PF04191834
PF04191834 Basic information
- Product Name:
- PF04191834
- Synonyms:
-
- PF04191834
- PF-4191834
- 2H-Pyran-4-carboxamide, tetrahydro-4-[3-[[4-(1-methyl-1H-pyrazol-5-yl)phenyl]thio]phenyl]-
- PF-4191834 >=98% (HPLC)
- PF4191834,Lipoxygenase,PF 4191834,inhibit,LOX,PF 04191834,PF-4191834,PF04191834,Inhibitor
- PF-4191834, 10 mM in DMSO
- 4-(3-((4-(1-Methyl-1H-pyrazol-5-yl)phenyl)thio)phenyl)tetrahydro-2H-pyran-4-carboxamide
- CAS:
- 1029317-21-2
- MF:
- C22H23N3O2S
- MW:
- 393.5
- Mol File:
- 1029317-21-2.mol
PF04191834 Chemical Properties
- 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
PF04191834 Usage And Synthesis
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
| 5-LOX < span> |
IC 50
5-LOX
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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