1. GPCR/G Protein
  2. Orexin Receptor (OX Receptor)

Almorexant hydrochloride (Synonyms: ACT-078573 hydrochloride)

Cat. No.: HY-10805A Purity: 99.87%
Data Sheet SDS Handling Instructions

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.

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Almorexant hydrochloride Chemical Structure

Almorexant hydrochloride Chemical Structure

CAS No. : 913358-93-7

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  

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Other Forms of Almorexant hydrochloride:

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  • References

Description

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00606593 Midnight Pharma, LLC Chronic Primary Insomnia December 2007 Phase 2
NCT00608985 Midnight Pharma, LLC Primary Insomnia March 2008 Phase 3
NCT01987739 Midnight Pharma, LLC Abuse Potential Study September 2009 Phase 1
NCT00640848 Midnight Pharma, LLC Insomnia|Primary Insomnia May 2006 Phase 1
NCT01243060 Northern California Institute of Research and Education|U.S. Army Medical Research and Materiel Command Healthy Volunteers May 2011
NCT01954589 Actelion Safety|Tolerability|Pharmacodynamics|Pharmacokinetics November 2011 Phase 1
NCT00606593 Midnight Pharma, LLC Chronic Primary Insomnia December 2007 Phase 2
NCT00608985 Midnight Pharma, LLC Primary Insomnia March 2008 Phase 3
NCT01987739 Midnight Pharma, LLC Abuse Potential Study September 2009 Phase 1
NCT00640848 Midnight Pharma, LLC Insomnia|Primary Insomnia May 2006 Phase 1
NCT01243060 Northern California Institute of Research and Education|U.S. Army Medical Research and Materiel Command Healthy Volunteers May 2011
NCT01954589 Actelion Safety|Tolerability|Pharmacodynamics|Pharmacokinetics November 2011 Phase 1
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References
Molecular Weight

549.02

Formula

C₂₉H₃₂ClF₃N₂O₃

CAS No.

913358-93-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 46 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.87%

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