| HZ525-lipoxygenase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
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| 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. | ||
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.
