SB-334867 SB 334867A|cas:249889-64-3|西域试剂

SB-334867 SB 334867A,99.44%

产品编号：Bellancom-10895| CAS NO：249889-64-3| 分子式：C₁₇H₁₄ClN₅O₂| 分子量：355.78

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货号	价格	库存与货期
Bellancom-10895	￥700.00	杭州北京（现货）
Bellancom-10895	￥1200.00	杭州北京（现货）
Bellancom-10895	￥3950.00	杭州北京（现货）
Bellancom-10895	￥6350.00	杭州北京（现货）

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SB-334867 SB 334867A

产品介绍

SB-334867 (SB 334867A) 是一种优良的选择性血脑屏障通透性 orexin-1 (OX1) receptor 拮抗剂，对 OX2 有选择性(pK_b=7.4)，对 5-HT_2B、5-HT_2C 的选择性是 100 倍，pK_i 值分别为 5.4 和 5.3。SB-334867 降低体内乙醇消耗量，抑制吗啡诱导的对运动活性的敏感性。

生物活性

SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

体外研究

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 pK_b values 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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Swiss mice
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice.

Animal Model:	C57BL/6J Mice
Dosage:	3, 10 and 30 mg/kg
Administration:	Intraperitoneal injection
Result:	Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Swiss mice
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice.

Animal Model:	C57BL/6J Mice
Dosage:	3, 10 and 30 mg/kg
Administration:	Intraperitoneal injection
Result:	Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.

性状

Solid

溶解性数据

In Vitro:

H₂O : 10 mg/mL (28.11 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8107 mL	14.0536 mL	28.1073 mL
5 mM	0.5621 mL	2.8107 mL	5.6215 mL
10 mM	0.2811 mL	1.4054 mL	2.8107 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

1.

SB-334867 is dissolved in the aCSF (in mM: 133.3 NaCl, 3.4 KCl, 1.3 CaCl₂, 1.2 MgCl₂, 0.6 NaH₂PO₄, 32.0 NaHCO₃, and 3.4 glucose, with pH adjusted to 7.4)^[5].