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

435801
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      Overview

      Replacement Information

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      435801-25MG
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      In Stock 
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          Glass bottle 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 Image
          Applications
          Biological Information
          Primary Target5-LOX
          Primary Target IC<sub>50</sub>0.21 µ
          Secondary targetCOX
          Purity≥99% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          References

          Reference overview
          Laufer, 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.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision14-June-2013 JSW
          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
          DescriptionA cell-permeable, orally active arylpyrrolizine carboxylate that is both structurally and pharmacologically similar to, but less potent than, MK-886 (Cat. No. 475889). Both MK-886 and Licofelone effectively suppress cellular Cox pathway PGE2 (prostaglandin E2) production by inhibiting COX-1 and mPGES-1 (microsomal PGE2 synthase-1), but not COX-2 (IC50 = 0.8, 6, and >30 µM, respectively, by Licofelone), and both compounds suppress cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation (IC50 = 0.18 to 3.6 µM against ionophore-stimulated bovine and human PMNL LB4 production by Licofelone) by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity (No inhibition up to 10 µM Licofelone). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, Licofelone does not cause gastrointestinal damages when applied in vivo.
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number156897-06-2
          Chemical formulaC₂₃H₂₁ClKNO₂•H₂O
          Structure formula
          Purity≥99% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -20°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsUnstable in solution. Reconstitute just prior to use.
          Toxicity Standard Handling
          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.