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: 99.44%
COA 产品使用指南

摩尔计算器

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(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敏感性。

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SB-334867 Chemical Structure

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]

    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) 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[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 (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[2].
    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[3].
    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[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
    细胞实验： 

    H2O 中的溶解度 : 10 mg/mL (28.11 mM; 超声助溶 (<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
    查看完整储备液配制表

    * 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。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料
    参考文献

    SB-334867 相关分类

    完整储备液配制表

    * 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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 2.8107 mL 14.0536 mL 28.1073 mL 70.2681 mL
    5 mM 0.5621 mL 2.8107 mL 5.6215 mL 14.0536 mL
    10 mM 0.2811 mL 1.4054 mL 2.8107 mL 7.0268 mL
    15 mM 0.1874 mL 0.9369 mL 1.8738 mL 4.6845 mL
    20 mM 0.1405 mL 0.7027 mL 1.4054 mL 3.5134 mL
    25 mM 0.1124 mL 0.5621 mL 1.1243 mL 2.8107 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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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