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Synonyms: Example 1 [US20090137530] | MT-1303 | MT1303
Compound class: Synthetic organic
Comment: Amiselimod (MT-1303) is claimed in patent US20090137530 (Compound 1-3 is the hydrochloride used experimentally) as a potential immunomodulatory agent . It is a sphingosine-1-phosphate (SIP) receptor prodrug agonist, similar in action to the approved MS drug fingolimod, but with improved receptor subtype selectivity .
Selective SIP1 receptor agonists are being investigated for immunomodulatory/immunosuppresant action in MS and other autoimmune conditions .
|In vivo (in mice) amiselimod (MT-1303) hydrochloride decreases peripheral blood lymphocyte count with an ED50 value of 0.04mg/kg body weight . Affinity for S1P receptors is not provided in the patent. Note that bioactivity is attributed to the active metabolite amiselimod phosphate , the prodrug is almost completely inactive at S1P1R.|