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HZ52 5-lipoxygenase inhibitor

Catalog No.C4199
Size Price Stock Qty
5mg
$104.00
In stock
10mg
$192.00
In stock
25mg
$436.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

HZ52

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Chemical Properties

Cas No. 1077626-51-7 SDF Download SDF
Chemical Name 2-(4-(bipheny-4-ylamino)-6-chloropyrimidiny-2-ylthio)-octanoic acid
Canonical SMILES ClC1=CC(NC2=CC=C(C3=CC=CC=C3)C=C2)=NC(SC(CCCCCC)C(O)=O)=N1
Formula C24H26ClN3O2S M.Wt 456.0
Solubility ≤10mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

2-(4-(biphenyl-4-ylamino)-6-chloropyrimidin-2- ylthio)octanoic acid (HZ52) is an inhibitor for 5-Lipoxygenase (5-LO) [1]. 5-Lipoxygenase (5-LO), the key enzyme involved in the biosynthesis of pro-inflammatory leukotrienes (LTs), is a potential target for pharmacological intervention with inflammation and allergic disorders [1].

In vitro: In cell-free assays using partially purified recombinant 5-LO enzyme, HZ52 inhibited 5-LO with an IC50 of 1.5 μM. In PMNL homogenates, HZ52 inhibited 5-LO with an IC50 of 9 μM [1]. HZ52 (10 or 30 μM) promoted 5-LO translocation to the nuclear membrane in PMNL [1]. The cell-based and cell-free assays revealed that inhibition of 5-LO by HZ52 did not depend on radical scavenging properties and was reversible [1].

In vivo: In rats with carrageenan-induced pleurisy and in mice bearing platelet-activating factor (PAF)-induced lethal shock, HZ52 (1.5 mg/kg, i.p) prevented carrageenan-induced pleurisy accompanied by reducing LTB4 levels. HZ52 protected mice (10 mg/kg, i.p) against PAF-induced shock. [1].

Reference:
[1] Greiner C, Hrnig C, Rossi A, et al.  2‐(4‐(Biphenyl‐4‐ylamino)‐6‐chloropyrimidin‐2‐ylthio) octanoic acid (HZ52)–a novel type of 5‐lipoxygenase inhibitor with favourable molecular pharmacology and efficacy in vivo[J]. British journal of pharmacology, 2011, 164(2b): 781-793.