| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
TRPV2 0.46 μM (IC50)
SET2 targets the transient receptor potential vanilloid 2 (TRPV2) channel as a selective antagonist with an IC50 of 0.46 μM. TRPV2 is a non-selective cation channel involved in calcium signaling, cell migration, and cancer progression. By blocking TRPV2, SET2 suppresses prostate cancer cell migration. The compound reduces lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases. The compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. The compound's mechanism involves inhibition of calcium influx through TRPV2 channels. |
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| ln Vitro |
TRPV2-expressing PC-3M cells' ability to migrate is eliminated by SET2 (20 μM; 24 hours) [1]. When TRPV2 and LPAR1 are transiently co-transfected in HEK293T cells, SET2 (20 μM; 24 hours) suppresses 2-APB-evoked currents [1]. LPA (0.1 μM; 3 minutes)-induced rise in cytoplasmic calcium and LPA-induced PC-3M cell migration are inhibited by SET2 (20 μM; 24 hours) [1].
In vitro studies demonstrate that SET2 is a selective TRPV2 antagonist with an IC50 of 0.46 μM. The compound blocks the TRP channel and suppresses prostate cancer cell migration. SET2 reduces lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases. The compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. It is a valuable research tool for studying TRPV2 function in cancer cell biology and calcium signaling pathways. The compound's IC50 of 0.46 μM indicates potent antagonistic activity against TRPV2. |
| ln Vivo |
In vivo studies of SET2 are limited in publicly available literature, as the compound is primarily characterized through in vitro assays. Given its role as a selective TRPV2 antagonist and its ability to suppress prostate cancer cell migration, the compound may have potential for in vivo investigations of cancer metastasis and TRPV2-related pathologies. TRPV2 is involved in cancer progression and cell migration, suggesting that SET2 could be useful in preclinical cancer models. However, specific in vivo efficacy data and animal model studies have not been extensively reported in the available sources. Further research is needed to establish its in vivo activity profile.
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| Enzyme Assay |
For TRPV2 channel binding and functional assays, cells expressing TRPV2 channels (e.g., HEK293 cells transfected with TRPV2) are cultured and loaded with calcium-sensitive fluorescent dyes. SET2 is dissolved in DMSO and diluted in assay buffer to varying concentrations. Cells are treated with the compound and TRPV2 activation is induced by lysophosphatidic acid (LPA) or other TRPV2 agonists. Calcium flux is measured using fluorescence plate readers. IC50 values are calculated from dose-response curves by measuring the reduction in agonist-induced calcium increases. For cell migration assays, prostate cancer cells are treated with SET2 and migration is assessed using Transwell or wound-healing assays. Assays are performed in replicate with vehicle controls.
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| Cell Assay |
Cell Migration Assay [1]
Cell Types: PC-3M prostate cancer cells Tested Concentrations: 0, 5 μM, 10 μM, and 20 μM Incubation Duration: 24 hr and 48 hr Experimental Results: Inhibited cell migration of PC-3M cells, without inhibiting cell viability at 48 hrs (hours). For in vitro cellular assays, prostate cancer cells or TRPV2-expressing cell lines are cultured in appropriate media under standard conditions (37°C, 5% CO2). SET2 is dissolved in DMSO and diluted in culture medium to desired concentrations (typically μM range). Cells are treated with compound for specified durations. TRPV2 channel activity is assessed by measuring intracellular calcium flux using fluorescent indicators upon LPA stimulation. Cell migration is assessed using Transwell chambers or wound-healing assays. Cell viability and proliferation can also be assessed using MTT or similar assays. Each concentration is tested in replicate wells with vehicle controls and positive controls. |
| Animal Protocol |
For in vivo animal studies of SET2, no specific protocols have been published in the available literature. For general in vivo administration of TRPV2 antagonists, compounds are typically formulated in suitable vehicles (e.g., DMSO/PEG300/saline or CMC-Na suspensions) and administered via oral gavage, intraperitoneal (i.p.) injection, or intravenous (i.v.) injection. Dosing regimens vary by study objective. For cancer models, tumor-bearing animals may be treated with compound and tumor growth and metastasis are monitored. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SET2 are characteristic of a small-molecule TRPV2 antagonist. The compound has a molecular weight of 402.43, formula C17H21F3N4O2S, and CAS number 2313525-20-9. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO and other organic solvents. The compound has an IC50 of 0.46 μM for TRPV2 inhibition. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported in publicly available sources. The compound is for research use only.
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| Toxicity/Toxicokinetics |
According to available safety information, SET2 is intended for research use only and not for human therapeutic applications. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. The compound is not for human use and no clinical toxicity data are available. Specific GHS hazard classifications have not been detailed in publicly available sources.
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| References | |
| Additional Infomation |
SET2 is a selective TRPV2 antagonist with an IC50 of 0.46 μM. It blocks the TRP channel and suppresses prostate cancer cell migration. SET2 reduces lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases. It effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. The compound is a valuable research tool for studying TRPV2 function in cancer cell biology and calcium signaling pathways. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C17H21F3N4O2S
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|---|---|
| Molecular Weight |
402.434452772141
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| Exact Mass |
402.133
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| CAS # |
2313525-20-9
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| PubChem CID |
155541857
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| Appearance |
White to off-white solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
27
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| Complexity |
470
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(C1=NC(SCCC(=O)NCC2OC=CC=2)=NC(C(F)(F)F)=C1)(C)CCC
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| InChi Key |
LZHSWRWIMQRTOP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21F3N4O2S/c1-3-7-24(2)14-10-13(17(18,19)20)22-16(23-14)27-9-6-15(25)21-11-12-5-4-8-26-12/h4-5,8,10H,3,6-7,9,11H2,1-2H3,(H,21,25)
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| Chemical Name |
N-(furan-2-ylmethyl)-3-[4-[methyl(propyl)amino]-6-(trifluoromethyl)pyrimidin-2-yl]sulfanylpropanamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (248.49 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 | 2.4849 mL | 12.4245 mL | 24.8490 mL | |
| 5 mM | 0.4970 mL | 2.4849 mL | 4.9698 mL | |
| 10 mM | 0.2485 mL | 1.2425 mL | 2.4849 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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