| Identification | Back Directory | [Name]
PF04191834 | [CAS]
1029317-21-2 | [Synonyms]
PF04191834
PF-4191834
PF-4191834 >=98% (HPLC)
2H-Pyran-4-carboxamide, tetrahydro-4-[3-[[4-(1-methyl-1H-pyrazol-5-yl)phenyl]thio]phenyl]- | [Molecular Formula]
C22H23N3O2S | [MOL File]
1029317-21-2.mol | [Molecular Weight]
393.5 |
| Chemical Properties | Back Directory | [Melting point ]
173 °C | [Boiling point ]
663.0±55.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
15.78±0.20(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain[1]. | [Biological Activity]
PF-4191834 (PF-04191834) is an orally active, non-iron-chelating, non-redox 5-lipoxygenase (5-LOX) inhibitor (IC50=229 nM), 5-LOX is about 300 times more selective than 12-LOX and 15-LOX, has no activity against cyclooxygenase, and is effective against inflammation and pain. | [in vitro]
PF-4191834 (PF-04191834) inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC 50 values between 100 and 190 nM and do not inhibit significantly the COX-1/2 enzymes or the 12- or 15-LOX enzymes at concentrations up to 30 μM. PF-4191834 (PF-04191834) exerts a concentration-dependent inhibition of human 5-LOX, with an IC 50 value of 130 nM and an IC 80 value of 370 nM. | [target]
| [IC 50]
5-LOX | [storage]
Store at -20°C | [References]
[1] Masferrer JL, et al. Pharmacology of PF-4191834, a novel, selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. J Pharmacol Exp Ther. 2010 Jul;334(1):294-301. DOI:10.1124/jpet.110.166967 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|