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500523 ASIC Channel Modulator II, GMQ - Calbiochem

500523
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₀H₁₁N₅

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      Glass bottle 25 mg
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      Description
      OverviewA positively charged guanidium-containing quinazoline that modulates ASIC function by blocking acid-induced maximal peak current as well as by altering ASICs pH dependence for activation and inactivation, enabling a partial, but sustained ASIC3 activation around neutral pH (4.4% of pH 5-induced peak current with 1 mM GMQ at pH 7.4), which is inhibitable by Amiloride (Cat. No. 129876). Intraplantar paw injection (10 µL 100 µM) is reported to elicit a pain response in asic3+/+, but not asic3-/-, mice in vivo. GMQ targeting area appears to overlap with Amiloride binding site in the pore region, but is distinct from ASIC calcium binding site.
      Catalogue Number500523
      Brand Family Calbiochem®
      Synonyms2-guanidine-4-methylquinazoline, Acid-Sensing Ion Channel Modulator II
      References
      ReferencesAlijevic, O., and Kellenberger, S. 2012. J Biol Chem. 287, 36059.
      Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
      Yu, Y., et al. 2010. Neuron. 68, 61.
      Product Information
      FormWhite solid
      Hill FormulaC₁₀H₁₁N₅
      Chemical formulaC₁₀H₁₁N₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetASIC3
      Purity≥99% 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 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

      ASIC Channel Modulator II, GMQ - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Alijevic, O., and Kellenberger, S. 2012. J Biol Chem. 287, 36059.
      Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
      Yu, Y., et al. 2010. Neuron. 68, 61.
      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-June-2013 JSW
      Synonyms2-guanidine-4-methylquinazoline, Acid-Sensing Ion Channel Modulator II
      DescriptionA positively charged guanidium-containing quinazoline that modulates ASIC (acid-sensing ion channel) function by blocking acid-induced maximal peak current (IC50 = 3.24 mM and 1.52 mM, respectively, against pH 4.5-induced human ASIC1a and rat ASIC1b peak current; IC50 = 6.74 mM against pH 5.0-induced rat ASIC3 peak current; by whole-cell patch clamp) as well as by altering ASICs pH dependence for activation (pH50 with/without 1 mM GMQ = 6.30/6.49, 6.14/6.27, and 6.94/6.71, for hASIC1a, rASIC1b, and rASIC3, respectively) and inactivation (pHIn50 with/without 1 mM GMQ = 6.92/7.11, 6.48/6.66, and 6.59/7.07, for hASIC1a, rASIC1b, and rASIC3, respectively; pHIn50 with/without 5 mM GMQ = 5.42/5/63 for rASIC2b) in a dose-dependent manner (EC50 of hASIC1a ΔpH50 = 1.97 mM). The combined pH sensitivity shift, activation reduction, and inactivation blockage enables a partial, but sustained ASIC3 activation around neutral pH by GMQ (4.4% of pH 5-induced peak current by 1 mM GMQ at pH 7.4), which is inhibitable by Amiloride (Cat. No. 129876) in a dose-dependent manner (IC50 against 0.5 mM GMQ activated channel activity at pH 7.0 by Amiloride = 98.5 µM). Likewise, GMQ intraplantar paw injection (10 µL 100 µM) is reported to elicit a pain response in asic3+/+, but not asic3-/-, mice (538% vs 14%, respectively, above background paw licking response) in vivo. GMQ targeting area appears to overlap with Amiloride binding site in the pore region, but is distinct from ASIC calcium binding site.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₀H₁₁N₅
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (16.6 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
      ReferencesAlijevic, O., and Kellenberger, S. 2012. J Biol Chem. 287, 36059.
      Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
      Yu, Y., et al. 2010. Neuron. 68, 61.