| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C15H18OS2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
TRPV2-selective blocker 1 is a selective blocker of TRPV2 that reduces calcium influx and ionic currents through the channel. It shows an IC50 of 6.3 μM against rat TRPV2, with no activity at TRPV1, TRPV3 or TRPV4. The compound attenuates macrophage phagocytosis, LPS-induced macrophage migration and calcium microdomains generated by peripheral TRPV2, and is non-cytotoxic, making it suitable for investigating TRPV2 function in immune processes[1]. It is supplied as a white to off-white solid (C15H18OS2, MW 278.43) at 99.84% purity.
Physical & Chemical Properties
| CAS Number | 2242724-49-6 |
|---|---|
| Molecular Formula | C15H18OS2 |
| Molecular Weight | 278.43 g/mol |
| Purity | 99.84% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CC(CC(C)/C(C1=CC=CC=C1)=C2SCCS\2)=O |
| Target | TRPV2 |
| Signaling Pathway | Membrane Transporter/Ion Channel; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 100 mg/mL (359.16 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | -20°C, protect from light, stored under nitrogen. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
|
TRPV2 6.3 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (359.16 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light, stored under nitrogen; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 0.83 mg/mL (2.98 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.83 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (8.3 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 0.83 mg/mL (2.98 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.83 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (8.3 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 0.83 mg/mL (2.98 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.83 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (8.3 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In HEK_TRPV2 cells, TRPV2-selective blocker 1 (0.1-100 μM; 30 min, 60-second) potently and selectively blocks rat TRPV2-mediated Ca2+ influx, with an IC50 of 6.3 μM, while showing no activity on TRPV1, TRPV3, or TRPV4 channels at up to 50 μM[1]. TRPV2-selective blocker 1 (20 μM; 30 min) fully blocks TRPV2-mediated [Ca2+]i increases in HEK_TRPV2 cells activated by high-dose 2-APB or by a low-dose combination of 2-APB and Probenecid[1]. In HEK_TRPV2 cells, TRPV2-selective blocker 1 (0.1-20 μM) inhibits rat TRPV2 ionic currents, with an IC50 of 0.8 μM, and lowers single-channel open probability in a membrane-delimited manner[1]. In primary mouse BMDM activated by 300 μM 2-APB, TRPV2-selective blocker 1 (20 μM; 30 min) strongly lowers TRPV2-mediated [Ca2+]i increases[1]. TRPV2-selective blocker 1 (20-50 μM; 1 h, 24 h) reduces phagocytosis of zymosan and S. aureus bioparticles in primary mouse BMDM, and shows no cytotoxicity at concentrations up to 50 μM after 24 h incubation[1]. TRPV2-selective blocker 1 (20 μM; 1-2 h, 14 h) reduces LPS-induced migration of primary mouse BMDM and blocks the increased migration produced by TRPV2 activation with a 2-APB/probenecid combination[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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TRPV2 Regulates Function of Human Neutrophil Granulocytes. FASEB J 2025 Sep 30;39(18):e71052. PMID: 40948391
Lysophosphatidylcholine sensitizes TRPV2 by indirect mechanisms. Pflugers Arch 2025 Dec 12;478(1):8. PMID: 41381750
