ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.
|Solubility (25°C)||DMSO 43 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Maike R Pollmanns, et al. Front Cell Neurosci. Activated Endolysosomal Cation Channel TRPML1 Facilitates Maturation of α-Synuclein-Containing Autophagosomes
 Katharina Kriegler, et al. Arch Pharm (Weinheim). Effective chiral pool synthesis of both enantiomers of the TRPML inhibitor trans-ML-SI3
 Philip Schmiege, et al. Structure. Atomic insights into ML-SI3 mediated human TRPML1 inhibition
 Charlotte Leser, et al. Eur J Med Chem. Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3
 Dan Li, et al. Autophagy. Sulforaphane Activates a lysosome-dependent transcriptional program to mitigate oxidative stress
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