Amiseimod hydrochloride 是一种新型鞘氨醇 1-磷酸受体 1 (S1P1) 调节剂，旨在减少与芬戈莫德和其他 S1P 受体调节剂相关的心动过缓效应。
| Cas No. | 942398-84-7 |
| 别名 | MT-1303盐酸盐,MT-1303 hydrochloride |
| Canonical SMILES | OCC(CCC1=CC=C(OCCCCCCC)C(C(F)(F)F)=C1)(N)CO.[H]Cl |
| 分子式 | C19H31ClF3NO3 |
| 分子量 | 413.9 |
| 溶解度 | DMSO : ≥ 32 mg/mL (77.31 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: S1P1In 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] References:
[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. |
