1221971-47-6
1221971-47-6 structure
- Name: PF 9184
- Chemical Name: pf-9184
- CAS Number: 1221971-47-6
- Molecular Formula: C21H14Cl2N2O4S
- Molecular Weight: 461.31800
- Catalog: Signaling Pathways Immunology/Inflammation PGE synthase
- Create Date: 2018-01-23 07:18:44
- Modify Date: 2024-01-15 12:33:28
-
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro[1].
| Name | pf-9184 |
|---|---|
| Synonyms | N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide |
| Description | PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 16.5 nM (mPGES-1)[1] |
| In Vitro | PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in rheumatoid arthritis (RASF) in synovial fibroblasts derived from patients and has no apparent cytotoxic effects up to 100 μM[1]. PF-9184 (0.015-100 μM) potently blocks mPGES-1 ability to synthesize PGE2 from PGH2, and with no apparent inhibitory effects on COX-2 and prostacyclin synthase in cells[1]. PF-9184 (0.015-100 μM) inhibits PGE2 weakly but has no effect on TXB2 synthesis except at 100 μM in human whole blood and modified blood assays[1]. PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM)[1]. |
| In Vivo | PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1]. |
| References |
| Molecular Formula | C21H14Cl2N2O4S |
|---|---|
| Molecular Weight | 461.31800 |
| Exact Mass | 460.00500 |
| PSA | 103.88000 |
| LogP | 6.30020 |
| Hazard Codes | Xi |
|---|