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435801 Licofelone, Potassium Salt, Monohydrate - CAS 156897-06-2 - Calbiochem

435801
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435801-25MG
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      Glasflasche 25 mg
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      Description
      OverviewA cell-permeable, orally active arylpyrrolizine carboxylate that is structurally and pharmacologically similar to, but less potent than, MK-886 (Cat. No. 475889). Effectively suppresses cellular Cox pathway PGE2 production by inhibiting COX-1 and mPGES-1, but not COX-2 (IC50 = 0.8, 6, and >30 µM, respectively), and inhibits cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation (IC50 = 0.18 to 3.6 µM against ionophore-stimulated LB4 production from bovine and human PMNL, respectively) by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity. Unlike NSAIDs that target only COX pathway, Licofelone does not cause gastrointestinal damages when applied in vivo.
      Catalogue Number435801
      Brand Family Calbiochem®
      Synonyms2,2-Dimethyl-6-(4-chlorophenyl)-7-phenyl, 2,3-dihydro-1H-pyrrolizine-5-yl)-acetic acid, ML3000, ML-3000, COX-1 Inhibitor V, FLAP Inhibitor II, mPGES-1 Inhibitor II
      References
      ReferencesLaufer, S. A., et al. 1994. Arzneimittelforschung. 44, 629.
      Laufer, S., et al. 1994. Arzneimittelforschung. 45, 27.
      Wallace, J. L., et al. 1994. Eur J Pharmacol. 271, 525.
      Alvaro-Garcia, J. M., et al. 2004. Rheumatology. 43 Supple1, i21.
      Koeberle, A., et al. 2008. J Pharmacol Exp Ther. 326, 975.
      Fischer, L., et al. 2007. Br J Pharmacol. 152, 471.
      Laufer, S. A., et al. 1994. J Med Chem. 37, 1894.
      Vidal, C., et al. 2007. J Pharmacol Exp Ther. 320, 108.
      Liedtke, A. J., et al. 2009. J Med Chem. 52, 4968.
      Bias, P., et al. 2004. Am J Gastroenterol. 99, 611.
      Product Information
      CAS number156897-06-2
      FormWhite powder
      Hill FormulaC₂₃H₂₁ClKNO₂•H₂O
      Chemical formulaC₂₃H₂₁ClKNO₂•H₂O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary Target5-LOX
      Primary Target IC<sub>50</sub>0.21 µ
      Secondary targetCOX
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsUnstable in solution. Reconstitute just prior to use.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      435801-25MG 04055977210323