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Submit ReviewPF 514273
Description: High affinity and selective CB1 antagonist
Chemical Name: 2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one
Purity: ≥98% (HPLC)
Biological Activity for PF 514273
PF 514273 is a high affinity 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.
Technical Data for PF 514273
| M. Wt | 452.28 |
| Formula | C21H17Cl2F2N3O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 851728-60-4 |
| PubChem ID | 11316919 |
| InChI Key | FJMQJSUOOGOWBD-UHFFFAOYSA-N |
| Smiles | O=C2C1=NN(C4=CC=CC=C4Cl)C(C3=CC=C(Cl)C=C3)=C1OCCN2CC(C)(F)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for PF 514273
References for PF 514273
References are publications that support the biological activity of the product.
Dow et al (2009) Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazole[3,4-f][1,4]oxazepin-8-(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of J.Med.Chem. 52 2652 PMID: 19351113
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Keywords: PF 514273, PF 514273 supplier, Potent, and, selective, CB1, agonists, cannabinoids, Receptors, PF514273, cb1r, 3676, Tocris Bioscience
1 Citation for PF 514273
Citations are publications that use Tocris products. Selected citations for PF 514273 include:
Rozenfeld et al (2011) AT1R-CB1R heteromerization reveals a new mechanism for the pathogenic properties of angiotensin II. EMBO J 30 2350 PMID: 21540834
Reviews for PF 514273
Average Rating: 4 (Based on 1 Review.)
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Works as described.
By
Anonymous on 05/14/2019
Assay Type: In Vivo
Species: Mouse
Used in vivo for mouse behavioral work to test CB1 receptor involvement in alcohol reward learning and seeking behavior. Data show product did work centrally, as it reduced locomotor activity.
Drug can be difficult to get into solution, as would be expected for a cannabinoid compound. So don't expect to use high concentrations unless you are OK w/ using in suspension.
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