1259389-38-2

生物活性靶点体外研究体内研究 1259389-38-2 试剂级价格

1259389-38-2

CAS号:1259389-38-2
英文名:AMG 837 (calciuM hydrate)
中文名:1259389-38-2
CBNumber:CB32715608
分子式:C26H25CaF3O4
分子量:498.56
MOL File:1259389-38-2.mol

1259389-38-2化学性质

储存条件 :Store at -20°C
溶解度 :DMSO: ≥ 42 mg/mL (92.22 mM)
形态 :Solid
颜色 :White to off-white

1259389-38-2性质、用途与生产工艺

生物活性 AMG 837 calcium hydrate 是 GPR40/FFA1 的有效的、具有口服活性的部分激动剂，抑制 [3H]AMG 837 与人类 FFA1 受体的特异性结合， pIC50 值为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。
靶点

pIC50: 8.13 (FFA1)
体外研究

AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC ₅₀ of 142±20 nM on islets isolated from mice.
AMG 837 stimulates Ca ²⁺ flux with the EC ₅₀ s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.

体内研究

AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo.
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats.
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma C _max of 1.4 µM.

Animal Model:	8-week old Zucker Fatty Rats
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	Oral gavage once daily for 21 days
Result:	Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively. Increased insulin levels in the mid- and high-dose groups. Not affected body weights during the 21-day treatment.

Animal Model:	8-week old Sprague-Dawley rats
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	A single p.o. administration
Result:	Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.