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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- No. CAS: 1469976-70-2
- Fòrmula: C24H16ClF5N4O3
- Peso molecular:538.85
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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
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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
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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
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[PMID: 27865703] |
| CHO | IC50 |
>10000 nM
Compound: 17d
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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] |
Chemical Information
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No. CAS 1469976-70-2
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Peso molecular 538.85
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
mPGES1-IN-3 Related Classifications
HY-100864 Related Classifications
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