1259389-38-2
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- CAS号:
- 1259389-38-2
- 英文名:
- AMG 837 (calciuM hydrate)
- 英文别名:
- AMG 837 (calciuM hydrate);AMG-837 calcium salt hydrate;AMG-837 CALCIUM HYDRATE;AMG837 CALCIUM HYDRATE;AMG 837 calcium,FFAR,AMG 837 calcium hydrate,insulin,FFA1,Inhibitor,Free Fatty Acid Receptor,inhibit,glucose,GPR40
- 中文名:
- 1259389-38-2
- 中文别名:
- AMG 837氢氧化钙
- CBNumber:
- CB32715608
- 分子式:
- C26H25CaF3O4
- 分子量:
- 498.56
- MOL File:
- 1259389-38-2.mol
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1259389-38-2化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: ≥ 42 mg/mL (92.22 mM)
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1259389-38-2性质、用途与生产工艺
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。
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.
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.
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Animal Model:
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8-week old Zucker Fatty Rats
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Dosage:
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0.03, 0.1, 0.3 mg/kg
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Administration:
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Oral gavage once daily for 21 days
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Result:
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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.
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Animal Model:
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8-week old Sprague-Dawley rats
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Dosage:
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0.03, 0.1, 0.3 mg/kg
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Administration:
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A single p.o. administration
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Result:
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Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.
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1259389-38-2
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-13967B | AMG 837 calcium hydrate | | 1 mg | 380元 |
| 2024/04/30 | HY-13967B | 1259389-38-2
AMG 837 calcium hydrate | 1259389-38-2 | 5mg | 1000元 |
1259389-38-2, 1259389-38-2 相关搜索:
- AMG 837氢氧化钙
- 1259389-38-2
- AMG 837 calcium,FFAR,AMG 837 calcium hydrate,insulin,FFA1,Inhibitor,Free Fatty Acid Receptor,inhibit,glucose,GPR40
- AMG-837 calcium salt hydrate
- AMG-837 CALCIUM HYDRATE;AMG837 CALCIUM HYDRATE
- AMG 837 (calciuM hydrate)