2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. SB-334867

SB-334867  (Synonyms: SB 334867A)

目录号: HY-10895 纯度: 99.31%
COA 产品使用指南 技术支持

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 OX1 的选择性比 OX2 (pKb=7.4) 高，比对 5-HT2B、5-HT2C 的选择性高 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敏感性。

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SB-334867

SB-334867 Chemical Structure

CAS No. : 249889-64-3

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Other Forms of SB-334867:

SB-334867 相关抗体

Top Publications Citing Use of Products

    SB-334867 purchased from MCE. Usage Cited in: Front Neurosci. 2016 Jul 26;10:355.  [Abstract]

    Effects of the orexin receptor type 1 (OX1R) antagonist SB334867 on the vestibular deficit syndrome after vestibular lesions induced by arsanilate (A) and IDPN (B) in rats.

    查看 Orexin Receptor (OX Receptor) 亚型特异性产品:

    查看所有亚型
    OX2 Receptor OX1 Receptor

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values 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]

    5-HT2B Receptor

     

    5-HT2C Receptor

     

    OX1

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    40 nM
    Compound: SB-334867
    Antagonist activity at OX1 receptor expressed in CHO cells assessed as inhibition of OXA-stimulated intracellular calcium mobilization after 30 mins by FLIPR assay
    Antagonist activity at OX1 receptor expressed in CHO cells assessed as inhibition of OXA-stimulated intracellular calcium mobilization after 30 mins by FLIPR assay
    		[PMID: 22617492]
    体外研究
    (In Vitro)

    SB-334867 (100 pM-10 μM)以浓度依赖性方式抑制食欲素-A (10 nM)和食欲素-B (100 nM)诱导的钙反应，其表观 pKb 值分别为 7.27 和 7.23，但对 UTP (3 μM) 引起的钙反应没有影响，后者可激活 CHO-OX1 和 CHO-OX2 细胞中的内源性嘌呤受体[4]。

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

    SB-334867 相关抗体:
    体内研究
    (In Vivo)

    SB-334867 (腹膜内注射；20 mg/kg；20 天) 在注射吗啡前 15 分钟给药，可显著降低小鼠吗啡激发剂量的影响[2]。
    SB334867 (腹膜内注射；3、10 和 30 mg/kg) 相对于载体显著减少乙醇摄入量，并且不影响雌性 P 大鼠的饮水量[3]。
    SB334867 (腹膜内注射；3、10 和 30 mg/kg) 在 30 mg/kg 剂量下减少乙醇消耗，高剂量相对于载体抑制蔗糖摄入，并且导致血液乙醇浓度 (BEC) 相对于 10 和 30 mg/kg 均降低剂量[3].

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

    Animal Model: Male Swiss mice[2]
    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[3]
    Dosage: 3, 10 and 30 mg/kg
    Administration: Intraperitoneal injection
    Result: Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.
    分子量

    355.78

    Formula

    C17H14ClN5O2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

    • 方案 一

      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].

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献

    SB-334867 相关分类

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SB-334867249889-64-3SB 334867ASB334867SB 334867Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorBECsucroseintakeethanollocomotoractivityCHOcellInhibitorinhibitorinhibit

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    目录号：
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