Pitolisant oxalateNonimidazole inverse agonist CAS# 362665-57-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 362665-57-4 | SDF | Download SDF |
PubChem ID | 23137286 | Appearance | Powder |
Formula | C19H28ClNO5 | M.Wt | 385.88 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : 50 mg/mL (129.57 mM; Need ultrasonic) | ||
Chemical Name | 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine;oxalic acid | ||
SMILES | C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl.C(=O)(C(=O)O)O | ||
Standard InChIKey | OZTKSXOIWBLDBB-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C17H26ClNO.C2H2O4/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19;3-1(4)2(5)6/h7-10H,1-6,11-15H2;(H,3,4)(H,5,6) | ||
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. |
Pitolisant oxalate Dilution Calculator
Pitolisant oxalate Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.5915 mL | 12.9574 mL | 25.9148 mL | 51.8296 mL | 64.787 mL |
5 mM | 0.5183 mL | 2.5915 mL | 5.183 mL | 10.3659 mL | 12.9574 mL |
10 mM | 0.2591 mL | 1.2957 mL | 2.5915 mL | 5.183 mL | 6.4787 mL |
50 mM | 0.0518 mL | 0.2591 mL | 0.5183 mL | 1.0366 mL | 1.2957 mL |
100 mM | 0.0259 mL | 0.1296 mL | 0.2591 mL | 0.5183 mL | 0.6479 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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Description: IC50 Value: 0.16 nM(Ki value); 1.5 nM(EC50) [1] Pitolisant (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor. BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan. in vitro: BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan. Pitolisant in vitro potency was approximately 6 times lower at the rodent receptor [1]. in vivo: In mice, the oral bioavailability coefficient, i.e., the ratio of plasma areas under the curve after oral and i.v. administrations, respectively, was 84%. BF2.649 dose dependently enhanced tele-methylhistamine levels in mouse brain, an index of histaminergic neuron activity, with an ED50 value of 1.6 mg/kg p.o., a response that persisted after repeated administrations for 17 days [1]. A statistically significant suppressive effect (standardized photosensitive response [SPR] reduction as measured with paired t-tests) for 20-, 40-, or 60-mg doses of pitolisant was seen in 9/14 (64%) patients of whom 6/14 (43%) showed abolition of the response to intermittent photic stimulation (IPS) [2]. BF2.649 showed significant inhibitory activity in several mouse models of schizophrenia [3]. Clinical trial: HARMONYIII: Long-term, Open-label Study in Narcolepsy With BF2.649 (Pitolisant). Phase3
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