PF-514273
PF-514273 is an orally active, selective antagonist for cannabinoid-1 receptor (CB1) with IC50 of 1 nM. PF-514273 reduces the food uptake in mice, and can be used for obesity research.
For research use only. We do not sell to patients.
- CAS No.: 851728-60-4
- Formula: C21H17Cl2F2N3O2
- Molecular Weight:452.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HTLA | EC50 |
>10 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in agonist mode with target: APLNR
GPCR PRESTO-Tango dose-response in agonist mode with target: APLNR
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
0.001 mM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
1.06 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRA2A
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRA2A
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
1.21033 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4
GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
1.25937 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1
GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
1.43821 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
17.5642 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1
GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
2.04185 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in agonist mode with target: ADGRF1
GPCR PRESTO-Tango dose-response in agonist mode with target: ADGRF1
|
10.6019/CHEMBL5442687 |
| HTLA | EC50 |
2.26515 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R
GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R
|
10.6019/CHEMBL5442687 |
| HTLA | IC50 |
>10 μM
Compound: EUB0000810a
|
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
|
10.6019/CHEMBL5442687 |
Chemical Information
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CAS No. 851728-60-4
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Molecular Weight 452.28
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Formula C21H17Cl2F2N3O2
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SMILES
O=C1N(CC(F)(F)C)CCOC2=C(C3=CC=C(Cl)C=C3)N(C4=CC=CC=C4Cl)N=C12
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Dow RL, et al., Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[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. J Med Chem. 2009 May 14;52(9):2652-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)