533304 DHODH Inhibitor, DSM1 - Calbiochem

533304
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₃N₅

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33304.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable triazolopyrimidine compound that potently inhibits malaria parasite Plasmodium falciparum dihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH2 to Coenzyme Q10 (CoQ or ubiquinone) in a potent (IC50 = 47 nM), CoQ-competitive (Ki = 15 nM), and species-specific manner, without affecting PfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 µM). Reported to inhibit the proliferation of P. falciparum parasites (EC50 = 79 nM against 3D7 strain) in vitro, including the drug-resistant strain Dd2 (EC50 = 140 nM), while displaying no inhibitory potency against murine lymphocytic leukemia cell line L1210 even at concentrations as high as 10 µM. DSM1 is not recommended for in vivo use due to reduced plasma exposure upon repeat dosing in mice.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533304
          Brand Family Calbiochem®
          Synonyms5-Methyl-N-(2-naphthyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, Malaria Parasite Dihydroorotate Dehydrogenase Inhibitor, P. falciparum Dihydroorotate Dehydrogenase Inhibitor, Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitor; TCMDC-125840
          References
          ReferencesGuler, J.L., et al. 2013. PLoS Pathog. 9, e1003375.
          Ke, H., et al. 2011. Eukaryot. Cell. 10, 1053.
          Ganesan, S.M., et al. 2011. Mol. Biochem. Parasitol. 177, 29.
          Booker, M.L., et al. 2010. J. Biol. Chem. 285, 33054.
          Gujjar, R., et al. 2009. J. Med. Chem. 52, 1864.
          Phillips, M.A., et al. 2008. J. Med. Chem. 51, 3649.
          Product Information
          FormOff-white solid
          Hill FormulaC₁₆H₁₃N₅
          Chemical formulaC₁₆H₁₃N₅
          ReversibleY
          Applications
          Biological Information
          Primary TargetPf*DHODH
          Primary Target K<sub>i</sub>15 nM)
          Purity≥97% 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 Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          DHODH Inhibitor, DSM1 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Guler, J.L., et al. 2013. PLoS Pathog. 9, e1003375.
          Ke, H., et al. 2011. Eukaryot. Cell. 10, 1053.
          Ganesan, S.M., et al. 2011. Mol. Biochem. Parasitol. 177, 29.
          Booker, M.L., et al. 2010. J. Biol. Chem. 285, 33054.
          Gujjar, R., et al. 2009. J. Med. Chem. 52, 1864.
          Phillips, M.A., et al. 2008. J. Med. Chem. 51, 3649.
          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.

          Revision20-November-2015 JSW
          Synonyms5-Methyl-N-(2-naphthyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, Malaria Parasite Dihydroorotate Dehydrogenase Inhibitor, P. falciparum Dihydroorotate Dehydrogenase Inhibitor, Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitor; TCMDC-125840
          DescriptionA cell-permeable triazolopyrimidine compound that potently inhibits malaria parasite Plasmodium falciparum dihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH2 to Coenzyme Q10 (CoQ or ubiquinone) in a potent (IC50 = 47 nM), CoQ-competitive (Ki = 15 nM), and species-specific manner, without affecting PfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 µM). Reported to inhibit the proliferation of P. falciparum parasites (EC50 = 79 nM against 3D7 strain) in vitro, including the drug-resistant strain Dd2 (EC50 = 140 nM), while displaying no inhibitory potency against murine lymphocytic leukemia cell line L1210 even at concentrations as high as 10 µM. DSM1 is not recommended for in vivo use due to reduced plasma exposure upon repeat dosing in mice.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₁₃N₅
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesGuler, J.L., et al. 2013. PLoS Pathog. 9, e1003375.
          Ke, H., et al. 2011. Eukaryot. Cell. 10, 1053.
          Ganesan, S.M., et al. 2011. Mol. Biochem. Parasitol. 177, 29.
          Booker, M.L., et al. 2010. J. Biol. Chem. 285, 33054.
          Gujjar, R., et al. 2009. J. Med. Chem. 52, 1864.
          Phillips, M.A., et al. 2008. J. Med. Chem. 51, 3649.