货号	规格	价格	上海	北京	武汉	南京
S89358-5mg	98.40%	￥260.00 S89358-5mg ￥260.00 现货	5 5	-	-	-
S89358-10mg	98.40%	￥400.00 S89358-10mg ￥400.00 现货	5 5	-	-	-
S89358-25mg	98.40%	￥680.00 S89358-25mg ￥680.00 现货	5 5	-	-	-
S89358-100mg	98.40%	￥1980.00 S89358-100mg ￥1980.00 现货	3 3	-	-	-

货号

规格

价格

上海

北京

武汉

南京

购买数量

S89358-5mg

98.40%

￥260.00

S89358-10mg

98.40%

￥400.00

S89358-25mg

98.40%

￥680.00

S89358-100mg

98.40%

￥1980.00

产品描述：

GSK620 是一种泛 BD2 的抑制剂，在人全血中显示出抗炎表型，具有优良的广泛选择性、显影性和体内口服药代动力学

靶点：

BD2;EpigeneticReaderDomain

体外研究：

GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 is capable of reducing the MCP-1 response in a concentration-dependent manner, providing strong evidence that GSK620 is indeed engaging BD2 in cells

体内研究：

GSK620 is a potent and selective pan-BD2 inhibitor with excellent in vivo PK properties and excellent developability properties, with the exception of moderate FaSSIF solubility driven by its highly crystalline nature

细胞实验：

Cell lines: human whole blood, hepatocytes Concentrations: 0.5 μM Incubation Time: 60 min, 120 min Method: GSK620 is diluted in 100% DMSO to give a range of appropriate concentrations at 140× the required final assay concentration, of which 1 μL is added to a 96 well tissue culture plate. Then 130 μL of human whole blood, collected into sodium heparin anticoagulant (1 unit/mL final) is added to each well and plates are incubated at 37℃ (5% CO2) for 30 min before the addition of 10 μL of 2.8 μg/mL LPS, diluted in complete RPMI 1640 (final concentration 200 ng/mL), to give a total volume of 140 μL per well. After further incubation for 24 h at 37℃, 140 μL of PBS is added to each well. The plates are sealed, shaken for 10 min, and then centrifuged (2500 rpm × 10 min). Finally, 100 μL of the supernatant is removed and MCP-1 levels assayed immediately by immunoassay.

动物实验：

Animal Models: Male Wistar Han rats, male Beagle dog Dosages: 0.5 mg/kg, 1 mg/kg, 3 mg/kg Administration: IV, Oral gavage

参考文献：

1. Jonathan T Seal, et al. The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor. J Med Chem. 2020 Sep 10;63(17):9093-9126. 2. Massimo Petretich, et al. Domain-selective targeting of BET proteins in cancer and immunological diseases. Curr Opin Chem Biol . 2020 Aug;57:184-193.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.073 ml	15.367 ml	30.734 ml
5 mM	0.615 ml	3.073 ml	6.147 ml
10 mM	0.307 ml	1.537 ml	3.073 ml
50 mM	0.061 ml	0.307 ml	0.615 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

GSK620

1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)