| Identification | Back Directory | [Name]
HZ-52 | [CAS]
1077626-51-7 | [Synonyms]
HZ-52
MLNIGXYHGQLWLD-UHFFFAOYSA-N
2-[[4-([1,1'-biphenyl]-4-ylaMino)-6-chloro-2-pyriMidinyl]thio]octanoic Acid
Octanoic acid, 2-[[4-([1,1'-biphenyl]-4-ylamino)-6-chloro-2-pyrimidinyl]thio]- | [Molecular Formula]
C24H26ClN3O2S | [MDL Number]
MFCD28138598 | [MOL File]
1077626-51-7.mol | [Molecular Weight]
456 |
| Chemical Properties | Back Directory | [Boiling point ]
625.3±55.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥10mg/mL | [form ]
powder | [pka]
3.03±0.21(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
A potent, reversible inhibitor of 5-lipoxygenase, blocking leukotriene synthesis with an IC50 value of 0.7 μM in intact human polymorphonuclear leukocytes. It also attenuates leukotriene B4 synthesis, prevents carrageenan-induced pleurisy, and protects against platelet-activating factor-induced shock in mice when given intraperitoneally. | [Definition]
ChEBI: HZ52 is a member of biphenyls. | [Biological Activity]
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]. | [storage]
Store at -20°C | [References]
[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. |
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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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