中文名 | TC-G-1008 |
英文名 | TC-G-1008 |
别名 | 化合物TC-G-1008 N-(3-氯-4-(((2-(甲基氨基)-6-(吡啶-2-基)嘧啶-4-基)氨基)甲基)苯基)甲磺酰胺 |
英文别名 | GPR39C3 CS-2374 GPR39 C3 GPR39-C3 TC-G-1008 16211175-65-2 TC-G-1008 (GPR39-C3) N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide N-(3-Chloro-4-(((2-(methylamino)-6-(pyridin-2-yl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide Methanesulfonamide, N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]- |
CAS | 1621175-65-2 |
化学式 | C18H19ClN6O2S |
分子量 | 418.9 |
密度 | 1.462±0.06 g/cm3(Predicted) |
沸点 | 662.1±65.0 °C(Predicted) |
溶解度 | DMSO: ≥ 100 mg/mL |
酸度系数 | 7.43±0.10(Predicted) |
存储条件 | 2-8°C |
体外研究 | TC-G-1008 shows selectivity over a panel of kinases (IC 50 s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC 50 s>30 μM). In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound. |
体内研究 | Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.387 ml | 11.936 ml | 23.872 ml |
5 mM | 0.477 ml | 2.387 ml | 4.774 ml |
10 mM | 0.239 ml | 1.194 ml | 2.387 ml |
5 mM | 0.048 ml | 0.239 ml | 0.477 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!