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CAS No.: 942398-84-7

Amiselimod HCl Catalog No. CSN18986

Synonyms: MT-1303 hydrochloride;MT-1303 HCl;Amiselimod (hydrochloride)

Amiselimod HCl is a sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.

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生物活性

描述Sphingosine 1‐phosphate (S1P), a multi‐functional lysophospholipid mediator, is generated from sphingosine by sphingosine kinases (SPHKs) and binds to five subtypes of G protein‐coupled S1P receptors (S1P_1–5). Amiselimod is a second-generation sphingosine 1-phosphate (S1P) receptor modulator which is used to reduce the bradycardia associated with fingolimod and other S1P receptor modulators. The active metabolite amiselimod‐P showed agonist activity at S1P₁ (EC₅₀ 75 pM). In rats, the concentration of amiselimod‐P in the heart was relatively lower than fingolimod‐P following a single oral administration of amiselimod or fingolimod at 1 mg/kg. A dose‐dependent reduction in lymphocyte counts was observed in healthy subjects, receiving between 0.125 and 0.5 mg amiselimod. Trough lymphocyte counts on day 21 decreased by 66 and 60% at doses of 0.5 and 0.75 mg respectively^[3]. Amiselimod 0.2 mg and 0.4 mg significantly reduced the total number of gadolinium-enhanced T1-weighted lesions^[4].
参考文献

[1] Sugahara K, Maeda Y, 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.
[2] Kappos L, Arnold DL, 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.
[3] Sugahara K, Maeda Y, Shimano 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;174(1):15‐27
[4] Kappos L, Arnold DL, Bar-Or A, et al. Safety and efficacy of amiselimod in relapsing multiple sclerosis (MOMENTUM): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet Neurol. 2016;15(11):1148‐1159

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4160 mL
- 12.0801 mL
- 24.1603 mL
- 5 mM
- 0.4832 mL
- 2.4160 mL
- 4.8321 mL
- 10 mM
- 0.2416 mL
- 1.2080 mL
- 2.4160 mL

技术信息

CAS号

942398-84-7

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H31ClF3NO3

运输

蓝冰

分子量

413.90

别名

MT-1303 hydrochloride;MT-1303 HCl;Amiselimod (hydrochloride);MT-1303;Amiselimod HCl;Amiselimod Hydrochloride

溶解度

DMSO	290.0 mg/mL (700.6 mM)
Water	insoluble

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