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

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

Cat. No.: HY-10895A Purity: 99.89%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 92 In-stock
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5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
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50 mg USD 468 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of SB-334867 free base:

Top Publications Citing Use of Products

Publications Citing Use of MCE SB-334867 free base

    SB-334867 free base purchased from MCE. Usage Cited in: Front Neurosci. 2016 Jul 26;10:355.

    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.
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    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[1]

    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].

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

    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].

    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.

    792173-99-0

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 49 mg/mL (153.45 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.3132 mL 1.5658 mL 3.1317 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.89%

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    Keywords:

    SB-334867SB334867ASB334867SB 334867Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorBECsucroseintakeethanollocomotoractivityCHOcellInhibitorinhibitorinhibit

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    Product Name:
    SB-334867 free base
    Cat. No.:
    HY-10895A
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