TUG-469|1236109-67-3|-陌孚医药/Medlife

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TUG-469

目录号: PL02598 纯度: ≥99%

CAS No. :1236109-67-3

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中文名称	TUG-469
英文名称	TUG-469
英文别名	3-(4-(((2'-methyl-[1,1'-biphenyl]-3-yl)methyl)amino)phenyl)propanoic acid;3-[4-[[3-(2-methylphenyl)phenyl]methylamino]phenyl]propanoic acid;3-(4-((3-(2-Methylphenyl)phenyl)methylamino)phenyl)propanoic acid;BDBM50343141;3-(4(2''-Methylbiphenyl-3-ylmethylamino)phenyl)propanoic acid
Cas No.	1236109-67-3
分子式	C₂₃H₂₃NO₂
分子量	345.43
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TUG-469 是选择性的游离脂肪酸受体 1 (FFA1/GPR40) 激动剂，EC₅₀ 值为 19 nM。TUG-469 对 FFA1 的选择性是 FFA4 的 200 倍。TUG-469 显著改善糖尿病早期小鼠的糖耐量。TUG-469 可用于糖尿病的研究。
生物活性	TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC 50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.
性状	Solid
体外研究(In Vitro)	TUG-469 (0-10 μM) shows efficacy to hFFA1 with a pEC50 value of 7.73. TUG-469 (10 μM) increases the insulin secretion under 10 mM glucose stimulation. TUG-469 (0-100 μM) is >200-fold selective for FFA1 over FFA4 with EC50 values of 19 nM and 4.4 μM for FFA1 and FFA4, respectively. TUG-469 (5 μM; 30 min) significantly increases insulin secretion of INS-1 cells with the presence of high glucose concentration (16.7 mM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	TUG-469 (5 mg/kg; i.p.; 60 and 90 min after glucose administration) affects blood glucose level. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male NZO mice with glucose administrat
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Christiansen E, et al. Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. ACS Med Chem Lett. 2010 Jul 2;1(7):345-9. [2]. Urban C, et al. In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1021-30.

溶解度数据	In Vitro: DMSO : 100 mg/mL (289.49 mM; Need ultrasonic)配制储备液

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