AF3442
AF3442 is a potent and selective mPGES-1 inhibitor (IC50 = 0.06 μM) which reduces monocyte PGE2 generation also in the presence of plasma proteins. AF3442 shows selectivity over other prostanoids (TXB2, PGF2α and 6-keto-PGF1α). AF3442 can be used for research in analgesia.
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: 924636-93-1
- 分子式: C22H17F3N2O
- 分子量:382.38
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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
IC50 & Target
[1]|
mPGES-1 0.06 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.06 μM
Compound: S7
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Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
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[PMID: 26088337] |
体外実験
AF3442 (0.01-10 μM, 15 min) causes a concentration-dependent inhibition of PGE2 generation by human recombinant mPGES-1 with an IC50 of 0.06 μM[1].
AF3442 (0.01-100 μM, 24 h) causes a concentration-dependent reduction of PGE2 biosynthesis (IC50 = 0.41 μM), while at 100 μM, the inhibition of PGE2 was associated with a reduction in TXB2, suggesting a possible off-target effect on COX-2 activity and expression[1].
AF3442 (0.01-100 μM, 24 h) significantly reduces COX-2 levels in lipopolysaccharide (LPS) (HY-D1056)-stimulated human monocytes specifically at 100 μM, without affecting COX-1, mPGES-1, mPGES-2, cPGES and TXS levels[1].
AF3442 (0.01-100 μM, 24 h) is a selective inhibitor of mPGES-1 in LPS-stimulated human whole blood, as evidenced by causing a potent inhibition of PGE2 by approximately 70% at 100 μM without significantly affecting other prostanoids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LPS-stimulated human monocytes
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Concentration:0.01, 0.1, 1, 10 and 100 μM
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Incubation Time:24 h
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Result:Did not significantly affect the levels of COX-2, COX-1, mPGES-1, mPGES-2, cPGES and TXS at concentrations up to 10 μM.
Caused a significant reduction only of COX-2 levels by 31.4% at 100 μM, without affecting the other proteins.
化学情報
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CAS 番号 924636-93-1
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分子量 382.38
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分子式 C22H17F3N2O
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SMILES
O=C(NC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3)C4=CC=CC=C4C(F)(F)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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)