LY3023703
LY3023703 is an orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor. LY3023703 inhibits the production of PGE2. LY3023703 is applicable to research related to inflammatory diseases and osteoarthritis pain.
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- No. CAS: 1415089-24-5
- Fòrmula: C23H22F5N5O2
- Peso molecular:495.45
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
12 nM
Compound: 20
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Inhibition of mPGES-1 in human A549 cells assessed as PEG2 formation preincubated for 30 mins followed by recombinant human interleukin 1beta addition measured after 18 hrs by LC/MS analysis
Inhibition of mPGES-1 in human A549 cells assessed as PEG2 formation preincubated for 30 mins followed by recombinant human interleukin 1beta addition measured after 18 hrs by LC/MS analysis
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[PMID: 26791385] |
LY3023703 (Compound 8) potently inhibits human mPGES-1 microsomes, with an IC50 of 0.9 nM[1].
LY3023703 weakly inhibits rat mPGES-1 microsomes, with an IC50 value of 33.9 μM[1].
LY3023703 inhibits the production of PGE2 in IL-1β-stimulated A549 cells with an IC50 of 12 nM, without affecting the production of PGI2[1].
LY3023703 inhibits LPS (HY-D1056)-stimulated PGE2 production in human whole blood, with an IC50 of 12 nM and an IC80 of 69 nM, without affecting the production of TXB2 or PGF2α[1].
LY3023703 inhibits LPS-stimulated PGE2 production in canine whole blood, with an IC50 of 139 nM and an IC80 of 703 nM[1].
LY3023703 (10 μM; 30 min preincubation, 1 min reaction) weakly inhibits microsomal CYP3A4 in a time-dependent manner[1].
LY3023703 inhibits hERG channels with an IC50 of 82.6 μM, compared with an IC80 of 69 nM against HWB PGE2[1].
LY3023703 (Compound 2) potently inhibits mPGES-1-mediated PGE2 production in human whole blood, with an IC50 of 0.012 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1415089-24-5
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Peso molecular 495.45
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Fòrmula C23H22F5N5O2
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SMILES
O=C(C1=CC(CNC(C(C)C)=O)=CN=C1C(F)F)NC2=NC(C)=C(C3=CC=C(C(F)(F)F)C=C3)N2
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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
[1]. Schiffler MA, et al. Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. J Med Chem. 2016;59(1):194-205. [Content Brief]
[2]. Norman BH, et al. Identification and Mitigation of Reactive Metabolites of 2-Aminoimidazole-Containing Microsomal Prostaglandin E Synthase-1 Inhibitors Terminated Due to Clinical Drug-Induced Liver Injury. J Med Chem. 2018;61(5):2041-2051. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY3023703 Related Classifications
HY-182647 Related Classifications
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