CAS NO: | 249889-64-3 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeableorexin-1 (OX1) receptorantagonist, shows selectivity overOX2(pKb=7.4), 100-fold over 5-HT2B, 5-HT2CwithpKivalues of 5.4 and 5.3, respectively[1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo[2][3]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | SB-334867 (100 pM– 10 μM) inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses in a concentration-dependent manner, with apparent pKbvalues of 7.27±0.04 and 7.23±0.03, but has no effect on the calcium response elicited by UTP (3 μM), which activates an endogenous purinergic receptor in CHO-OX1 and CHO-OX2 cells[4]. | ||||||||||||||||
体内研究 (In Vivo) | SB-334867 (intraperitoneal injection; 20 mg/kg; 20 days) administers 15 min before morphine injection can significantly decrease the effect of the morphine challenge dose in mice in comparison with the sporadically morphine-treated group[2].SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) significantly reduces ethanol intake relative to vehicle and does not effect water consumption in female P rats[3].SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) reduces ethanol consumption at the 30 mg/kg dose, high dose suppresses sucrose intake relative to vehicle, and it results in lower blood ethanol concentrations (BECs) relative to both the 10 and 30 mg/kg doses[3].
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分子量 | 355.78 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H14ClN5O2 | ||||||||||||||||
CAS 号 | 249889-64-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vivo:
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