For research use only. Not for therapeutic Use.
Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
target: S1P1
In vivo: After oral administration of amiselimod or fingolimod at 1 mg/kg, the concentration of amiselimod-P in rat heart tissue was relatively lower than that of fingolimod-P, potentially contributing to the minimal cardiac effects of amiselimod. Amiselimod-P showed potent selectivity for S1P1 , high selectivity for S1P5 , minimal agonist activity for S1P4 , no distinct agonist activity for S1P2 or S1P3 , and approximately 5-fold weaker GIRK activation than fingolimod-P. [1] Amiselimod 0·2 mg and 0·4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions. [2]
| Catalog Number | I005600 |
| CAS Number | 942398-84-7 |
| Synonyms | 2-amino-2-[2-[4-heptoxy-3-(trifluoromethyl)phenyl]ethyl]propane-1,3-diol;hydrochloride |
| Molecular Formula | C19H31ClF3NO3 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H30F3NO3.ClH/c1-2-3-4-5-6-11-26-17-8-7-15(12-16(17)19(20,21)22)9-10-18(23,13-24)14-25;/h7-8,12,24-25H,2-6,9-11,13-14,23H2,1H3;1H |
| InChIKey | GEDVJGOVRLHFQG-UHFFFAOYSA-N |
| SMILES | CCCCCCCOC1=C(C=C(C=C1)CCC(CO)(CO)N)C(F)(F)F.Cl |
| Reference | [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. 2016 Oct 7. [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. |
