942398-84-7

942398-84-7 structure

Name: Amiselimod hydrochloride
Chemical Name: amiselimod hydrochloride
CAS Number: 942398-84-7
Molecular Formula: C₁₉H₃₁ClF₃NO₃
Molecular Weight: 413.902
Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
Create Date: 2018-08-06 06:24:22
Modify Date: 2024-01-05 18:19:39
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]

Name	amiselimod hydrochloride
Synonyms	MT-1303 UNII-AY898D6RU1 AMISELIMOD HYDROCHLORIDE 2-Amino-2-{2-[4-(heptyloxy)-3-(trifluorométhyl)phényl]éthyl}-1,3-propanediol, chlorhydrate (1:1) 2-Amino-2-{2-[4-(heptyloxy)-3-(trifluormethyl)phenyl]ethyl}-1,3-propandiolhydrochlorid (1:1) 2-Amino-2-{2-[4-(heptyloxy)-3-(trifluoromethyl)phenyl]ethyl}-1,3-propanediol hydrochloride (1:1) 1,3-Propanediol, 2-amino-2-[2-[4-(heptyloxy)-3-(trifluoromethyl)phenyl]ethyl]-, hydrochloride (1:1) Amiselimod HCl

Description	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]
Related Catalog	Signaling Pathways >> GPCR/G Protein >> LPL Receptor Research Areas >> Cancer
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.