TC-G 1005|1415407-60-1|-陌孚医药/Medlife

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TC-G 1005

目录号: PL01827 纯度: ≥99%

CAS No. :1415407-60-1

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中文名称	TC-G 1005
中文别名	(4-环丙基-3,4-二氢-1(2H)-喹喔啉基)[4-(2,5-二甲基苯氧基)-3-吡啶基]甲酮
英文名称	TC-G 1005
英文别名	TC-G 1005;(4-Cyclopropyl-3,4-dihydro-1(2H)-quinoxalinyl)[4-(2,5-dimethylphenoxy)-3-pyridinyl]methanone;BCP21245;BDBM50399966;[4-(2,5-dimethylphenoxy)pyridin-3-yl]-(4-cyclopropyl-3,4-dihydro-2h-quinoxalin-1-yl)methanone;(4-Cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)(4-(2,5-dimethylphenoxy)pyridin-3-yl)methanone;(4-Cyclopropyl-2,3-dihydroquinoxalin-1-yl)-[4-(2,5-dimethylphenoxy)pyridin-3-yl]methanone
Cas No.	1415407-60-1
分子式	C₂₅H₂₅N₃O₂
分子量	399.48
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TC-G 1005 是一种有效，选择性和口服活性的 TGR5 激动剂，激活 hTGR5 和 mTGR5 的 EC₅₀ 值分别为 0.72 和 6.2 nM。TC-G 1005 可降低小鼠体内葡萄糖水平。
生物活性	TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC 50 s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
性状	Solid
IC50 & Target[1][2]	IC50: 0.72 nM (hTGR5); 6.2 nM (mTGR5)
体外研究(In Vitro)	TC-G 1005 activates human and mouse TGR5 with EC50s of 0.72 nM and 6.2 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	TC-G 1005 (25-100 mg/kg; a single p.o.) stimulates GLP-1 secretion in imprinting control region (ICR) mice. TC-G 1005 (50 mg/kg; a single p.o.) causes a 49% reduction in blood glucose AUC 0-120 min in ICR mice. TC-G 1005 (50 mg/kg; a single p.o.) signi?cantly reduces blood glucose at 4, 6, 10, and 24 h in db/db mice. TC-G 1005 (5 mg/kg; p.o.) exhibits rather low plasma exposure, with a C max of 56 ng/mL and a t 1/2 of 1.5 in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Duan H, et, al. Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J Med Chem. 2012 Dec 13;55(23):10475-89. [2]. Urso A, et, al. Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am J Physiol Lung Cell Mol Physiol. 2020 Feb 1;318(2):L264-L275.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (83.43 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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