1334294-76-6
中文名稱
1334294-76-6
英文名稱
GSK682753A
CAS
1334294-76-6
分子式
C23H21Cl3N2O3
分子量
479.78
MOL 文件
1334294-76-6.mol
1334294-76-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 T11498 英文別名
GSK682753AEBI2 inhibitor GS682753A
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]-
物理化學(xué)性質(zhì)
沸點(diǎn)731.8±60.0 °C(Predicted)
密度1.44±0.1 g/cm3(Predicted)
儲(chǔ)存條件4°C, protect from light
溶解度DMSO : ≥ 27 mg/mL (56.28 mM)
酸度系數(shù)(pKa)-0.50±0.20(Predicted)
形態(tài)Solid
顏色White to light yellow
常見問題列表
生物活性
GSK682753A是EB病毒誘導(dǎo)受體2 (EBI2) 的反向激動(dòng)劑, IC50值為 53.6 nM。靶點(diǎn)
IC50: 53.6 nM (EBI2)
體外研究
GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and guanosine5'-3-O-(thio)-triphosphate (GTPγS) binding assays, the potency of this compound is 2.6-53.6 nM, and its inhibitory efficacy is 75%. GSK682753A dose-dependently inhibits EBI2 with an IC 50 of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency.