Amiselimod hydrochloride

Amiselimod hydrochloride (MT-1303 hydrochloride) 是一种鞘氨醇 1-磷酸受体 1 (S1P1) 调节剂。

CAS号

942398-84-7

分子式

C19H31ClF3NO3

主要靶点

LPL Receptor|S1P Receptor

仅限科研使用

Cat No : CM04981

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Synonyms

MT-1303 hydrochloride



产品信息

Amiselimod hydrochloride is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.

CAS号 942398-84-7
分子式 C19H31ClF3NO3
主要靶点 LPL Receptor|S1P Receptor
主要通路 G蛋白偶联受体
分子量 413.9
纯度 99.68%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 MT-1303 hydrochloride

体内活性

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].

溶解度

DMSO:27mg/ml (65.23 mM)

参考文献

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.

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