cim0216

SKU: orb1298232

Description

CIM0216 is a potent synthetic activator of the TRPM3 ion channel, demonstrating significantly higher efficacy and binding affinity than its endogenous agonist. This small molecule is a valuable research tool for investigating TRPM3 function in pain sensation, insulin release, and thermal hyperalgesia in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1031496-06-6
• MW: 347.41
• Purity: 99.87% (May vary between batches)
• Formula: C₂₁H₂₁N₃O₂
• SMILES: Cc1cc(NC(=O)C(N2CCCc3ccccc23)c2ccccc2)no1
• Target: TRP/TRPV Channel
• Solubility: DMSO:65 mg/mL (187.1 mM);Ethanol:17 mg/mL (48.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.76 mM)

Bioactivity

• In Vitro:
  CIM0216 Selectively Activates TRPM3 in Stably Transfected HEK293 Cells.A diverse small-molecule library was screened for compounds that modulate TRPM3-mediated Ca2+ responses in HEK293 cells stably expressing murine TRPM3 (HEK-TRPM3 cells), as described previously.In HEK-TRPM3 cells, CIM0216 elicited a dose-dependent Ca2+ response [negative logarithm of the EC50 value (pEC50) = 0.77 ± 0.1 μM], which was not observed in nontransfected HEK293 cells . The endogenous TRPM3 activator pregnenolone sulfate (PS) also elicited a dose-dependent Ca2+ response, typified by a smaller Ca2+ influx and a fivefold lower potency (pEC50 = 3.0 ± 0.1 μM; n = 2) compared with CIM0216 . In the presence of 40 μM PS, the dose dependency of CIM0216 shifted to a lower concentration in HEK-TRPM3 cells (pEC50 = 42 ± 0.6 nM CIM0216 in the presence of PS). Single-cell FURA2-ratiometric Ca2+ imaging revealed a robust increase in intracellular Ca2+ concentration (1,145 ± 26 nM; n = 603 from at least three independent measurements) on stimulation with 1 μM CIM0216 in all HEK-TRPM3 cells. These responses were not observed in nontransfected HEK cells (n = 166) or in the absence of extracellular Ca2+.

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

Inhibitor, neurogenic, N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide, inflammation, inhibit, CIM 0216, cim0216, cim-0216, sensory nerve, Transient receptor potential channels, TRPV Channel, TRPVChannel, TRP Channel, TRPChannel, TRPM3

Compound Identifiers

PubChem CID

42887770