| 产品编号 | D50882 |
| 英文名称 | TAK-875 (Fasiglifam) |
| 中文名称 | |
| 别 名 | GPR40激动剂 |
| 克 隆 号 | |
| CAS | 1374598-80-7 |
| 理论分子量 | 1067.27 kDa |
| 检测分子量 | |
| 性 状 | Lyophilized |
| 保存条件 | Store in dry, dark place for one year. |
| 注意事项 | This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications. |
| 产品介绍 |
TAK-875 (Fasiglifam) is the potent, selective and orally bioavailable partial GPR40 agonist with an EC50 ~14 nM. It has binding affinity to the human GPR40 receptor with Ki of 38 nM and the rat GPR40 receptor with Ki of 140 nM. TAK-875 has no agonist potency to other members of the FFA receptor family with EC50 >10 μM. The 2.3 ANG resolution co-complex structure of hGPR40-TAK-875 reveals a unique binding mode of TAK-875 and suggests that entry to the non-canonical binding pocket most probably occurs via the lipid bilayer. Consistent with the activation of the Gqα-mediated signaling pathway, TAK-875 augments glucose-dependent insulin secretion in pancreatic β cells. Prolonged stimulation of GPR40/FFA1 by TAK-875 does not cause pancreatic β Cell dysfunction or induction of apoptosis. Termination phase III development of TAK-875 (Fasiglifam) for the potential treatment of type-2 diabetes mellitus was announced in 2013 due to concerns about liver safety. |
| 1、抗体溶解方法 | |
| 2、抗体修复方式 | |
| 3、常用试剂的配制 | |
| 4、免疫组化操作步骤 | |
| 5、免疫组化问题解答 | |
| 6、Western Blotting 操作步骤 | |
| 7、Western Blotting 问题解答 | |
| 8、关于肽链的设计 | |
| 9、多肽的溶解与保存 | |
| 10、酶标抗体效价测定程序 | |
