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

373501
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₀F₆N₂O₃ 448895-37-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      373501-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA 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
          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

          Documentation

          Certificates of Analysis

          TitleLot Number
          373501

          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 +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesHansen, R., et al. 2006. Mol. Pharm. 69, 266.
          Schuster, A., et al. 2011. Mol. Pharm. 80, 930.