SB-334867 free base|792173-99-0|(SB334867A free base)-陌孚医药/Medlife

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SB-334867 free base (Synonyms: SB334867A free base)

目录号: PL08108 纯度: ≥99%

CAS No. :792173-99-0

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PL08108-100mg	100mg	询价	询价
PL08108-200mg	200mg	询价	询价
PL08108-10mM*1mLinDMSO	10mM*1mLinDMSO	¥952.00	请登录

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中文名称	SB-334867 free base
中文别名	1-(2-甲基苯并[d]噁唑-6-基)-3-(1,5-萘啶-4-基)脲;SB334867 抑制剂;N-(2-甲基-6-苯并恶唑基)-N'-1,5-二氮杂萘-4-基脲
英文名称	SB-334867 free base
英文别名	1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea;N-(2-METHYL-6-BENZOOXAZOLYL)-N''-1,5-NAPHTHYRIDIN-4-YL UREA;SB-334867 free base;N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl;SB 334867;Urea,N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl-;SB334867 free base;SB334867A free base;N-(2-Methyl-6-benzoxazolyl)-N′-1,5-naphthyridin-4-yl-urea;SB-334867;SB-334867A;SB-334867 (free base);SB334867;N-(2-METHYL-6-BENZOXAZOLYL)-N'-1,5-NAPHTHYRIDIN-4-YL UREA;N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl-Urea;1-(2-Methyl-benzooxazol-6-yl)-3-[1,5]naphthyridin-4-yl-urea;1-(2-Methylbenzo[d]oxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea;1-(2-methyl-1
Cas No.	792173-99-0
分子式	C₁₇H₁₃N₅O₂
分子量	319.32
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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 (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增敏。
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 (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]	OX2 ()
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 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. 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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
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. [2]. ?upina M, et al. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms.

溶解度数据	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

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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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