
簡(jiǎn)要描述:TAK875 1000413-72-8TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid.
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| 品牌 | absin | CAS | 1000413-72-8 |
|---|---|---|---|
| 分子式 | C29H32O7S | 純度 | >98% |
| 分子量 | 524.63 | 貨號(hào) | abs47028007 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a selective GPR40 | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
TAK875 1000413-72-8
| 產(chǎn)品描述 | |
| 描述 | TAK-875 is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
| 純度 | >98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | TAK-875;Fasiglifam |
| 外觀 | White to off white solid |
| 可溶性/溶解性 | DMSO : ≥ 128 mg/mL (243.98 mM) |
| 生物活性 | |
| 靶點(diǎn) | GPR40 |
| In vitro(體外研究) | TAK-875 (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. TAK-875 (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells. TAK-875 (3-30 μM) concentration-dependently augments i. In the presence of 10 mM glucose, TAK-875 (0.001-10 μM) dose-dependently stimulats insulin secretion from INS-1 833/15 cells. |
| In vivo(體內(nèi)研究) | TAK-875 (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. TAK-875 (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. TAK-875 at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, TAK-875 does not significantly alter insulin secretion in SD rats with normal fasting glucose levels . |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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