Name: TC-G-1008
Brand: TargetMol
SKU: T4648
Price: 376 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 376

现货

5 mg

¥ 892

现货

10 mg

¥ 1,530

现货

25 mg

¥ 3,230

现货

50 mg

¥ 4,530

现货

100 mg

¥ 6,350

现货

200 mg

¥ 8,560

现货

1 mL x 10 mM (in DMSO)

¥ 971

现货

产品介绍

生物活性

产品描述	TC-G-1008 (GPR39-C3) is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
靶点活性	GPR139 (human):0.8 nM, GPR39 (rat):0.4 nM
体外活性	TC-G-1008在一系列激酶上显示出选择性(IC50s>10 μM)，且对相关的ghrelin和neurotensin-1受体没有显著的结合亲和力(IC50s>30 μM)[1]。在HEK293-GPR39细胞中，GPR39-C3是一种正向异构调节因子，能激活cAMP产生（Gs下游）、IP1积累（Gq下游）、SRF-RE依赖的转录（G12/13下游）和β-arrestin招募。GPR39-C3通过第二次化合物挑战，以剂量和时间依赖的方式导致对cAMP产生的响应丧失[2]。
体内活性	TC-G-1008对大鼠和小鼠的血浆蛋白结合率分别为99.3%和99.1%。TC-G-1008是首个强效的GPR39激动剂（人类和大鼠受体的EC50s ≤ 1 nM），能够通过口服在小鼠中生物可用，并显著诱导急性GLP-1水平。经过一次性口服0.5%甲基纤维素/0.1%Tween 80水悬剂中的10、30和100 mg/kg剂量，TC-G-1008在1至1.5小时内分别达到1.4、6.1和25.3 μM的最大暴露水平[1]。
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°C in the presence of 5% CO2. For pretreatment of the cells with GPR39 ligands (TCG-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°C. 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°C. The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit[2] .
动物实验	Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1] .
别名	GPR39-C3

化学信息

分子量	418.9
分子式	C₁₈H₁₉ClN₆O₂S
CAS No.	1621175-65-2
Smiles	CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(n1)-c1ccccn1
密度	1.462 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 255 mg/mL (608.74 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.77 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3872 mL	11.9360 mL	23.8720 mL	119.3602 mL
5 mM	0.4774 mL	2.3872 mL	4.7744 mL	23.8720 mL
10 mM	0.2387 mL	1.1936 mL	2.3872 mL	11.9360 mL
20 mM	0.1194 mL	0.5968 mL	1.1936 mL	5.9680 mL
50 mM	0.0477 mL	0.2387 mL	0.4774 mL	2.3872 mL
100 mM	0.0239 mL	0.1194 mL	0.2387 mL	1.1936 mL

体内实验配液计算器