TRPM8 antagonist 4
TRPM8 antagonist 4 is a CB2R partial agonist (EC50=54.2 nM, Ki=3.2 μM) and TRPM8 antagonists (IC50=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β.
For research use only. We do not sell to patients.
- CAS No.: 3107363-68-5
- Formula: C20H27NO3
- Molecular Weight:329.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TRPM8 42.3 nM (IC50) |
CB2R 54.2 nM (EC50) |
CB2R 3.2 μM (Ki) |
IL-6 |
IL-1β |
TNF-α |
TRPM8 antagonist 4 (Compound 6b) exhibits neither antagonistic nor agonistic activity at the CB1R in the HTRF cAMP assay[1].
TRPM8 antagonist 4 (1 nM-1000 nM) inhibits hTRPM8 currents induced by 30.0 μM menthol in HEK293 cells, with IC50=42.3 nM[1].
TRPM8 antagonist 4 (1 μM-1 M) binds to CB2R by radioligand competition assay[1].
TRPM8 antagonist 4 (0.3 μM, 8h) reduces the mRNA expression of TNF-α, IL-6, and IL-1β in LPS-stimulated RAW264.7 macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS (HY-D1056)-stimulated (100 ng/mL, 8 h) RAW264.7 macrophages
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Concentration:0.3 μM
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Incubation Time:8h
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Result:Reduced the mRNA expression of TNF-α, IL-6, and IL-1β compared to LPS-induced model group.
Were comparable to those of CBG at the same concentration the inhibitory effects of on pro-inflammatory cytokine mRNA expression.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast |
|---|---|---|---|---|---|---|
| Mice | 25 mg/kg | p.o. | 3.6 h | 0.3 h | 39.0 ng/mL | 61.7 ng·h/mL |
TRPM8 antagonist 4 (Compound 6b) (2.5 mg/kg, i.p., once) shows anti-inflammatory effects in LPS (HY-D1056)-induced inflammation in C57BL/6J mice model[1].
TRPM8 antagonist 4 (5 mg/kg, i.p., once) exhibits pronounced analgesic effects in the Acetic acid (HY-Y0319)-induced in C57BL/6J mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS (HY-D1056)-induced (i.p., 0.5 mg/kg) inflammation in C57BL/6J mice[1]
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Dosage:2.5 mg/kg
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Administration:i.p., once
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Result:Suppressed LPS-induced increases in serum IL-6, TNF-α levels.
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Animal Model:The Acetic acid-induced (i.p., of 1% acetic acid, 10 mL/kg) in C57BL/6J mice[1]
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Dosage:2.5 mg/kg, 5 mg/kg
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Administration:i.p., once
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Result:Reduced the number of writhing, prolonged the latency to the first writhing at a concentration of 5 mg/kg.
Chemical Information
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CAS No. 3107363-68-5
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Molecular Weight 329.43
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Formula C20H27NO3
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SMILES
O=C(N)C1=C(O)C=C(OC/C=C(C)/CC/C=C(C)/C)C=C1C2CC2
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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)
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