| Name | cim0216 |
| Description | CIM0216 is a synthetic TRPM3 activator whose potency and apparent affinity greatly exceeds that of the canonical TRPM3 agonist. |
| 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[1].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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 65 mg/mL (187.1 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.76 mM), Sonication is recommended.
Ethanol : 17 mg/mL (48.93 mM), Sonication and heating are recommended.
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| Keywords | TRPVChannel | TRPV Channel | TRPM3 | TRPChannel | TRP Channel | Transient receptor potential channels | sensory nerve | neurogenic | Inhibitor | inhibit | inflammation | cim-0216 | cim0216 | CIM 0216 |
| Inhibitors Related | (+)-Camphor | Rosiglitazone | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Probenecid | Pregnenolone | Nonivamide | 1,4-Cineole | trans-Cinnamaldehyde | Methyl salicylate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
