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CAS No. : 1000413-72-8
MCE 国际站:Fasiglifam
产品活性:Fasiglifam (TAK-875) 是一种有效的,可口服的,具有选择性的 GPR40 激动剂,EC50 值为 72 nM。
研究领域:GPCR/G Protein
作用靶点:Free Fatty Acid Receptor
In Vitro: Fasiglifam (TAK-875) (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. Fasiglifam (TAK-875) (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells. Fasiglifam (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.
In Vivo: Fasiglifam (TAK-875) (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. Fasiglifam (TAK-875) (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. Fasiglifam (TAK-875) at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, Fasiglifam (TAK-875) does not significantly alter insulin secretion in SD rats with normal fasting glucose levels .
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-diabetic Compound Library | Orally Active Compound Library | Chemical Probe Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | AS2034178 free base | GW-1100 | Ginsenoside Rb2 | Grifolic acid | GPR40/FFAR1 modulator 1 | GLPG0974 | GPR40 Activator 1 | DC260126 | AZ1729 | GPR120 Agonist 1 | TUG-770 | Fezagepras | GPR120 Agonist 3 | HWL-088 | GPR40 agonist 4 | GPR40 Agonist 2 | GPR40 agonist 6 | AH-7614 | AMG 837 sodium salt | LY2922470 | AM-1638 | TP-051 | TUG-469 | TUG-1375 | GPR120 modulator 2 | BMS-986118 | LY2881835
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货号: HY-10480
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