Amiselimod (hydrochloride)

Amiselimod (MT-1303) hydrochloride is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod hydrochloride is an orally active and high selectivity sphingosine 1-phosphate receptor-1 (S1P1) agonist, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod hydrochloride inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod hydrochloride inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimod hydrochloride is promising for research of autoimmune diseases[1][2][3][4].

Product Specifications

CAS Number

[942398-84-7]

Product Name Alternative

MT-1303 hydrochloride

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

LPL Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Amiselimod-hydrochloride.html

Concentration

10mM

Purity

98.71

Solubility

DMSO : 110 mg/mL (ultrasonic)

Smiles

OCC(CCC1=CC=C(OCCCCCCC)C(C(F)(F)F)=C1)(N)CO.[H]Cl

Molecular Formula

C19H31ClF3NO3

Molecular Weight

413.90

Precautions

H302, H315, H319, H335

References & Citations

[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.|[3]Shimano K, et al. Amiselimod (MT-1303), a novel sphingosine 1-phosphate receptor-1 functional antagonist, inhibits progress of chronic colitis induced by transfer of CD4+CD45RBhigh T cells. PLoS One. 2019 Dec 5;14 (12) :e0226154. |[4]Sugahara K, et al. Amiselimod (MT-1303), a Novel Sphingosine 1-Phosphate Receptor-1 Modulator, Potently Inhibits the Progression of Lupus Nephritis in Two Murine SLE Models. J Immunol Res. 2019 Dec 23;2019:5821589.