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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 191 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 191 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 158 In-stock
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg USD 911 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1584 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Almorexant hydrochloride:

Top Publications Citing Use of Products

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

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

    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].

    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.
    SMILES

    CNC([[email protected]@H](C1=CC=CC=C1)N2CCC3=CC(OC)=C(OC)C=C3[[email protected]@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)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (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
    10 mM 0.1821 mL 0.9107 mL 1.8214 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 (4.55 mM); Clear solution

    • 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

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.55 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.98%

    References
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    • 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.

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    Product Name:
    Almorexant hydrochloride
    Cat. No.:
    HY-10805A
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