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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).
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.
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.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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).
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
384352-24-3
Chemical formula
C₁₆H₂₃ClN₂O₃S
Purity
≥92% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
