| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GMQ targets acid-sensing ion channel 3 (ASIC3) as a selective activator. It activates ASIC3 channels under neutral pH (pH 7.4) and blocks acid-induced maximal peak current. It alters the pH dependence of ASIC1a and ASIC1b but does not affect the activation curve of ASIC2a. At high concentrations, GMQ inhibits ASIC scaffolds.
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| ln Vitro |
At pH 7.4, GMQ (1 mM) causes a persistent inward current in CHO cells [1]. With IC50 values of 3.24, 1.52, and 6.74 mmol for ASIC1a, ASIC1b, and ASIC3, respectively, GMQ inhibits ASIC scaffolds at high concentrations [1].
In vitro, GMQ evokes rapid inward currents with little desensitization in CHO cells expressing ASIC3 (EC₅₀ = 67 µM at neutral pH). At pH 7.4, GMQ (1 mM) causes a persistent inward current in CHO cells. With IC₅₀ values of 3.24, 1.52, and 6.74 mM for ASIC1a, ASIC1b, and ASIC3 respectively, GMQ inhibits ASIC scaffolds at high concentrations. It also acts as a competitive GABAA receptor antagonist. |
| ln Vivo |
In vivo, GMQ is used as a pharmacological tool to study ASIC3 function in pain signaling, neuroinflammation, and mechanosensation. It modulates sensory neuron excitability and pain perception through ASIC3 activation. The compound serves as a critical tool for dissecting ASIC3-specific functions in various physiological and pathological processes.
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| Enzyme Assay |
Electrophysiological patch-clamp recordings: CHO cells expressing ASIC3 are cultured and subjected to whole-cell patch-clamp. GMQ hydrochloride is applied at various concentrations (typically 1 µM to 10 mM) in extracellular solution at pH 7.4. Inward currents are recorded and EC₅₀ values are calculated from dose-response curves. For acid-induced current blockade, cells are exposed to acidic pH in the presence of GMQ.
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| Cell Assay |
CHO cells stably or transiently expressing ASIC channels (ASIC1a, ASIC1b, ASIC2a, ASIC3) are cultured in F-12 medium with 10% FBS at 37°C with 5% CO₂. For electrophysiology, cells are plated on coverslips and whole-cell patch-clamp recordings are performed. For calcium imaging, cells are loaded with calcium-sensitive dyes and fluorescence changes upon GMQ application are measured. IC₅₀ and EC₅₀ values are calculated.
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| Animal Protocol |
In vivo studies are conducted in rodent models of pain and inflammation. GMQ hydrochloride is administered via intrathecal, intraplantar, or systemic routes. Pain behavioral tests (e.g., von Frey test for mechanical allodynia, Hargreaves test for thermal hyperalgesia) are performed. ASIC3-specific effects are evaluated by comparing responses in wild-type versus ASIC3 knockout animals.
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| ADME/Pharmacokinetics |
GMQ hydrochloride has molecular formula C₁₀H₁₂ClN₅ and molecular weight 237.69. It is soluble in water (~3.33 mg/mL, ~14.01 mM) and has LogP 2.918. The compound is a selective ASIC3 channel activator at pH 7.4 and a competitive GABAA receptor antagonist. Purity is ≥98%.
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| References | |
| Additional Infomation |
GMQ hydrochloride is a potent and selective acid-sensing ion channel modulator. It activates ASIC3 channels under neutral pH and blocks acid-induced maximal peak current. The compound serves as a critical pharmacological tool for dissecting ASIC3-specific functions in pain signaling, neuroinflammation, and mechanosensation. It also acts as a competitive GABAA receptor antagonist.
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| Molecular Formula |
C10H12CLN5
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|---|---|
| Molecular Weight |
237.69
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| Exact Mass |
237.078
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| CAS # |
5361-15-9
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| Related CAS # |
5361-15-9;
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| PubChem CID |
12253739
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| Appearance |
White to off-white solid powder
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| LogP |
2.918
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
248
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VNPZWQRWOHFAPD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11N5.ClH/c1-6-7-4-2-3-5-8(7)14-10(13-6)15-9(11)12;/h2-5H,1H3,(H4,11,12,13,14,15);1H
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| Chemical Name |
1-(4-methylquinazolin-2-yl)guanidine hydrochloride InChi Key
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| Synonyms |
GMQ hydrochloride GMQ HCl NSC-403387 hydrochloride NSC 403387 hydrochloride NSC403387 hydrochloride NSC-403387 HCl NSC 403387 HCl NSC403387 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~3.33 mg/mL (~14.01 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2072 mL | 21.0358 mL | 42.0716 mL | |
| 5 mM | 0.8414 mL | 4.2072 mL | 8.4143 mL | |
| 10 mM | 0.4207 mL | 2.1036 mL | 4.2072 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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