Product Information
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.

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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Neurochemicals > Channel Openers