505893 | Mycobacterium Bactericide, TCA1 - Calbiochem

505893
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₃N₃O₄S₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05893.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable benzothiazolylthiophene that exhibits bactericidal activity against mycobacteria, including M. smegmatis, M. bovis GCG, and M. tuberculosis (MIC50 = 30, 40, and 10 ng/mL, respectively, in biofilm medium; MIC50 = 4.5, 3, 0.19 µg/mL, respectively, in 7H9 medium), but not E. coli, Staphylococcus aureus, or Pseudomonas aeruginosa, by simultaneously targeting DprE1 FAD-binding domain of DprE1/DprE2 required for Mycobacterium cell wall arabinan biosynthesis and the Mtb MoeW protein involved in the biosynthesis of MoCo, molybdenum cofactor indispensable for nitrate assimilation via MoCo-dependent enzymes. Either alone or used in combination, TCA1 is shown to greatly complement INH (Isoniazid) and RIF (Rifampicin) against both wt and drug-resistant Mtb cultures in vitro (1-7.5 µg/mL) and in treating acute and chronic Mtb H37Rv infections in mice in vivo (10-100 mg/kg p.o.) with no apparent host toxicity.
          Catalogue Number505893
          Brand Family Calbiochem®
          SynonymsEthyl-(2-(benzo[d]thiazole-2-carboxamido)thiophene-3-carbonyl)carbamate, Ethyl-((2-((1,3-benzothiazol-2-ylcarbonyl)amino)-3-thienyl)carbonyl)carbamate, Mtb Inhibitor, Mycobacteria DprE1 Inhibitor, Mycobacteria MoeW Inhibitor
          References
          ReferencesWang, F., et al. 2013. Proc. Natl. Acad. Sci. USA 110, E2510.
          Product Information
          FormYellow solid
          Hill FormulaC₁₆H₁₃N₃O₄S₂
          Chemical formulaC₁₆H₁₃N₃O₄S₂
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetDprE1
          Secondary targetMoeW
          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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Wang, F., et al. 2013. Proc. Natl. Acad. Sci. USA 110, E2510.
          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-January-2014 JSW
          SynonymsEthyl-(2-(benzo[d]thiazole-2-carboxamido)thiophene-3-carbonyl)carbamate, Ethyl-((2-((1,3-benzothiazol-2-ylcarbonyl)amino)-3-thienyl)carbonyl)carbamate, Mtb Inhibitor, Mycobacteria DprE1 Inhibitor, Mycobacteria MoeW Inhibitor
          DescriptionA cell-permeable benzothiazolylthiophene that exhibits bactericidal activity against mycobacteria, including M. smegmatis, M. bovis GCG, and M. tuberculosis (MIC50 = 30, 40, and 10 ng/mL, respectively, in biofilm medium; MIC50 = 4.5, 3, 0.19 µg/mL, respectively, in 7H9 medium), but not E. coli, Staphylococcus aureus, or Pseudomonas aeruginosa, by simultaneously targeting DprE1 FAD-binding domain of the decaprenylphosphoryl-β-D-ribofuranose 2'-epimerase DprE1/DprE2 required for Mycobacterium cell wall arabinan biosynthesis and the Mtb MoeW protein (M. smegmatis MoeB homolog) involved in the biosynthesis of MoCo, molybdenum cofactor indispensable for nitrate assimilation via MoCo-dependent enzymes. Either alone or used in combination, TCA1 is shown to greatly complement INH (Isoniazid) and RIF (Rifampicin) against both wt and drug-resistant Mtb cultures in vitro (3.75-7.5 µg/mL, 1 µg/mL, and 2 µg/mL, respectively), including the XDR (extensively drug resistant) TF275 (strain# mc28013) that is resistant to 10 TB drugs, and in treating acute and chronic Mtb H37Rv infections in mice in vivo (40-100 mg/kg, 25 mg/kg, and 10 mg/kg, respectively; p.o.). TCA1 exhibits no host toxicity (≥25 µM in cultures and 100 mg/kg in mice) and no activity toward hERG or four CTP enzymes.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₁₃N₃O₄S₂
          Structure formulaStructure formula
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesWang, F., et al. 2013. Proc. Natl. Acad. Sci. USA 110, E2510.