A non-cytotoxic morpholinyl-cyclohexylbenzenesulfonamide compound that acts as a selective agonist of TRPML3 channel (EC50 = 873 nM in hTRPML3-YPF transfected HEK293 cells). Displays significantly weaker agonistic activity for TRPML2 channel (54.5% at 10 µM) and is shown to be inactive against hTRPML1, hTRPM2, mTRPV2, hTRPC3, drTRPN1, and hTRPA1 (~10 µM). Also binds to sigma-1 receptor at much higher concentrations (IC50 = 31 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target TRPML3
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Antolin, A.A., and Mestres, J. 2015. ACS Chem. Biol.10, 395.
Grimm, C., et al. 2012. J. Biol. Chem.287, 22701. Saldanha, S., et al. 2010. Probe Reports from the NIH Molecular Libraries Program. Grimm, C., et al. 2010. Chem. Biol.17, 135.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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