1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Apoptosis
  2. Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis
  3. Almorexant hydrochloride

Almorexant hydrochloride  (Synonyms: ACT 078573 hydrochloride)

Cat. No.: HY-10805A Purity: 99.98%
COA Handling Instructions

Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

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

Almorexant hydrochloride Chemical Structure

Almorexant hydrochloride Chemical Structure

CAS No. : 913358-93-7

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 134 In-stock
Solution
10 mM * 1 mL in DMSO USD 134 In-stock
Solid
5 mg USD 111 In-stock
10 mg USD 178 In-stock
25 mg USD 416 In-stock
50 mg USD 666 In-stock
100 mg USD 1000 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Almorexant hydrochloride:

Top Publications Citing Use of Products

    Almorexant hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jan 9;9(6):6952-6967.  [Abstract]

    Orexin-A and Almorexant promote tyrosine phosphorylation of SHP2/OX1R complex

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis[1][2][3][4].

    IC50 & Target

    human OX2R

    0.17 nM (Kd)

    human OX1R

    1.3 nM (Kd)

    Caspase-3

     

    In Vitro

    Almorexant hydrochloride (1 μM) promote tyrosine phosphorylation of SHP2/OX1R complex[1].
    Almorexant hydrochloride (1 μM) inhibits the cellular growth of AsPC-1 cells[1].

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

    In Vivo

    Almorexant hydrochloride (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors[2].
    Almorexant hydrochloride (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning[4].
    Almorexant hydrochloride (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance[3].

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

    Animal Model: Mice xenografted with AsPC-1 cells[2]
    Dosage: 1.8 μmol/kg, 100 μL
    Administration: IP, daily, starting at day 0 or day 38
    Result: Resulted in a significant decrease in tumor volume when treatment starting at day 0. Started after AsPC-1 tumors were developed (day 38), rapidly and strongly reduced the volume of established tumors.
    Animal Model: Long-Evans rats (24, male, 16-18 weeks of age)[4]
    Dosage: 300 mg/kg
    Administration: PO, once
    Result: Successfully learned the spatial task, established spatial memory.
    Animal Model: Male C57BL/6 mice (Orexin/ataxin-3 transgenic (TG) mice and WT mice, 32 ± 0.9 g, age 15 ± 0.5 week)[3]
    Dosage: 30, 100, 300 mg/kg (3, 10, and 30 mg/mL; 10 mL/kg)
    Administration: IP, once every 3 days
    Result: Exacerbated cataplexy in TG mice and increased nonrapid eye movement (NREM) sleep with heightened sleep/wake fragmentation in both genotypes during the 12-h dark period after dosing. Showed greater hypnotic potency in WT mice than in TG mice.
    Clinical Trial
    Molecular Weight

    549.02

    Formula

    C29H32ClF3N2O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CNC([C@@H](C1=CC=CC=C1)N2CCC3=CC(OC)=C(OC)C=C3[C@@H]2CCC4=CC=C(C(F)(F)F)C=C4)=O.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 : ≥ 46 mg/mL (83.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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 1.8214 mL 9.1071 mL 18.2143 mL
    5 mM 0.3643 mL 1.8214 mL 3.6429 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    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 (4.55 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 (4.55 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: 99.98%

    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 1.8214 mL 9.1071 mL 18.2143 mL 45.5357 mL
    5 mM 0.3643 mL 1.8214 mL 3.6429 mL 9.1071 mL
    10 mM 0.1821 mL 0.9107 mL 1.8214 mL 4.5536 mL
    15 mM 0.1214 mL 0.6071 mL 1.2143 mL 3.0357 mL
    20 mM 0.0911 mL 0.4554 mL 0.9107 mL 2.2768 mL
    25 mM 0.0729 mL 0.3643 mL 0.7286 mL 1.8214 mL
    30 mM 0.0607 mL 0.3036 mL 0.6071 mL 1.5179 mL
    40 mM 0.0455 mL 0.2277 mL 0.4554 mL 1.1384 mL
    50 mM 0.0364 mL 0.1821 mL 0.3643 mL 0.9107 mL
    60 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7589 mL
    80 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
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