1259389-38-2
中文名称 | 1259389-38-2 |
---|---|
中文同义词 | AMG 837氢氧化钙 |
英文名称 | AMG 837 (calciuM hydrate) |
英文同义词 | AMG 837 (calciuM hydrate);AMG-837 CALCIUM HYDRATE;AMG837 CALCIUM HYDRATE;AMG-837 calcium salt hydrate;AMG 837 calcium,FFAR,AMG 837 calcium hydrate,insulin,FFA1,Inhibitor,Free Fatty Acid Receptor,inhibit,glucose,GPR40 |
CAS号 | 1259389-38-2 |
分子式 | C26H25CaF3O4 |
分子量 | 498.56 |
EINECS号 | |
相关类别 | |
Mol文件 | 1259389-38-2.mol |
结构式 |
1259389-38-2 性质
储存条件 | Store at -20°C |
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溶解度 | 二甲基亚砜:≥ 42 mg/mL(92.22 mM) |
形态 | 固体 |
颜色 | 白色至米白色 |
pIC50: 8.13 (FFA1)
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.
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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-13967B | AMG 837 calcium hydrate | 1 mg | 380元 | |
2024/08/19 | HY-13967B | 1259389-38-2 AMG 837 calcium hydrate | 1259389-38-2 | 5mg | 1000元 |