Almorexant hydrochlorideOX1R/OX2R antagonist CAS# 913358-93-7 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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. | ||
| Description | Almorexant 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. | |||||
| Targets | OX2 | OX1 | ||||
| IC50 | 3.4 nM | 6.6 nM | ||||
Almorexant hydrochloride Dilution Calculator
Almorexant hydrochloride Molarity Calculator
| 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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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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