2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. JTC-801

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.

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

JTC-801 Chemical Structure

JTC-801 Chemical Structure

CAS No. : 244218-51-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 79 In-stock
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10 mg USD 80 In-stock
50 mg USD 330 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of JTC-801:

JTC-801 Related Antibodies

Top Publications Citing Use of Products

    JTC-801 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2019 Feb;17(2):1939-1945.  [Abstract]

    Western blot analysis of proteins from Hep G2 cells treated with JTC‑801 for 24 h. The band intensities are quantified.

    JTC-801 purchased from MedChemExpress. Usage Cited in: Pharmazie. 2018 May 1;73(5):283-287.  [Abstract]

    Expression levels of proteins (BCL2, BAX and Active Caspase3) involved in the apoptotic pathway in the different SKOV3 groups, as detected by western blotting.

    JTC-801 purchased from MedChemExpress. Usage Cited in: J Recept Signal Transduct Res. 2018 Apr;38(2):133-140.  [Abstract]

    JTC-801 down-regulates BCL-2 expression, and up-regulates BAX, Caspase-3 expression in U2OS cells.

    View All Opioid Receptor Isoform Specific Products:

    View All Isoforms
    μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.

    IC50 & Target

    NOP Receptor/ORL1

     

    In Vitro

    JTC-801 inhibits [3H]-nociceptin binding to ORL1 receptor expressed in HeLa cells with an IC50 value of 94±8.6 nm at a [3H]-nociceptin concentration of 50 pM. JTC-801 weakly inhibits the binding of the ligands to human δ receptor (IC50>10 μM), κ receptor (IC50>10 μM), and μ receptor (IC50=325 nM). In rat cerebrocortical membrane, JTC-801 inhibits ORL1 receptor (IC50=472 nM) and μ receptor (IC50=1831 nM). JTC-801 at a concentration of 10 μM reverses the inhibitory action of nociceptin against forskolin-induced increase in cyclic AMP level (IC50: 2.58 μM, 1 nM of nociceptin used). JTC-801 alone does not affect the the production of cyclic AMP[1]. The affinity of JTC-801 for ORL1 receptor, human opioid μ-, κ-, and δ-receptors is 8.2 nM, 102.9 nM, 1057.5 nM and 8647.2 nM[2].

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

    JTC-801 Related Antibodies
    In Vivo

    JTC-801 (≥0.01 mg/kg, i.v. or 1 mg/kg, p.o.) antagonizes the nociceptin-induced allodynia in mice. In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg by i.v. administration or 1 mg/kg by p.o. administration. This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10 mg/kg, s.c.). JTC-801 antagonizes the ORL1 receptor response, and has efficacious and potent anti-nociceptive effects in acute pain animal models not only by intravenous injection but also oral administration[1]. JTC-801 (0.3 mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice[2]. JTC-801 (6 mg/kg i.p., once daily) reverses SPS-induced mechanical allodynia, thermal hyperalgesia, anxiety-like behaviour and hypocortisolism. JTC-801 treatment also reverses NOP receptor protein and mRNA up-regulation in amygdala and PAG. JTC-801 blocks elevated N/OFQ levels in serum, CSF, PAG and hippocampus at day 21 of SPS[3]. JTC-801 (0.05-5 mg/kg, i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test[4].

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

    447.96

    Formula

    C26H26ClN3O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=CC(C)=NC2=C1C=C(NC(C3=C(COC4=CC=C(C=C4)CC)C=CC=C3)=O)C=C2.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (223.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : ≥ 0.33 mg/mL (0.74 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2323 mL 11.1617 mL 22.3234 mL
    5 mM 0.4465 mL 2.2323 mL 4.4647 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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

    ×
    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 (5.58 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 (5.58 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 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 98.91%

    COA (249 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    A suspension of membranes from human μ-opioid receptor-expressing CHO-K1 cells in 50 mM Tris-HCl buffer (pH 7.4) containing 5 mM MgCl2 and 10% sucrose is incubated at room temperature for 2.5 h with 0.33 nM 3H-labeled diprenorphine and various concentrations of JTC-801. The membranes are collected by filtration using Whatman 934-AH, and radioactivity is counted with a TopCount A9912V scintillation counter. Nonspecific binding (6.4%) is determined with 10 μM naloxone. Specific binding is calculated by subtracting nonspecific binding from the total binding. Data are the mean±SE (n=3).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    The antagonistic effect of naloxone, a non-specific opioid antagonist, on the anti-nociceptive effect of JTC-801 and morphine is examined by formalin stimulation test. Limb licking response is induced by subcutaneous injection of 50 μL of 5% formalin to the left hind limb of each rat. The first 5 min (from immediately after the injection of formalin) and the subsequent 15 min (15-30 min post-injection) are designated as the first and second phases, respectively. The limb licking time during each of the phases is measured and used as an indicator of pain. Fifteen min before the injection of formalin, naloxone (10 mg/kg, dissolved in physiological saline) is given subcutaneously. Five min before the injection of formalin, JTC-801 and morphine are dissolved in 5% sorbitol and given into the tail vein at doses of 0.03 and 1.0 mg/kg, respectively. JTC-801 (3.0 mg/kg) and morphine (30 mg/kg) are administered orally 60 min before the formalin injection.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2323 mL 11.1617 mL 22.3234 mL 55.8086 mL
    5 mM 0.4465 mL 2.2323 mL 4.4647 mL 11.1617 mL
    10 mM 0.2232 mL 1.1162 mL 2.2323 mL 5.5809 mL
    15 mM 0.1488 mL 0.7441 mL 1.4882 mL 3.7206 mL
    20 mM 0.1116 mL 0.5581 mL 1.1162 mL 2.7904 mL
    25 mM 0.0893 mL 0.4465 mL 0.8929 mL 2.2323 mL
    30 mM 0.0744 mL 0.3721 mL 0.7441 mL 1.8603 mL
    40 mM 0.0558 mL 0.2790 mL 0.5581 mL 1.3952 mL
    50 mM 0.0446 mL 0.2232 mL 0.4465 mL 1.1162 mL
    60 mM 0.0372 mL 0.1860 mL 0.3721 mL 0.9301 mL
    80 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6976 mL
    100 mM 0.0223 mL 0.1116 mL 0.2232 mL 0.5581 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    JTC-801 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:

    JTC-801244218-51-7JTC801JTC 801Opioid ReceptorInhibitorinhibitorinhibit

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