1. Metabolic Enzyme/Protease
  2. 5-Lipoxygenase
  3. PF-4191834

PF-4191834 (Synonyms: PF-04191834)

Cat. No.: HY-117048 Purity: >99.0%
Handling Instructions

PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (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.

For research use only. We do not sell to patients.

PF-4191834 Chemical Structure

PF-4191834 Chemical Structure

CAS No. : 1029317-21-2

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5 mg USD 190 Get quote

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Description

PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (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].

IC50 & Target

IC50: 229 nM (5-LOX), 130 nM (human 5-LOX)[1]

In Vitro

PF-4191834 (PF-04191834) inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC50 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[1].
PF-4191834 (PF-04191834) exerts a concentration-dependent inhibition of human 5-LOX, with an IC50 value of 130 nM and an IC80 value of 370 nM[1].

Molecular Weight

393.50

Formula

C₂₂H₂₃N₃O₂S

CAS No.

1029317-21-2

SMILES

O=C(C1(C2=CC=CC(SC3=CC=C(C4=CC=NN4C)C=C3)=C2)CCOCC1)N

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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PF-4191834
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HY-117048
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