An ASIC Channel Modulator and an ASIC3 Channel Opener
Cat #: G-165
Sizes: 5 mg, 10 mg, 50 mg, 250 mg
Source: Synthetic
MW: 237.1 Da.
Target: ASIC1a, ASIC2, ASIC3
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2-guanidine-4-methylquinazoline (GMQ) is a small synthetic nonproton molecule that activates ASIC channels (acid-sensing ion channels). ASICs are proton-gated ion channels which are activated by a decrease in extracellular pH. GMQ is an activator of ASIC3 channels under physiological pH conditions; it induces a window current at pH 7.4 only in ASIC3. Evidence shows that GMQ alters the pH dependence of all ASIC subtypes studied1,2.
GMQ contains basic groups that seem to form tight contacts with the carboxyl groups of acidic residues through hydrogen bonds (H-bonds) and electrostatic interactions that lead to the activation of ASIC3. In addition GMQ contains a guanidinium group and a heterocyclic ring.
Additional studies showed that GMQ activates sensory neurons and causes pain-related behaviors in an ASIC3-dependent manner3.
Alomone Labs is pleased to offer 2-GMQ hydrochloride (#G-165).
2-GMQ hydrochlorideReferences
Alijevic, O. and Kellenberger, S. (2012) J. Biol. Chem.287, 36059.
Li, W.G. et al. (2010) Mol. Pain 88, 1186.
Li, W.G. et al. (2011) J. Biol. Chem.286, 42635.
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Our bioassay
Alomone Labs 2-GMQ hydrochloride modulates ASIC3 channels expressed in Xenopus oocytes. Time course of ASIC3 currents elicited by stimulation with pH 6 every 50 sec, while membrane potential was held at -60 mV. 0.5 mM 2-GMQ hydrochloride (#G-165), applied for 3.5 min, as indicated causes reversible complex effect combining peak amplitude depression with diminished inactivation, as seen with superimposed traces in B.
Purity>99%.
Effective concentration1-5 mM
Chemical name2-(4-methylquinazolin-2-yl)guanidine hydrochloride.
Molecular formulaC10H12ClN5.
CAS number5361-15-9.
Activity2-GMQ is an ASIC modulator, ASIC3 opener and also induces an acidic shift of the pH dependence of inactivation of ASIC1a, -1b, -2a, and -31.
Storage before reconstitutionLyophilized powder can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitutionUp to four weeks at 4°C or three months at -20°C.