942399-20-4
Chemical Structure
Amiselimod
Synonym(s): MT-1303
- CAS No.: 942399-20-4
- Formula:C19H30F3NO3
- Molecular Weight:377.44
IUPAC Name: 2-amino-2-(4-(heptyloxy)-3-(trifluoromethyl)phenethyl)propane-1,3-diol
InChIKey: JVCPIJKPAKAIIP-UHFFFAOYSA-N
SMILES: FC(F)(C1=CC(CCC(CO)(CO)N)=CC=C1OCCCCCCC)F
Biological Activity: Amiselimod (MT-1303) is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod is an orally active and high selectivity sphingosine 1-phosphate receptor-1 (S1P1) agonist, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimodis promising for research of autoimmune diseases[1][2][3][4].
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Amiselimod | Amiselimod (MT-1303) is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod is an orally active and high selectivity sphingosine 1-phosphate receptor-1 (S1P1) agonist, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimodis promising for research of autoimmune diseases. | |||||||||||||||||||||
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- [1]. Sugahara K, et al., Amiselimod, a novel sphingosine 1-phosphate receptor-1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk. Br J Pharmacol. 2017 Jan;174(1):15-27. [Content Brief]
- [2]. Kappos L, et al. Safety and efficacy of amiselimod in relapsing multiple sclerosis (MOMENTUM): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet Neurol. 2016 Oct;15(11):1148-59. [Content Brief]
- [3]. Shimano K, et al. Amiselimod (MT-1303), a novel sphingosine 1-phosphate receptor-1 functional antagonist, inhibits progress of chronic colitis induced by transfer of CD4+CD45RBhigh T cells. PLoS One. 2019 Dec 5;14(12):e0226154. [Content Brief]
- [4]. Sugahara K, et al. Amiselimod (MT-1303), a Novel Sphingosine 1-Phosphate Receptor-1 Modulator, Potently Inhibits the Progression of Lupus Nephritis in Two Murine SLE Models. J Immunol Res. 2019 Dec 23;2019:5821589. [Content Brief]
Keywords
