PF 514273

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Cat.No. 3676 - PF 514273 | C21H17Cl2F2N3O2 | CAS No. 851728-60-4
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)
Datasheet
Citations (1)
Reviews (1)
Literature (6)

Biological Activity

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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.23 100
ethanol 22.61 50

Preparing Stock Solutions

The following data is based on the product molecular weight 452.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.21 mL 11.06 mL 22.11 mL
5 mM 0.44 mL 2.21 mL 4.42 mL
10 mM 0.22 mL 1.11 mL 2.21 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


Do you know of a great paper that uses PF 514273 from Tocris? Please let us know.

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.

PMID: 24954022
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