249889-64-3|SB-334867 hydrochloride，≥98%|Medlife|Medlife为MCE，Selleck，麦克林，阿拉丁试剂，罗恩试剂，Sigma，安耐吉试剂，泰坦等同类产品品牌，上海现货，高性价比小分子化合物

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SB-334867 hydrochloride

Orexin-1受体拮抗剂,SB-334867是非肽类食欲肽OX1受体拮抗剂，pKb为7.2。

目录号: PC10690 纯度: ≥98%

CAS No. :249889-64-3

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中文名称	SB-334867 hydrochloride
中文别名	密草通;仲丁通
英文名称	SB-334867 hydrochloride
英文别名	Urea,N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl-, hydrochloride (1:1);1-(2-methylbenzoxazole-6-yl)-3-[1,5]naphthyridine-4-yl urea hydrochloride;SB 334867;N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA;SB 334867A;Urea, N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl-, (Hydrochloride)
Cas No.	249889-64-3
分子式	C₁₇H₁₃N₅O₂
分子量	319.32
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

性状

Solid

IC50 & Target[1][2]

OX1

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 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.

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

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.
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.

Medlife 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.

运输条件

Room temperature or refrigerated transportation.

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)

参考文献

[1]. Porter RA, et al. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. [Information]

[2]. ?upina M, et al. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms. [Information]

[3]. Anderson RI, et al. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models.Front Neurosci. 2014 Feb 25;8:33. [Information]

[4]. Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist.Br J Pharmacol. 2001 Mar;132(6):1179-82. [Information]

溶解度数据	体内研究: 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).

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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