CS-2374
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- CAS号:
- 1621175-65-2
- 英文名:
- GPR39-C3
- 英文别名:
- CS-2374;GPR39-C3;TC-G-1008;GPR39C3;GPR39 C3;TC-G-1008 (GPR39-C3);inhibit,GHSR,Inhibitor,Growth hormone secretagogue receptor,TC G 1008,TCG1008;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]-
- 中文名:
- CS-2374
- 中文别名:
- 化合物TC-G-1008;16211175-65-2;TC-G 1008,GPR39激动剂;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
- CBNumber:
- CB13126726
- 分子式:
- C18H19ClN6O2S
- 分子量:
- 418.9
- MOL File:
- 1621175-65-2.mol
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CS-2374化学性质
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沸点:
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662.1±65.0 °C(Predicted)
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密度:
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1.462±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO:63.97(Max Conc. mg/mL);152.72(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:5):0.16(Max Conc. mg/mL);0.38(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);4.77(Max Conc. mM)-
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形态:
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A crystalline solid
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酸度系数(pKa):
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7.43±0.10(Predicted)
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CS-2374性质、用途与生产工艺
TC-G-1008（GPR39-C3）是一种有效的、口服活性的 G-protein coupled receptor 39 (GPR39)(zinc receptor) 激动剂，对大鼠受体和人类受体的EC50值分别为0.4 nM 和0.8 nM。
| Target | Value |
rGPR39
(Cell-free assay)
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0.4 nM(EC50)
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hGPR39
(Cell-free assay)
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0.8 nM(EC50)
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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.
CS-2374
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-103007 | TC-G-1008 | | 1 mg | 500元 |
| 2024/01/25 | HY-103007 | CS-2374
TC-G-1008 | 1621175-65-2 | 5mg | 1100元 |
1621175-65-2, CS-2374 相关搜索:
- 药靶配体
- 16211175-65-2
- TC-G 1008,GPR39激动剂
- 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
- 化合物TC-G-1008
- 16211175-65-2
- 1621175-65-2
- inhibit,GHSR,Inhibitor,Growth hormone secretagogue receptor,TC G 1008,TCG1008
- 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]-
- TC-G-1008 (GPR39-C3)
- CS-2374
- GPR39C3;GPR39 C3
- N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
- TC-G-1008
- GPR39-C3