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530923 Kir6.2/SUR1 Channel Activator, VU0071063 - CAS 333415-38-6 - Calbiochem

A fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC₅₀ = 7 µM).

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Synonyme: 7-(4-(tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione

Primary Target: SUR1-containing channels
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530923
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
333415-38-6C₁₈H₂₂N₄O₂

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      Description
      OverviewA xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC50 > 100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µM) and Kir2.3 (IC50 = 91 µM) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic β-cells.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530923
      Brand Family Calbiochem®
      Synonyms7-(4-(tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione
      References
      ReferencesRaphemot, R., et al. 2014. Mol. Pharmacol. 85, 858.
      Product Information
      CAS number333415-38-6
      FormWhite powder
      Hill FormulaC₁₈H₂₂N₄O₂
      Chemical formulaC₁₈H₂₂N₄O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSUR1-containing channels
      Primary Target IC<sub>50</sub>EC₅₀ = 7 µM for Kir6.2/SUR1 channel activation
      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 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
      Global Trade Item Number
      Bestellnummer GTIN
      5309230001 04055977243024

      Documentation

      Kir6.2/SUR1 Channel Activator, VU0071063 - CAS 333415-38-6 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Raphemot, R., et al. 2014. Mol. Pharmacol. 85, 858.
      Datenblatt

      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-June-2014 JSW
      Synonyms7-(4-(tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione
      DescriptionA xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC50 > 100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µM) and Kir2.3 (IC50 = 91 µM) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic β-cells.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number333415-38-6
      Chemical formulaC₁₈H₂₂N₄O₂
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesRaphemot, R., et al. 2014. Mol. Pharmacol. 85, 858.