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

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

Cat. No.: HY-10895A Purity: 99.88%
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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.

For research use only. We do not sell to patients.

SB-334867 free base Chemical Structure

SB-334867 free base Chemical Structure

CAS No. : 792173-99-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 101 In-stock
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10 mg USD 158 In-stock
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Based on 6 publication(s) in Google Scholar

Other Forms of SB-334867 free base:

SB-334867 free base Related Antibodies

Top Publications Citing Use of Products

    SB-334867 free base purchased from MedChemExpress. 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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo[2][3].

    IC50 & Target

    OX2

    ()

    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].

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

    SB-334867 free base Related Antibodies
    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].
    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[3].
    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[3].

    MedChemExpress (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.
    Molecular Weight

    319.32

    Formula

    C17H13N5O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC(OC(C)=N2)=C2C=C1)NC3=CC=NC4=CC=CN=C43
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (156.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

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

    • Protocol 2

      Add each solvent one by one:  50% HP-β-CD in Saline

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.88%

    COA (255 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    0.1 M HCL / DMSO 1 mM 3.1317 mL 15.6583 mL 31.3165 mL 78.2914 mL
    5 mM 0.6263 mL 3.1317 mL 6.2633 mL 15.6583 mL
    10 mM 0.3132 mL 1.5658 mL 3.1317 mL 7.8291 mL
    15 mM 0.2088 mL 1.0439 mL 2.0878 mL 5.2194 mL
    DMSO 20 mM 0.1566 mL 0.7829 mL 1.5658 mL 3.9146 mL
    25 mM 0.1253 mL 0.6263 mL 1.2527 mL 3.1317 mL
    30 mM 0.1044 mL 0.5219 mL 1.0439 mL 2.6097 mL
    40 mM 0.0783 mL 0.3915 mL 0.7829 mL 1.9573 mL
    50 mM 0.0626 mL 0.3132 mL 0.6263 mL 1.5658 mL
    60 mM 0.0522 mL 0.2610 mL 0.5219 mL 1.3049 mL
    80 mM 0.0391 mL 0.1957 mL 0.3915 mL 0.9786 mL
    100 mM 0.0313 mL 0.1566 mL 0.3132 mL 0.7829 mL
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    SB-334867 free base Related Classifications

    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-334867792173-99-0SB334867ASB334867SB 334867Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorBECsucroseintakeethanollocomotoractivityCHOcellInhibitorinhibitorinhibit

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