TRPM8 antagonist 5
TRPM8 antagonist 5 is a TRPM8 antagonist. TRPM8 antagonist 5 exhibits anticancer activity against melanoma and prostate cancer. TRPM8 antagonist 5 can be used for research on melanoma and prostate cancer.
For research use only. We do not sell to patients.
- Formula: C26H24F2N2O2
- Molecular Weight:434.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TRPM8 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.69 μM
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Antagonism of menthol-induced TRPM8-mediated Ca2+ responses in HEK293 cells stably expressing rat TRPM8, preincubated for 5-10 min with compound 7 followed by stimulation with 300 μM menthol, measured by Ca2+ microfluorimetric assay using Fluo-4 AM.
Antagonism of menthol-induced TRPM8-mediated Ca2+ responses in HEK293 cells stably expressing rat TRPM8, preincubated for 5-10 min with compound 7 followed by stimulation with 300 μM menthol, measured by Ca2+ microfluorimetric assay using Fluo-4 AM.
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42566740 |
| Malme-3M | IC50 |
10.4 μM
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Antiproliferative activity against human Malme-3M melanoma cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human Malme-3M melanoma cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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42566740 |
| LNCaP | IC50 |
7.9 μM
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Antiproliferative activity against human LNCaP prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human LNCaP prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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42566740 |
| PC-3 | IC50 |
17.2 μM
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Antiproliferative activity against human PC3 prostate cancer cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.
Antiproliferative activity against human PC3 prostate cancer cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.
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42566740 |
| PC-3 | IC50 |
15.0 μM
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Antiproliferative activity against human PC3 prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human PC3 prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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42566740 |
| PNT2 | IC50 |
28.1 μM
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Antiproliferative activity against non-transformed human PNT-2 prostate cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against non-transformed human PNT-2 prostate cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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42566740 |
| NIH3T3 | IC50 |
32 μM
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Antiproliferative activity against mouse NIH3T3 fibroblasts assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.
Antiproliferative activity against mouse NIH3T3 fibroblasts assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.
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42566740 |
| NIH3T3 | IC50 |
29.7 μM
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Antiproliferative activity against mouse NIH3T3 fibroblasts assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against mouse NIH3T3 fibroblasts assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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42566740 |
| HEK293 | IC50 |
0.87 μM
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Antagonism of menthol-induced human TRPM8 calcium currents in HEK-293 cells stably transfected with human TRPM8, measured by whole-cell voltage clamp patch-clamp assay (QPatch 48X) with voltage ramps every 4 s.
Antagonism of menthol-induced human TRPM8 calcium currents in HEK-293 cells stably transfected with human TRPM8, measured by whole-cell voltage clamp patch-clamp assay (QPatch 48X) with voltage ramps every 4 s.
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42566740 |
In Vitro
TRPM8 antagonist 5 (Compound 7) (0.1-40 μM; 24-72 h) exhibits time-dependent antiproliferative activity against MEL-CAL, Malme-3M, LNCaP, and PC3 cancer cell lines with IC50 values between 7.9 and 26.3 μM, while showing reduced effects on non-transformed PNT-2 and NIH3T3 cells[1].
TRPM8 antagonist 5 (20 μM; 21 days) significantly impairs spheroid growth and viability in the MEL-CAL 3D model at 20 μM[1].
TRPM8 antagonist 5 acts as a submicromolar antagonist of human TRPM8 in HEK-293 cells with an IC50 of 0.87 μM[1].
TRPM8 antagonist 5 (0.01-100 μM) does not produce detectable modulation of TRPV1 or TRPA1[1].
TRPM8 antagonist 5 (20-60 min) demonstrates moderate metabolic stability in liver microsomes with a t1/2 of 19.4 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MEL-CAL, Malme-3M, LNCaP, PC3, PNT-2, NIH3T3
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Concentration:0.1-40 μM
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Incubation Time:24 h; 72 h
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Result:Reduced MEL-CAL viability with IC50 values of 26.3 μM at 24 h and 15.0 μM at 72 h.
Reduced Malme-3M viability with an IC50 of 10.4 μM at 72 h.
Reduced LNCaP viability with an IC50 of 7.9 μM at 72 h.
Reduced PC3 viability with IC50 values of 17.2 μM at 24 h and 15.0 μM at 72 h.
Reduced PNT-2 viability with an IC50 of 28.1 μM at 72 h.
Reduced NIH3T3 viability with IC50 values of 32 μM at 24 h and 29.7 μM at 72 h.
Chemical Information
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Molecular Weight 434.48
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Formula C26H24F2N2O2
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SMILES
O=C(OC)[C@H](CC1=CNC2=C1C=CC=C2)N(CC3=CC=CC=C3)CC4=CC=C(F)C=C4F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRPM8 antagonist 5 Related Classifications
HY-189375 Related Classifications
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