| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
TRPC3 and TRPC6 ion channels (transient receptor potential canonical channels). GSK1702934A is a potent and selective TRPC3/6 activator.
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| ln Vitro |
In HEK293 cells transduced with recombinant human TRPC3/6, GSK1702934A may produce TRPC3/6 currents, with EC50 values of 0.08 mM and 0.44 mM, respectively [1]. In TRPC3-overexpressing muscle cells, GSK1702934A causes a brief, non-conductive conductance, and in longer-term TRPC3-overexpressing muscle cells, GSK1702934A dramatically increases NCX current [2].
GSK1702934A activates current in HEK293 cells transduced with recombinant human TRPC3 or TRPC6 with EC50s of approximately 80 nM for TRPC3 and 440 nM for TRPC6. It induces TRPC3- and TRPC6-dependent currents in whole-cell patch-clamp assays. GSK1702934A exhibits no activity at TRPV4, TRPA1, M1, M4, CaV1.2, hERG, NaV1.5, or CXCR5 receptors at concentrations <10 μM. In rat cardiomyocyte-like H9C2 cells, GSK1702934A (1 μM) activated TRPC6-like current and was completely blocked by GSK-417651A. It transiently increased the perfusion pressure of isolated rat heart retrogradely perfused via aortic cannulation at 1 μM. |
| ln Vivo |
The intravenous infusion of GSK1702934A (0.3-3 mg/kg) elevates the blood glucose level of awake Sprague Dawley by 15 to 35 mmHg [3].
In vivo, GSK1702934A modulates cardiac contractility and arrhythmogenesis through TRPC3 activation. Intravenous administration (0.3-3 mg/kg) produces transient blood pressure elevation (15-35 mmHg) in conscious Sprague Dawley rats. The compound has proarrhythmic and positive inotropic effects. GSK1702934A may be used for research in diabetes. Specific animal model data and detailed dosing regimens are available in the primary literature. |
| Enzyme Assay |
TRPC3/6 channel activation is assessed using whole-cell patch-clamp electrophysiology in HEK293 cells expressing recombinant human TRPC3 or TRPC6. Cells are held at a holding potential of -60 mV and currents are evoked by voltage ramps or step protocols. GSK1702934A is applied at various concentrations (typically 0.001-100 μM) and current amplitudes are measured. EC50 values are calculated from dose-response curves using nonlinear regression analysis. Calcium influx is measured using fluorescent calcium indicators (e.g., Fluo-4 AM) in plate-reader-based or imaging assays. Selectivity is evaluated by testing against other ion channels (TRPV4, TRPA1, CaV1.2, hERG, NaV1.5) and receptors (M1, M4, CXCR5) at concentrations <10 μM.
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| Cell Assay |
Cellular activity is evaluated in HEK293 cells expressing recombinant human TRPC3 or TRPC6, or in rat cardiomyocyte-like H9C2 cells. Cells are treated with GSK1702934A at various concentrations (typically 0.001-100 μM) and channel activity is measured by whole-cell patch-clamp electrophysiology or calcium imaging. In H9C2 cells, TRPC6-like current activation is assessed and confirmed by blockade with GSK-417651A. Cardiac contractility may be assessed in isolated cardiomyocyte preparations by measuring sarcomere shortening or calcium transients. Isolated rat heart perfusion assays are used to measure perfusion pressure changes.
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| Animal Protocol |
In vivo efficacy is studied in animal models of cardiac arrhythmia, heart failure, or hypertension. GSK1702934A is administered intravenously at doses of 0.3-3 mg/kg. Blood pressure is measured by telemetry or tail-cuff plethysmography. Cardiac contractility is assessed by echocardiography or by measuring left ventricular pressure. Arrhythmia susceptibility is assessed by programmed electrical stimulation or by monitoring electrocardiograms (ECG). Pharmacodynamic markers include TRPC3/6 channel activation and downstream signaling in cardiac tissue. Specific protocols are detailed in the primary literature.
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| ADME/Pharmacokinetics |
GSK1702934A has a molecular formula of C22H25N3O2S and a molecular weight of 395.52 g/mol. CAS Number: 924377-85-5. Purity: typically ≥98% by HPLC. The compound is a selective TRPC3/6 activator. Solubility: DMSO 100 mg/mL (252.83 mM; with sonication; hygroscopic DMSO significantly affects solubility, use freshly opened DMSO). Storage: store at -20°C for long-term stability, protected from light and moisture. Detailed pharmacokinetic parameters including half-life, oral bioavailability, volume of distribution, and plasma protein binding are available from the primary literature.
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| Toxicity/Toxicokinetics |
Safety data for GSK1702934A indicate it is a research compound for laboratory use only. As a TRPC3/6 activator with proarrhythmic and positive inotropic effects, it should be handled with appropriate safety precautions. The compound may cause cardiovascular effects including blood pressure elevation and arrhythmias. Standard laboratory safety practices should be followed, including the use of personal protective equipment and adequate ventilation. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Consult the material safety data sheet (MSDS) for detailed safety information.
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| References |
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| Additional Infomation |
GSK1702934A is a research tool compound for studying TRPC3/6 channel biology and cardiovascular physiology. It is not approved for clinical use. The compound has been investigated for research in cardiac contractility, arrhythmogenesis, and diabetes. GSK1702934A directly activates TRPC channels, bypassing phospholipase-C signaling. Reference: Biophys J (2013) 104: 454a. The compound's selectivity for TRPC3/6 over other channels and receptors at concentrations <10 μM makes it a valuable tool for dissecting TRPC3/6-specific functions in cardiovascular physiology and disease. GSK1702934A is also known as GSK 1702934A.
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| Molecular Formula |
C22H25N3O2S
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|---|---|
| Molecular Weight |
396
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| Exact Mass |
395.166
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| CAS # |
924377-85-5
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| PubChem CID |
16376051
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
607
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C=2C([H])=C1C(N1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N1C(N([H])C2=C([H])C([H])=C([H])C([H])=C12)=O)=O
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| InChi Key |
AXWRAIIIBRLXBP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25N3O2S/c26-21(20-14-15-6-2-1-3-9-19(15)28-20)24-12-10-16(11-13-24)25-18-8-5-4-7-17(18)23-22(25)27/h4-5,7-8,14,16H,1-3,6,9-13H2,(H,23,27)
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| Chemical Name |
3-[1-(5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-2-carbonyl)piperidin-4-yl]-1H-benzimidazol-2-one
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| Synonyms |
GSK-1702934A; GSK 1702934A; GSK1702934A
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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 |
| 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) |
DMSO : ~100 mg/mL (~252.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5253 mL | 12.6263 mL | 25.2525 mL | |
| 5 mM | 0.5051 mL | 2.5253 mL | 5.0505 mL | |
| 10 mM | 0.2525 mL | 1.2626 mL | 2.5253 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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