HZ52
目录号 : GC12159
A reversible inhibitor of 5-lipoxygenase
Cas No.:1077626-51-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 1077626-51-7 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C24H26ClN3O2S | 分子量 | 456.0 |
| 溶解度 | ≤10mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.193 mL | 10.9649 mL | 21.9298 mL |
| 5 mM | 0.4386 mL | 2.193 mL | 4.386 mL |
| 10 mM | 0.2193 mL | 1.0965 mL | 2.193 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。