1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1H-INDOL-2-ONE
- CAS号:303149-14-6
- 英文名:HT-2157
- 中文名:1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1H-INDOL-2-ONE
- CBNumber:CB83155060
- 分子式:C21H13F3N2O
- 分子量:366.34
- MOL File:303149-14-6.mol
- 熔点 :141-144 °C
- 沸点 :484.0±55.0 °C(Predicted)
- 密度 :1.29±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMF:30.0(Max Conc. mg/mL);81.89(Max Conc. mM)
DMSO:44.0(Max Conc. mg/mL);120.11(Max Conc. mM)
Ethanol:7.0(Max Conc. mg/mL);19.11(Max Conc. mM) - 形态 :A solid
- 酸度系数(pKa) :-0.36±0.20(Predicted)
- 颜色 :Yellow to orange
1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1H-INDOL-2-ONE性质、用途与生产工艺
- 生物活性 HT-2157(SNAP 37889) 是一种选择性的高亲和力甘丙肽-3 受体 (Gal3) 竞争性拮抗剂。
-
靶点
Galanin-3 receptor
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体外研究
HT-2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK - cells expressing the human Gal 3 receptor (K i =17.44±0.01 nM; n>100) and is highly selective for Gal 3 over the Gal 1 and Gal 2 subtypes (K i >10,000 nM for each subtype; n=46 of each subtype). When tested for the antagonism of galanin-evoked inhibition of adenylyl cyclase, HT-2157 (0.1-10 μM) produces concentration-dependent rightward shifts of the concentration-effect curve to galanin.
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体内研究
The galanin-3 receptor antagonist, HT-2157 (SNAP 37889), reduces operant responding for ethanol in alcohol-preferring rats. The novel selective GALR3 antagonist, HT-2157, to reduce anxiety-like behaviour and voluntary ethanol consumption in the iP (alcohol-preferring) rat. Male iP rats treated with HT-2157 at a dose of 30 mg/kg (i.p.) do not show altered locomotor activity or changes in anxiety-like behaviour in the elevated plus maze or light-dark paradigms. Treatment with HT-2157 (30 mg/kg, i.p.) reduces operant responding for solutions containing ethanol, sucrose and saccharin. Collectively, results from the current study shows that HT-2157 (30 mg/kg, i.p.) is effective in reducing operant responding for ethanol, independent of a sedative effect.
- 更新日期:2024/11/08
- 产品编号:HY-100717
- 产品名称:1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1H-INDOL-2-ONE HT-2157
- CAS编号:303149-14-6
- 包装:1mg
- 价格:900元
- 更新日期:2024/11/08
- 产品编号:HY-100717
- 产品名称:1-PHENYL-3-[[3-(TRIFLUOROMETHYL)PHENYL]IMINO]-1H-INDOL-2-ONE HT-2157
- CAS编号:303149-14-6
- 包装:10mM * 1mLin DMSO
- 价格:2176元
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