2. GPCR/G Protein
  3. Free Fatty Acid Receptor
  4. AMG 837 hemicalcium

AMG 837 hemicalcium 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 hemicalcium 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。

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AMG 837 hemicalcium Chemical Structure

AMG 837 hemicalcium Chemical Structure

CAS No. : 1291087-14-3

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AMG 837 hemicalcium 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents[1][2][3].

IC50 & Target

pIC50: 8.13 (FFA1)[3]
体外研究
(In Vitro)

AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice[1].
AMG 837 stimulates Ca2+ flux with the EC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AMG 837 hemicalcium 相关抗体:
体内研究
(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[1].
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[1].
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma Cmax of 1.4 µM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-week old Zucker Fatty Rats[1]
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[1]
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.
分子量

457.48

Formula

C26H21F3O3.1/2Ca
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AMG 837 hemicalcium 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG 837 hemicalcium1291087-14-3Free Fatty Acid ReceptorFFARGPR40FFA1insulinglucoseInhibitorinhibitorinhibit

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