AKP-11 treatment caused milder and reversible lymphopenia as compared to the severe and long lasting lymphopenia observed with FTY720. Secondly, AKP-11 treatment did not cause adverse effects observed with FTY720 treatment. These findings indicate that AKP-11 mediated S1P1 agonist activity may be of therapeutic value for MS and other immune mediated disorders with better safety profile.
|Cell lines||CHO cells|
|Preparation method||Before treatment with AKP-11 or FTY720 or FTY720P (Echelon Biosciences Inc. Salt Lake City, UT), the cells were serum starved in six well plates for 4hrs at 37°C and then they were incubated with the above compounds at 37°C.|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
AKP-11 - A Novel S1P1 Agonist with Favorable Safety Profile Attenuates Experimental Autoimmune Encephalomyelitis in Rat Model of Multiple Sclerosis.
Samuvel DJ, et al. PLoS One. 2015 Oct 29;10(10):e0141781. PMID: 26513477.
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