HZ52 |
| Catalog No.GC12159 |
HZ52는 온전한 인간 다형핵 백혈구에서 0.7μM의 IC50으로 류코트리엔 합성을 차단하는 강력하고 가역적인 5-리폭시게나제 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1077626-51-7
Sample solution is provided at 25 µL, 10mM.
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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 | |
| 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 |
| Solubility | ≤10mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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