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373501 Herg Activator, NS1643 - CAS 448895-37-2 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Human ether-a-go-go related gene (hERG) K+ channel activator, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea, NS 1643, KV11.1 Channel Activator

373501
  
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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      448895-37-2C₁₅H₁₀F₆N₂O₃
      Description
      Overview

      This product has been discontinued.



      A diphenolurea compound that selectively activates human ether-a-go-go-related gene (hERG) K+-channel (EC50 = 10.5 µM). Shown to significantly increase both steady-state and peak tail currents of hERG channels, but exhibits only a trivial effect on Kv4.3 and Kv1.5 channels. Causes a significant reduction in action potential duration (APD90 ) in patch clamp assays in Xenopus oocytes, HEK293 cells, and guinea pig cardiamyocyes that can be reversed by the addition of E-4031 (Cat. No. 324470), a specific blocker of hERG channels. Also shown to activate IKr channel in cardiomyocytes and increase post-repolarization refractory time thereby alleviating hyper-excitability and producing antiarrhythmic effects. It can also restore IKr reduced by down-regulation of IKr expression.
      Catalogue Number373501
      Brand Family Calbiochem®
      SynonymsHuman ether-a-go-go related gene (hERG) K+ channel activator, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea, NS 1643, KV11.1 Channel Activator
      References
      ReferencesHansen, R., et al. 2006. Mol. Pharm. 69, 266.
      Schuster, A., et al. 2011. Mol. Pharm. 80, 930.
      Product Information
      CAS number448895-37-2
      FormOff-white powder
      Hill FormulaC₁₅H₁₀F₆N₂O₃
      Chemical formulaC₁₅H₁₀F₆N₂O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      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 +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freee (-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
      Global Trade Item Number
      Catalogue Number GTIN
      373501 0

      Documentation

      References

      Reference overview
      Hansen, R., et al. 2006. Mol. Pharm. 69, 266.
      Schuster, A., et al. 2011. Mol. Pharm. 80, 930.
      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.

      Revision13-July-2012 JSW
      SynonymsHuman ether-a-go-go related gene (hERG) K+ channel activator, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea, NS 1643, KV11.1 Channel Activator
      DescriptionA diphenolurea compound that selectively activates human ether-a-go-go-related gene (hERG) K+-channel (EC50 = 10.5 µM). Shown to significantly increase both steady-state and peak tail currents of hERG channels, but exhibits only a trivial effect on Kv4.3 and Kv1.5 channels. Causes a significant reduction in action potential duration (APD90 ) in patch clamp assays in Xenopus oocytes, HEK293 cells, and guinea pig cardiamyocyes that can be reversed by the addition of E-4031 (Cat. No. 324470), a specific blocker of hERG channels. Also shown to activate IKr channel in cardiomyocytes and increase post-repolarization refractory time thereby alleviating hyper-excitability and producing antiarrhythmic effects. It can also restore IKr reduced by down-regulation of IKr expression.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number448895-37-2
      Chemical formulaC₁₅H₁₀F₆N₂O₃
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml; clear, nearly colorless solution)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freee (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesHansen, R., et al. 2006. Mol. Pharm. 69, 266.
      Schuster, A., et al. 2011. Mol. Pharm. 80, 930.