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Almorexant hydrochloride

OX1R/OX2R antagonist CAS# 913358-93-7

Almorexant hydrochloride

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Chemical structure

Almorexant hydrochloride

3D structure

Chemical Properties of Almorexant hydrochloride

Cas No. 913358-93-7 SDF Download SDF
PubChem ID 25227440 Appearance Powder
Formula C29H32ClF3N2O3 M.Wt 549.02
Type of Compound N/A Storage Desiccate at -20°C
Synonyms ACT-078573 hydrochloride
Solubility DMSO : ≥ 46 mg/mL (83.79 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (2R)-2-[(1S)-6,7-dimethoxy-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-3,4-dihydro-1H-isoquinolin-2-yl]-N-methyl-2-phenylacetamide;hydrochloride
SMILES CNC(=O)C(C1=CC=CC=C1)N2CCC3=CC(=C(C=C3C2CCC4=CC=C(C=C4)C(F)(F)F)OC)OC.Cl
Standard InChIKey BYGBTDRDPBJUBB-LHIMUUITSA-N
Standard InChI InChI=1S/C29H31F3N2O3.ClH/c1-33-28(35)27(20-7-5-4-6-8-20)34-16-15-21-17-25(36-2)26(37-3)18-23(21)24(34)14-11-19-9-12-22(13-10-19)29(30,31)32;/h4-10,12-13,17-18,24,27H,11,14-16H2,1-3H3,(H,33,35);1H/t24-,27+;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Almorexant hydrochloride

DescriptionAlmorexant HCl is an orally active, dual antagonist of orexin receptor with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively.
TargetsOX2OX1    
IC503.4 nM6.6 nM    

Almorexant hydrochloride Dilution Calculator

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Almorexant hydrochloride Molarity Calculator

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Preparing Stock Solutions of Almorexant hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8214 mL 9.1071 mL 18.2143 mL 36.4285 mL 45.5357 mL
5 mM 0.3643 mL 1.8214 mL 3.6429 mL 7.2857 mL 9.1071 mL
10 mM 0.1821 mL 0.9107 mL 1.8214 mL 3.6429 mL 4.5536 mL
50 mM 0.0364 mL 0.1821 mL 0.3643 mL 0.7286 mL 0.9107 mL
100 mM 0.0182 mL 0.0911 mL 0.1821 mL 0.3643 mL 0.4554 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Almorexant hydrochloride

Almorexant is an antagonist of Orexin 1 receptor (OX1R) and Orexin 2 receptor (OX2R) with Kd values of 1.3nM and 0.17nM, respectively [1].

Almorexant is a dual OX antagonist. It inhibits the binding of orexin-A to both OX1R and OX2R with IC50 values of 6.6nM and 3.4nM, respectively. In the inositol phosphates assay, almorexant acts as a competitive antagonist of hOX1R but a noncompetitive-like antagonist of hOX2R. Besides that, almorexant is found to block the increase in locomotor activity induced by ICV orexin in C57BL/6 mice. Furthermore, almorexant shows effects on sleep in multiple species, including man. It reduces the time spent awake and increased the time spent in NREM and REM sleep dose-dependently in normal C57BL/6 mice. These effects on sleep caused by almorexant are mediated by OX2Rs as almorexant has no effect in mice lacking both OX1R and OX2R but has effects in mice lacking only OX1R [1, 2].

References:
[1] Malherbe P, Borroni E, Pinard E, Wettstein JG, Knoflach F. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31.
[2] Mang GM1, Dürst T, Bürki H, Imobersteg S, Abramowski D, Schuepbach E, Hoyer D, Fendt M, Gee CE. The dual orexin receptor antagonist almorexant induces sleep and decreases orexin-induced locomotion by blocking orexin 2 receptors. Sleep. 2012 Dec 1;35(12):1625-35.

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Description

Almorexant hydrochloride (ACT 078573 hydrochloride) 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, respectively.

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