الصفحة الرئيسية>>Signaling Pathways>> Proteases>> Lipoxygenase>>5-Lipoxygenase-In-1

5-Lipoxygenase-In-1

رقم الكتالوجGC31997

5-Lipoxygenase-In-1 هو مثبط 5-Lipoxygenase مستخرج من براءة اختراع EP 331232 A2 ، الجدول 4 ، مثال مركب 4.10

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5-Lipoxygenase-In-1 التركيب الكيميائي

Cas No.: 125235-15-6

الحجم السعر المخزون الكميّة
10mM (in 1mL Water)
257٫00
متوفر
5mg
234٫00
متوفر
10 mg
378٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of 5-Lipoxygenase-In-1

5-Lipoxygenase-In-1 is a 5-Lipoxygenase inhibitor extracted from patent EP 331232 A2, table 4, compound example 4.10.

[1]. Wauwe V, et al. 5-Lipoxygenase-inhibiting 4-(4-phenyl-1-piperazinyl)phenols and their preparation and pharmaceutical compositions. EP0331232A2

Protocol of 5-Lipoxygenase-In-1

Kinase experiment:

The enzyme activity is assayed at 37°C in a reaction mixture (total volume of 0.4 mL) containing 50 mM sodium phosphate buffer (pH7.4), 2mM ATP, 2mM CaC12, 2mM glutathion, 5-Lipoxygenase-In-1 (10-5 to 10-8 M) and the enzyme (60 mg protein). For inhibition studies, concentration response curves and IC50-values are obtained by determining the percentage of inhibition of lipoxygenase products formation in the presence of 5-Lipoxygenase-In-1 compared with the uninhibited control[1].

Animal experiment:

Mice[1]Unfasted male Swiss mice weighing 24-26 g are used in the experiments. The mice are treated orally with 5-Lipoxygenase-In-1 dissolved in a volume of 150 mL of either polyethyleneglycol (PEG 200) of hydroxypropyl cyclodextrine at doses varying between 1.25 and 40 mg per kg bodyweight. In control experiments the mice are administered an indentical amount of solvent alone. One hour after treatment there is injected intravenously an isotonic saline solution containing 60 mg/mL Dextran T5000 and 13 mg/mL pontamine sky-blue dye in a volume of 0.1 mL per 10 bodyweight. One hour and forty-five minutes later the animals are sacrificed by ether and their ears are removed. Extraction and quantification of the extravasated dye are performed[1].

References:

[1]. Wauwe V, et al. 5-Lipoxygenase-inhibiting 4-(4-phenyl-1-piperazinyl)phenols and their preparation and pharmaceutical compositions. EP0331232A2

Chemical Properties of 5-Lipoxygenase-In-1

Cas No. 125235-15-6 SDF
Canonical SMILES O=C(C(C)(C)N1CC)N(C2=CC=C(N3CCN(C4=CC=C(O)C=C4)CC3)C=C2)C1=S
Formula C23H28N4O2S M.Wt 424.56
الذوبان DMSO: 250 mg/mL (588.84 mM) 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of 5-Lipoxygenase-In-1

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3554 mL 11.7769 mL 23.5538 mL
5 mM 0.4711 mL 2.3554 mL 4.7108 mL
10 mM 0.2355 mL 1.1777 mL 2.3554 mL
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In vivo Formulation Calculator (Clear solution) of 5-Lipoxygenase-In-1

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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.

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