IMMH001

IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research[1][2].

Signaling Pathways >> GPCR/G Protein >> LPL Receptor

Research Areas >> Inflammation/Immunology

S1PR1

IMMH001 is converted to the active form, its monophosphate ester (S)-IMMH001-P, by sphingosine kinase 1 (SphK1) and sphingosine kinase 2 (SphK2) in vivo[1]. IMMH001 suppresses both Th1 cell (IL-1β, IL-18, and IP10) and Th2 cell (IL-5)-mediated disease reactions in damaged joints[2]. IMMH001 (0.3-2.4 mg/kg, Orally; twice a week, for 28 days, AA rats; for 30 days, CIA rats) relieves the damage of AA (adjuvant-induced arthritis) and CIA (collagen-induced arthritis) rats’ joints[2].

[1]. Xiao Q, et al. Design and synthesis of analogues of the sphingosine-1-phosphate receptor 1 agonist IMMH001 with improved phosphorylation rate in human blood. Bioorg Med Chem. 2020 Nov 1;28(21):115722.

[2]. Jin J, et al. Sphingosine-1-Phosphate Receptor Subtype 1 (S1P1) Modulator IMMH001 Regulates Adjuvant- and Collagen-Induced Arthritis. Front Pharmacol. 2019 Sep 19;10:1085.