CS-2374
| 中文名称 | CS-2374 |
|---|---|
| 中文同义词 | 16211175-65-2;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;TC-G 1008,GPR39激动剂 |
| 英文名称 | GPR39-C3 |
| 英文同义词 | GPR39-C3;TC-G-1008;N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide;GPR39C3;GPR39 C3;CS-2374;TC-G-1008 (GPR39-C3);Methanesulfonamide, N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]-;N-(3-Chloro-4-(((2-(methylamino)-6-(pyridin-2-yl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide |
| CAS号 | 1621175-65-2 |
| 分子式 | C18H19ClN6O2S |
| 分子量 | 418.9 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1621175-65-2.mol |
| 结构式 |  |
CS-2374 性质
| 沸点 | 662.1±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.462±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO:63.97(最大浓度 mg/mL);152.72(最大浓度 mM) DMSO:PBS (pH 7.2) (1:5):0.16(最大浓度 mg/mL);0.38(最大浓度. mM) 乙醇:2.0(最大浓度 mg/mL);4.77(最大浓度 mM) |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 7.43±0.10(Predicted) |
| Target | Value |
|
rGPR39
(Cell-free assay) | 0.4 nM(EC50) |
|
hGPR39
(Cell-free assay) | 0.8 nM(EC50) |
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.
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-103007 | TC-G-1008 | 1 mg | 500元 | |
| 2024/04/30 | HY-103007 | CS-2374 TC-G-1008 | 1621175-65-2 | 5mg | 1100元 |