SB-334867 free base (Synonyms:SB334867A free base)
目录号 : KM4605 CAS No. : 792173-99-0 纯度 : 98%

SB-334867 free base (SB334867A free base) 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 (pKb=7.4),对 5-HT2B、5-HT2C 的选择性是 100 倍,pKi 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增敏。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg 询价 In-stock
200mg 询价 In-stock

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生物活性

SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi 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 pKb 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.

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.
SB-334867 (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.
SB-334867 (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.

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.
分子式
C17H13N5O2
分子量
319.32
CAS号
792173-99-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (156.58 mM; Need ultrasonic)

0.1 M HCL : 6 mg/mL (18.79 mM; ultrasonic and adjust pH to 3 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1317 mL 15.6583 mL 31.3165 mL
5 mM 0.6263 mL 3.1317 mL 6.2633 mL
10 mM 0.3132 mL 1.5658 mL 3.1317 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。-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:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (31.32 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 50% HP-β-CD in saline

    Solubility: 7.69 mg/mL (24.08 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.83 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.83 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 5.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.83 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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