PF-4191834 (Synonyms: PF-04191834) |
| رقم الكتالوجGC36883 |
PF-4191834 (PF-04191834) هو مثبط نشط شفويًا وغير مخلب للأكسدة وغير مؤكسد لـ 5-Lipoxygenase (5-LOX) (IC50 = 229 نانومتر) ، ويعرض انتقائية بمقدار 300 ضعف تقريبًا لـ 5-LOX أكثر من 12 -LOX و 15-LOX ، لا يظهر أي نشاط تجاه إنزيمات الأكسدة الحلقية ، وهو فعال في الالتهاب والألم
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Cas No.: 1029317-21-2
Sample solution is provided at 25 µL, 10mM.
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PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain[1]. IC50: 229 nM (5-LOX), 130 nM (human 5-LOX)[1]
PF-4191834 (PF-04191834) inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC50 values between 100 and 190 nM and do not inhibit significantly the COX-1/2 enzymes or the 12- or 15-LOX enzymes at concentrations up to 30 μM[1].PF-4191834 (PF-04191834) exerts a concentration-dependent inhibition of human 5-LOX, with an IC50 value of 130 nM and an IC80 value of 370 nM[1].
[1]. Masferrer JL, et al. Pharmacology of PF-4191834, a novel, selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. J Pharmacol Exp Ther. 2010 Jul;334(1):294-301.
| Cas No. | 1029317-21-2 | SDF | |
| المرادفات | PF-04191834 | ||
| Canonical SMILES | O=C(C1(C2=CC=CC(SC3=CC=C(C4=CC=NN4C)C=C3)=C2)CCOCC1)N | ||
| Formula | C22H23N3O2S | M.Wt | 393.5 |
| الذوبان | Soluble in DMSO | 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 | 2.5413 mL | 12.7065 mL | 25.413 mL |
| 5 mM | 0.5083 mL | 2.5413 mL | 5.0826 mL |
| 10 mM | 0.2541 mL | 1.2706 mL | 2.5413 mL |
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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.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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