Fasiglifam

CAS号

1000413-72-8

分子式

C29H32O7S

主要靶点

GPR

仅限科研使用

Cat No : CM04307

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Synonyms

FFAR|Fasiglifam|Free Fatty Acid Receptor|GPR40|GPR40(FFA1)|inhibit|Inhibitor|TAK 875|TAK-875|TAK875



产品信息

CAS号 1000413-72-8
分子式 C29H32O7S
主要靶点 GPR
主要通路 G 蛋白偶联受体|内分泌与激素
分子量 524.63
纯度 99.82%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 FFAR|Fasiglifam|Free Fatty Acid Receptor|GPR40|GPR40(FFA1)|inhibit|Inhibitor|TAK 875|TAK-875|TAK875

靶点活性

FFA1/GPR40:72 nM.(EC50)

体内活性

Fasiglifam(10 mg/kg,p.o.)在ZDF大鼠中提高了血浆胰岛素水平。Fasiglifam(30 mg/kg,p.o.)改善了空腹高血糖,而不影响空腹正常血糖。与改善糖尿病大鼠葡萄糖耐量的剂量相比,Fasiglifam在30 mg/kg的剂量,即3至10倍较高剂量,不会改变具有正常葡萄糖稳态的SD大鼠的空腹血糖水平。同样,Fasiglifam在具有正常空腹血糖水平的SD大鼠中并未显著改变胰岛素分泌[1]。

体外活性

Fasiglifam在CHO-hGPR40細胞中以濃度依賴的方式增加細胞內IP產量,其EC50值為0.072 μM。在CHO細胞中,Fasiglifam以濃度範圍0.1-10 μM呈濃度依賴性提高細胞內IP產量[1]。此外,Fasiglifam在3-30 μM的濃度範圍內,依賴於濃度地增加[Ca2+]i。在10 mM葡萄糖存在的環境下,Fasiglifam以0.001-10 μM的濃度範圍內,依賴於濃度地促進INS-1 833/15細胞中胰島素的分泌[2]。

溶解度

DMSO:50 mg/mL (95.31 mM)

细胞实验

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.

参考文献

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

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