Description
2-(4-(biphenyl-4-ylamino)-6-chloropyrimidin-2- ylthio)octanoic acid (HZ52) is an inhibitor for 5-Lipoxygenase (5-LO) . 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 . 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 . HZ52 (10 or 30 μM) promoted 5-LO translocation to the nuclear membrane in PMNL . 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 . 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. .
Product information
CAS Number: 1077626-51-7
Molecular Weight: 456.00
Formula: C24H26ClN3O2S
Chemical Name: 2-{[4-({[1,1'-biphenyl]-4-yl}amino)-6-chloropyrimidin-2-yl]sulfanyl}octanoic acid
Smiles: CCCCCCC(SC1N=C(C=C(Cl)N=1)NC1C=CC(=CC=1)C1C=CC=CC=1)C(O)=O
InChiKey: MLNIGXYHGQLWLD-UHFFFAOYSA-N
InChi: InChI=1S/C24H26ClN3O2S/c1-2-3-4-8-11-20(23(29)30)31-24-27-21(25)16-22(28-24)26-19-14-12-18(13-15-19)17-9-6-5-7-10-17/h5-7,9-10,12-16,20H,2-4,8,11H2,1H3,(H,29,30)(H,26,27,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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