TC-G-1008 - CAS:1621175-65-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	TC-G-1008
英文名称:	TC-G-1008
别名:	TC-G 1008 GPR39C3；N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
CAS No:	1621175-65-2	分子式:	C₁₈H₁₉ClN₆O₂S	分子量:	418.90
CAS No:	1621175-65-2
分子式:	C₁₈H₁₉ClN₆O₂S
分子量:	418.90

点击下载产品说明书(PDF)

T10469 TC-G-1008 ≥98% (psaitong)

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包装规格：

5mg 10mg 25mg 50mg in glass bottle

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℃

UN码：

HazardClass：

危害声明：

安全说明：

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