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Chemical compound
SET2 JSmol)
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)
Key:LZHSWRWIMQRTOP-UHFFFAOYSA-N
SET2 is a drug which acts as a selective
antagonist for the
TRPV2 receptor. It is moderately potent with an IC
50 of 460nM, but is highly selective for TRPV2 over the other subtypes of
TRPV , and is the first such compound to be developed. A role has been suggested for TRPV2 in tumor
metastasis , making this a target of interest in the treatment of cancer.
[1] See also References
TRPA
TRPC
TRPM
TRPML
TRPP
TRPV
Activators
2-APB 5',6'-EET 9-HODE 9-oxoODE 12S-HETE 12S-HpETE 13-HODE 13-oxoODE 20-HETE )
Allicin (garlic )AM404 Anandamide Bisandrographolide (Andrographis paniculata )
Cannabidiol (cannabis )Cannabidivarin (cannabis )Capsaicin (chili pepper )Carvacrol (oregano , thyme , pepperwort , wild bergamot , others)DHEA Diacyl glycerol Dihydrocapsaicin (chili pepper )Estradiol Eugenol (basil , clove )Evodiamine (Euodia ruticarpa Gingerols (ginger )GSK1016790A Heat Hepoxilin A3
Hepoxilin B3
Homocapsaicin (chili pepper )Homodihydrocapsaicin (chili pepper )Incensole (incense )Lysophosphatidic acid Low pH (acidic conditions)
Menthol (mint )N-Arachidonoyl dopamine N-Oleoyldopamine N-Oleoylethanolamide Nonivamide (PAVA) (PAVA spray )Nordihydrocapsaicin (chili pepper )Paclitaxel (Pacific yew )Paracetamol (acetaminophen) Phenylacetylrinvanil Phorbol esters (e.g., 4α-PDD )Piperine (black pepper , long pepper )Polygodial (Dorrigo pepper )Probenecid Protons RhTx Rutamarin (Ruta graveolens Resiniferatoxin (RTX) (Euphorbia resinifera /pooissonii Shogaols (ginger , Sichuan and melegueta peppers )Tetrahydrocannabivarin (cannabis )Thymol (thyme , oregano )Tinyatoxin (Euphorbia resinifera /pooissonii Tramadol Vanillin (vanilla )Zucapsaicin Blockers
