dosage of 30 mg/kg, it ameliorates fasting hyperglycemia without impacting fasting normoglycemia. Interestingly, a 3- to 10-fold increase in the dose that ameliorated glucose tolerance in diabetic models, specifically 30 mg/kg, does not modify fasting glucose levels in SD rats maintaining normal glucose homeostasis. Similarly, TAK-875 does not significantly affect insulin secretion in SD rats demonstrating normal fasting glucose levels [1].
Kinase Assay	INS-1 832/13 cells are suspended in RPMI medium containing 11 mM glucose and the supplements described above. These cells are seeded at a density of 2×104?cells/well in a 96-well black plate coated with poly-D-lysine, 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) is added to the plate with 1% BSA and 0.1% DMSO, followed by culture for 72 h. After the culture, caspase 3/7 activity is measured with the Apo-one homogeneous caspase 3/7 assay according to the manufacturer's instructions. Fluorescence intensity is measured at an excitation of 485 nm and an emission at 535 nm.
Cell Research	TAK-875 is dissolved in 1% BSA and 0.1% DMSO.? INS-1 832/13 cells are suspended in RPMI medium and seeded in a 96-well plate at a density of 2×104 cells/well; 1% BSA and 0.1% DMSO alone (control), palmitic acid (10, 100, and 1000 μM), oleic acid (10, 100, and 1000 μM), or TAK-875 (1, 10, and 100 μM) is added to the plate. After 72-h culture, medium is discarded, and cells are preincubated for 2 h with KRBH containing 1 mM glucose and 0.2% BSA at 37°C. After discarding of the preincubation buffer, KRBH containing 1 or 20 mM glucose and 0.2% BSA is added, and the plate is further incubated for 2 h. The insulin concentration in the supernatant is measured as described above. To measure intracellular insulin content, INS-1 832/13 cells are exposed to 1% BSA and 0.1% DMSO alone (control), palmitic acid (1000 μM), oleic acid (1000 μM), or TAK-875 (100 μM) with 1% BSA and 0.1% DMSO. After incubation, cells are washed once with phosphate-buffered saline, and acid-ethanol solution is added to each well, followed by sonication on ice. Intracellular insulin is extracted by overnight incubation at ?30°C, followed by separation of supernatant by centrifugation at 12,000 rpm×5 min at 4°C.

Synonyms	TAK875
Molecular Weight	524.63
Formula	C29H32O7S
CAS No.	1000413-72-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Metabolism Disease Compound Library Clinical Compound Library Target-Focused Phenotypic Screening Library Anti-Diabetic Compound Library Bioactive Compounds Library Max ReFRAME Related Library

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Keywords

Fasiglifam 1000413-72-8 Endocrinology/Hormones GPCR/G Protein GPR TAK 875 inhibit FFAR Inhibitor TAK-875 Free Fatty Acid Receptor TAK875 inhibitor

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