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Almorexant hydrochloride

HY-10805A

(ACT-078573 hydrochloride; ACT 078573 hydrochloride; ACT078573 hydrochloride)

Almorexant hydrochloride

Almorexant hydrochloride Chemical Structure

Almorexant Hcl (ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $145 In-stock
5 mg $120 In-stock
10 mg $200 In-stock
50 mg $690 In-stock
100 mg $1200 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €142 In-stock
5 mg €118 In-stock
10 mg €196 In-stock
50 mg €676 In-stock
100 mg €1176 In-stock
200 mg Get quote
500 mg Get quote

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

Almorexant hydrochloride Data Sheet

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    Purity: 99.81%

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Biological Activity of Almorexant hydrochloride

Almorexant Hcl (ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]
Target: Dual OX!/OX2 receptor
in vitro: [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. 
in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 549.02 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C29H32ClF3N2O3
CAS No 913358-93-7
Solvent & Solubility

DMSO:72 mg/mL,H2O: <1 mg/mL

Preparing Stock Solutions

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

References on Almorexant hydrochloride

Other Forms

Inhibitor Kit
  • Lemborexant

    Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.

  • MK-3697

    MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.

  • MK-6096

    MK-6096(Filorexant) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).

  • Orexin 2 Receptor Agonist

    Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.

  • SB-674042

    SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.

  • TCS 1102

    TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).

  • TCS-OX2-29

    TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.