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.
For research use only. We do not sell to patients.
- CAS No.: 924636-93-1
- Formula: C22H17F3N2O
- Molecular Weight:382.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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mPGES-1 0.06 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| 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] |
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.
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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.
Chemical Information
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CAS No. 924636-93-1
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Molecular Weight 382.38
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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