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。
| 生物活性 | AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist ofGPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with apIC50of 8.13. AMG 837 hemicalcium could enhanceinsulinsecretion and lower glucose levels in rodents[1][2][3]. |
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体外研究
(In Vitro) | AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50of 142±20 nM on islets isolated from mice[1].
AMG 837 stimulates Ca2+flux with theEC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively[1].
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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 Cmaxof 1.4 μM[1].
| 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. |
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| 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. |
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