mPGES1-IN-3
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM).
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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: 1469976-70-2
- 分子式: C24H16ClF5N4O3
- 分子量:538.85
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 8 nM (mPGES-1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.9 μM
Compound: 17d
|
Inhibition of mPGES-1 in human A549 cells assessed as reduction in IL-1beta-induced PGF2alpha production incubated for 24 hrs by enzyme immunoassay
Inhibition of mPGES-1 in human A549 cells assessed as reduction in IL-1beta-induced PGF2alpha production incubated for 24 hrs by enzyme immunoassay
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[PMID: 27865703] |
| A549 | IC50 |
16.24 nM
Compound: 17d
|
Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay
Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay
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[PMID: 27865703] |
| CHO | IC50 |
>10000 nM
Compound: 17d
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Inhibition of rat mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min
Inhibition of rat mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min
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[PMID: 27865703] |
| CHO | IC50 |
10.79 nM
Compound: 17d
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Inhibition of guinea pig mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min
Inhibition of guinea pig mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min
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[PMID: 27865703] |
| CHO | IC50 |
8 nM
Compound: 17d
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Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH
Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH
|
[PMID: 27865703] |
| CHO | IC50 |
>10000 nM
Compound: 17d
|
Inhibition of mouse mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min
Inhibition of mouse mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min
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[PMID: 27865703] |
化学情報
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CAS 番号 1469976-70-2
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分子量 538.85
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分子式 C24H16ClF5N4O3
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SMILES
O=C(NC1=CC(F)=CC(C(F)(F)F)=C1)C2=C(OCCO3)C3=C(N(C)C(NC4=C(Cl)C=CC=C4F)=N5)C5=C2
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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)
mPGES1-IN-3 関連分類
HY-100864 関連分類
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