500523 | ASIC Channel Modulator II, GMQ - Calbiochem

500523
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₀H₁₁N₅

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00523.0001
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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
          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

          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.