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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 851728-60-4
- 分子式: C21H17Cl2F2N3O2
- 分子量:452.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
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Cell Line
|
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 |
化学情報
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CAS 番号 851728-60-4
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分子量 452.28
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)