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TC-G-1008  ≥98%

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产品描述：基本信息 产品编号： T10469 产品名称： TC-G-1008 CAS: 1621175-65-2   储存条件 粉末 -20℃ 四年     分子式： C18H19ClN6O2S 溶于液体 -80℃ 6个月 分子量 418.90 -20℃ 1个月 化学名：  N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide Solubility (25°C)：   体外:   DMSO 84mg/mL (200.52mM) Ethanol 2mg/mL (4.77mM) Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3872mL 11.9360mL 23.8720mL 5mM 0.4774mL 2.3872mL 4.7744mL 10mM 0.2387mL 1.1936mL 2.3872mL 50mM 0.0477mL 0.2387mL 0.4774mL   生物活性 产品描述 一种有效的口服活性的GPR39激动剂。 靶点 0.4nM (GPR39),0.8nM (GPR39)   体外研究 TC-G-1008 shows selectivity over a panel of kinases (IC50s>10μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30μM).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 100mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80,TC-G-1008 achieves, between 1 and 1.5h,maximal exposures of 1.4,6.1,and 25.3μM,respectively.   推荐实验方法(仅供参考) 激酶实验： HEK293-GPR39 cells are plated and cultured in poly-d-lysine-coated, white,384-well plates (4000 cells/well) in the growth medium overnight at 37℃ in the presence of 5% CO2.For pretreatment of the cells with GPR39 ligands (TC-G-1008) or vehicle control (DMSO),the culture medium is removed and the cells are stimulated with GPR39 ligands in assay buffer for the indicated time at 37℃.Then,the compound solution is removed and washed twice with PBS containing 0.1% BSA.For measurement of intracellular cAMP,the cells are stimulated with drugs in stimulation buffer for 30 min at 37℃.The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit.   动物实验: Mice:Mice are given single oral doses of 10,30,and 100mg/kg of TC-G-1008.
保存条件：-20℃

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