PF 514273Potent and selective CB1 antagonist CAS# 851728-60-4 |
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Quality Control & MSDS
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Chemical structure
3D structure
Cas No. | 851728-60-4 | SDF | Download SDF |
PubChem ID | 11316919 | Appearance | Powder |
Formula | C21H17Cl2F2N3O2 | M.Wt | 452.28 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO and to 50 mM in ethanol | ||
Chemical Name | 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-5,6-dihydropyrazolo[3,4-f][1,4]oxazepin-8-one | ||
SMILES | CC(CN1CCOC2=C(N(N=C2C1=O)C3=CC=CC=C3Cl)C4=CC=C(C=C4)Cl)(F)F | ||
Standard InChIKey | FJMQJSUOOGOWBD-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C21H17Cl2F2N3O2/c1-21(24,25)12-27-10-11-30-19-17(20(27)29)26-28(16-5-3-2-4-15(16)23)18(19)13-6-8-14(22)9-7-13/h2-9H,10-12H2,1H3 | ||
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 | Potent and selective CB1 receptor antagonist (Ki values are 1 and > 10000 nM at CB1 and CB2 receptors respectively). Inhibits food intake in vivo following oral administration. |
PF 514273 Dilution Calculator
PF 514273 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.211 mL | 11.0551 mL | 22.1102 mL | 44.2204 mL | 55.2755 mL |
5 mM | 0.4422 mL | 2.211 mL | 4.422 mL | 8.8441 mL | 11.0551 mL |
10 mM | 0.2211 mL | 1.1055 mL | 2.211 mL | 4.422 mL | 5.5275 mL |
50 mM | 0.0442 mL | 0.2211 mL | 0.4422 mL | 0.8844 mL | 1.1055 mL |
100 mM | 0.0221 mL | 0.1106 mL | 0.2211 mL | 0.4422 mL | 0.5528 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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Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyraz olo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.[Pubmed:19351113]
J Med Chem. 2009 May 14;52(9):2652-5.
We report the design, synthesis, and structure-activity relationships of novel bicyclic lactam-based cannabinoid type 1 (CB(1)) receptor antagonists. Members of these series are potent, selective antagonists in in vitro/in vivo efficacy models of CB(1) antagonism and exhibit robust oral activity in rodent models of food intake. These efforts led to the identification of 19d, which has been advanced to human clinical trials for weight management.
Effects of the novel cannabinoid CB1 receptor antagonist PF 514273 on the acquisition and expression of ethanol conditioned place preference.[Pubmed:24954022]
Alcohol. 2014 Aug;48(5):427-31.
The centrally expressed cannabinoid receptor (CB1) has been considered a potential therapeutic target in treating alcoholism. Though CB1 receptors have been shown to modulate primary and conditioned ethanol reward, much of this research employed animal models that require ethanol ingestion or oral routes of administration. This is problematic considering CB1 antagonist drugs have high anorectic liability and have been used clinically in the treatment of obesity. Therefore, the present study examined CB1 antagonism in DBA/2J mice using an unbiased ethanol-induced conditioned place preference (CPP) procedure, a paradigm that does not require ethanol ingestion. To evaluate the role of CB1 receptors in primary ethanol reward, the highly potent and selective novel CB1 antagonist 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyraz olo[3,4-f][1,4]oxazepin-8(5H)-one (PF 514273) was administered 30 min before place preference conditioning with a fixed dose of ethanol (acquisition). To evaluate the role of CB1 receptors in ethanol-conditioned reward, PF 514273 was administered 30 min before place preference testing (expression). Although PF 514273 reduced ethanol-stimulated and basal locomotor activity, it did not perturb the acquisition or expression of ethanol-induced CPP. Results from the present study appear inconsistent with other studies that have demonstrated a role for CB1 antagonism in ethanol reward using oral administration paradigms. Our findings suggest that CB1 antagonism may have greater involvement in consummatory behavior than ethanol reward.