PF-3052334
PF-3052334 is an orally active, hepatically selective HMG-CoA reductase inhibitor with an IC50 of 1.9 nM. PF-3052334 inhibits cholesterol synthesis, with IC50 values of 0.9 and 730 nM in hepatocytes and muscle cells, respectively. PF-3052334 can be used to study hypercholesterolemia.
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: 887702-61-6
- 分子式: C28H33FN3NaO5
- 分子量:533.57
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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
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
0.9 nM
Compound: 35, PF-3052334
|
Inhibition of cholesterol synthesis in rat hepatocytes
Inhibition of cholesterol synthesis in rat hepatocytes
|
[PMID: 18072721] |
| L6 | IC50 |
730 nM
Compound: 35, PF-3052334
|
Inhibition of cholesterol synthesis in rat L6 cells
Inhibition of cholesterol synthesis in rat L6 cells
|
[PMID: 18072721] |
体内実験
PF-3052334 (20 mg/kg, p.o., once daily for 7 days) causes low density lipoprotein (LDL) reduction in guinea pigs with an ED50 of 3.6 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute cholesterol synthesis inhibition model established in Male Syrian hamster (Golden hamster)[1]
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Dosage:10 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Significantly inhibited cholesterol synthesis at both 2-4 h and 4-6 h.
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Animal Model:Chronic LDL-C reduction experiment established in male Hartley guinea pig[1]
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Dosage:20 mg/kg
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Administration:Oral administration (p.o.), once daily for 7 days
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Result:Reduced LDL-C by 45%
化学情報
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CAS 番号 887702-61-6
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分子量 533.57
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分子式 C28H33FN3NaO5
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SMILES
O=C(O[Na])C[C@H](O)C[C@H](O)CCC1=C(C(C)C)C(C(NCC2=CC=C(C=C2)C)=O)=NN1C3=CC=C(C=C3)F
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)