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TUG-770
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TUG-770图片
CAS NO:1402601-82-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
TUG-770 是一种有效的、选择性的、具有口服活性的 GPR40/FFA1 激动剂,对人 FFA1 的 EC50 为 6 nM。
Cas No.1402601-82-4
别名TUG770;TUG 770
化学名3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
Canonical SMILESC1=CC=C(C(=C1)CC#N)C#CC2=CC(=C(C=C2)CCC(=O)O)F
分子式C19H14FNO2
分子量307.32
溶解度≥ 11.85 mg/mL in DMSO, ≥ 9.5 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 6 nM

TUG-770 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. Free fatty acid receptor 1 (FFA1 or GPR40) enhances the glucose-stimulated insulin secretion from pancreatic β-cells and attracts high interest as a new target for the treatment of type 2 diabetes.

In vitro: TUG-770 showed a pronounced increase in potency on FFA1 with EC50 = 6 nM and 150-fold selectivity over FFA4. TUG-770 showed a high selectivity over FFA2, FFA3, PPARγ, and 54 diverse transporters, receptors, and enzymes. In the rat INS-1E cell line, TUG-770 caused significantly increased insulin secretion at high glucose concentration and, as expected, no effect at low glucose concentration [1].

In vivo: Pharmacokinetic studies of TUG-770 in mice showed a fast oral absorption, higher plasma concentration, a longer half-life, lower clearance, and increased bioavailability. No adverse effects were seen in mice after four weeks of daily oral treatment of 20 mg/kg and acute treatment in doses up to 250 mg/kg. In vivo examination of TUG-770 in an acute intraperitoneal glucose tolerance test in normal mice showed a good dose-dependent response with maximal reduction in glucose level reached at 50 mg/kg. The followed chronic oral glucose tolerance test study in DIO mice showed that TUG-770 was more effective than its analog. Further evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses [1].

Clinical trial: N/A

Reference:
[1] Christiansen E,Hansen SV,Urban C,Hudson BD,Wargent ET,Grundmann M,Jenkins L,Zaibi M,Stocker CJ,Ullrich S,Kostenis E,Kassack MU,Milligan G,Cawthorne MA,Ulven T.  Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett.2013 May 9;4(5):441-445.