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Description: Selective TRPV2 antagonist
Chemical Name: N-(2-Furanylmethyl)-3-[[4-(methylpropylamino)-6-(trifluoromethyl)-2-pyrimidinyl]thio]propanamide
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for SET 2

SET 2 is a TRPV2 (transient receptor potential vanilloid type 2) antagonist (IC50 = 0.46 μM). Selective for TRPV2 over TRPV1, TRPV3 and TRPV4 expressed in HEK293 cells. Inhibits lyosphosphatidic acid (LPA)-induced prostate cancer cell migration in vitro.

Compound Libraries for SET 2

SET 2 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SET 2

M. Wt 402.44
Formula C17H21F3N4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2313525-20-9
Smiles CCCN(C1=NC(SCCC(NCC2=CC=CO2)=O)=NC(C(F)(F)F)=C1)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SET 2

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 40.24 100
ethanol 20.12 50

Preparing Stock Solutions for SET 2

The following data is based on the product molecular weight 402.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.48 mL 12.42 mL 24.85 mL
5 mM 0.5 mL 2.48 mL 4.97 mL
10 mM 0.25 mL 1.24 mL 2.48 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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References for SET 2

References are publications that support the biological activity of the product.

Chai et al (2019) Structure-based discovery of a subtype-selective inhibitor targeting a transient receptor potential vanilloid channel. J.Med.Chem. 62 1373 PMID: 30620187

If you know of a relevant reference for SET 2, please let us know.

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Keywords: SET 2, SET 2 supplier, SET2, TRPV2, antagonist, antagonists, antagonism, transient, receptor, potential, vanilloid, metastasis, cell, migration, subtype, selective, TRPV, 6990, Tocris Bioscience

1 Citation for SET 2

Citations are publications that use Tocris products. Selected citations for SET 2 include:

Yaniv et al (2023) The Effect of Cannabis Plant Extracts on Head and Neck Squamous Cell Carcinoma and the Quest for Cannabis-Based Personalized Therapy. Cancers (Basel) 15 PMID: 36672446

Do you know of a great paper that uses SET 2 from Tocris? Please let us know.

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