TRPM8 antagonist 2

SKU: orb1301572

Description

TRPM8 antagonist 2 is a highly potent and selective inhibitor of the TRPM8 ion channel, exhibiting an IC50 of 0.2 nM. It is a valuable research tool for investigating neuropathic pain mechanisms in both in vitro cellular assays and in vivo animal models of cold allodynia.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 259674-19-6
• MW: 398.5
• Purity: 98.10% (May vary between batches)
• Formula: C₂₆H₂₆N₂O₂
• SMILES: COC(=O)[C@H](Cc1c[nH]c2ccccc12)N(Cc1ccccc1)Cc1ccccc1
• Target: TRP/TRPV Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.04 mM);DMSO:160 mg/mL (401.51 mM)

Bioactivity

• Target IC50:
  TRPM8:0.2 nM
• In Vivo:
  TRPM8 antagonist 2, administered subcutaneously at doses of 1, 10, and 30 mg/kg, demonstrates significant, dose-dependent antinociceptive effects and reduces wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at the 30 mg/kg dosage. Additionally, at lower doses of 0.1 and 1 μg, it effectively mitigates Oxaliplatin (OXP)-induced cold allodynia in mice.
• In Vitro:
  TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM, used in neuropathic pain research. It effectively inhibits menthol-induced increases in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells expressing the rat TRPM8 isoform (IC50, 40 nM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Transient receptor potential channels, TRP Channel, TRPV Channel, TRPM8 antagonist 2, TRPM-8 antagonist 2, TRPChannel, TRPM8, TRPVChannel

Compound Identifiers

PubChem CID

57055437