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Fasiglifam(TAK-875) Hemihydrate

Fasiglifam(TAK-875) Hemihydrate

ArtNr	S2637-200
Hersteller	Selleckchem
CAS-Nr.	1374598-80-7
Menge	200 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Kategorie	Metabolism Diabetes Glucose Homeostasis Cholesterol & Lipid Metabolism Regulation of Appetite Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
Smiles	CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.CC1=CC(=CC(=C1C2=CC=CC(=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	GPR40,GPR
Similar products	TAK-875
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	533, 63
Administration	Orally
Animal Models	Female Wistar fatty rats subjected to oral glucose tolerance test
Clinical Trials	A Phase III study of TAK-875 in adults with type 2 diabetes and cardiovascular disease or risk factors for cardiovascular disease is currently ongoing.
Dosages	ca.3 mg/kg
Formulation	Formulated in 0.5% methylcellulose
IC50	14 nM (EC50) [1], 14 nM (EC50) [1], 14 nM (EC50) [1], 14 nM (EC50) [1], 14 nM (EC50) [1], 14 nM (EC50) [1]
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 uM. [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 uM. Neither TAK-875 nor oleic acid elicits an IP response in control CHO cells devoid of hGPR40. Consistent with the activation of the Gqalpha-mediated signaling pathway, TAK-875 augments glucose-dependent insulin secretion in pancreatic beta cells. Prolonged stimulation of GPR40/FFA1 by TAK-875 does not cause pancreatic beta 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]
Kinase Assay	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 ug/mL fluorescent calcium indicator Fluo 4-AM, 2.5 mM probenecid and 0.1% fatty acid-free BSA) for 60 minutes at 37 C. 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.
Solubility (25C)	DMSO 105 mg/mL, Water <1 mg/mL, Ethanol 9 mg/mL
Information	Fasiglifam(TAK-875) Hemihydrate is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
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
Features	More potent at activating hGPR40 than oleic acid

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S2637-200-datasheet.pdf

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