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Art. -Nr.: HY-189375

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₆H₂₄F₂N₂O₂
Molecular Weight:434.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

TRPM8 antagonist 5 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

TRPM8

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	0.69 μM	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.	42566740
Malme-3M	IC50	10.4 μM	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.	42566740
LNCaP	IC50	7.9 μM	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.	42566740
PC-3	IC50	17.2 μM	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.	42566740
PC-3	IC50	15.0 μM	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.	42566740
PNT2	IC50	28.1 μM	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.	42566740
NIH3T3	IC50	32 μM	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.	42566740
NIH3T3	IC50	29.7 μM	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.	42566740
HEK293	IC50	0.87 μM	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.	42566740

In Vitro

Anti-cancerOthers

Anti-cancer

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].

Others

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 t_1/2 of 19.4 min^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

MEL-CAL, Malme-3M, LNCaP, PC3, PNT-2, NIH3T3
Concentration:

0.1-40 μM
Incubation Time:

24 h; 72 h
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

Molecular Weight 434.48
Formel C₂₆H₂₄F₂N₂O₂
SMILES

O=C(OC)[C@H](CC1=CNC2=C1C=CC=C2)N(CC3=CC=CC=C3)CC4=CC=C(F)C=C4F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Ciaglia T, et al. New TRPM8 Amino Acid-Based Antagonists Induce Antiproliferative Effect on 2D and 3D Melanoma and Prostate Cancer Models. Journal of medicinal chemistry. 2026 Aug 27;69(16):19644-19670.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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