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首页-小分子抑制剂&激动剂-GPCR-GPR183 (EBI2)-GSK682753A
GSK682753A

Chemical Structure : GSK682753A

CAS No.: 1334294-76-6

GSK682753A (GSK 682753A, GSK-682753A)

货号: PC-42332Not For Human Use, Lab Use Only.

GSK682753A (GSK 682753A, GSK-682753A) is a potent, selective EBI-2 (GPR183) inhibitor with IC50 of 53.6 nM.

规格 价格 库存 数量
5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3480 In stock
50 mg ¥5480 In stock
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK682753A (GSK 682753A, GSK-682753A) is a potent, selective EBI-2 (GPR183) inhibitor with IC50 of 53.6 nM.
GSK682753A displays high selectivity over other constitutively active receptors, including GPR39, the ghrelin receptor, GPR17, MC1R, and ORF74.
GSK682753A does not affect the cell surface expression of EBI2 in HEK293 cells.
GSK682753A dose-dependently suppresses the inhibition of forskolin-stimulated cAMP accumulation mediated by EBI2 with IC50 of 10.9 nM, inhibits EBI2-mediated ERK phosphorylation with IC50 of 76 nM.
GSK682753A inhibits the antibody-induced proliferation of murine WT B cells.

物理化学性质&存储条件

分子量 479.78344
分子式 C23H21Cl3N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 27 mg/mL

Chemical Name/SMILES

1-Oxa-3,8-diazaspiro[4.5]decan-2-one, 8-[(2E)-3-(4-chlorophenyl)-1-oxo-2-propen-1-yl]-3-[(3,4-dichlorophenyl)methyl]-

参考文献

1. Benned-Jensen T, et al. J Biol Chem. 2011 Aug 19;286(33):29292-302.

2. Benned-Jensen T, et al. FEBS Open Bio. 2013 Feb 19;3:156-60.

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