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Sphingosine-1-phosphate (S1P) receptor modulators act on S1PR1 to S1PR5, five G protein-coupled lipid receptors. In 1998 S1P was identified as a ligand of the orphan receptor endothelial differentiation gene 1 (EDG-1), now called S1PR1. FTY720 (fingolimod) was shown in 2002 to be phosphorylated in vivo and to act on four of the five S1P receptors. Two years later, lymphocyte egress from thymus and lymph nodes was found to depend on S1PR1. Ozanimod, BAF312 and ponesimod are further S1PR1-directed modulators, CYM 5442 HCl is a selective S1PR1 agonist and TY-52156 blocks S1PR3. Opaganib inhibits sphingosine kinase 2 (SphK2) and so limits S1P synthesis upstream of the receptors.
Synonyms: RPC-1063
RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-associated diseases.
Synonyms: ACT-128800
Ponesimod is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
Synonyms: AK174154
NS13001 is a selective SK2/3 modulator that acts as a potential therapeutic agent for treatment of SCA2 and possibly other cerebellar ataxias.
Synonyms: KRP-203 free base
Mocravimod is a sphingosine-1-phosphate receptor (S1PR) modulator that inhibits the signaling necessary for T cell egress from lymph nodes and other lymphoid tissues. It preferentially binds to S1PR1, exhibiting beneficial effects such as a reduction in reactive oxygen species (ROS) levels, prevention of mitochondrial permeability transition pore opening, and enhancement of mitochondrial membrane potential (MMP). Additionally, Mocravimod promotes the phosphorylation of key signaling proteins including AKT, ERK, GSK-3β, JAK2, and STAT3, while preserving T cell effector function. This reagent is suitable for research into acute myelogenous leukemia, diabetes, and myocardial ischemia-reperfusion injury.
Synonyms: MT-1303 hydrochloride
Amiselimod hydrochloride is a selective sphingosine 1-phosphate receptor-1 (S1P1) modulator that is converted in vivo to its active metabolite, amiselimod phosphate. It is orally active and designed to minimize bradycardia effects commonly seen with other S1P receptor modulators. Key biological activities include the inhibition of chronic colitis through the reduction of Th1 and Th17 cell infiltration into the colon, as well as the suppression of autoreactive T cell infiltration in lupus nephritis. Amiselimod hydrochloride is of considerable interest for research in autoimmune diseases.
Synonyms: RPC-1063 hydrochloride
Ozanimod hydrochloride, an S1P receptor modulator, selectively binds to sphingosine 1-phosphate receptor subtypes 1 (S1P1) and 5 (S1P5) with high affinity, exhibiting EC50 values of 1.03 nM and 8.6 nM, respectively. This compound demonstrates immunomodulatory effects, making it relevant for investigating mechanisms of action in relapsing multiple sclerosis (MS). Ozanimod hydrochloride serves as a valuable tool for research focused on S1P receptor signaling pathways and their implications in autoimmune disorders.
Synonyms: BAF-312 hemifumarate
Siponimod hemifumarate is a selective sphingosine-1-phosphate (S1P) receptor modulator, primarily targeting S1P1 and S1P5 receptors. It demonstrates potency with EC50 values of 0.39 nM and 0.98 nM, respectively, while showing significantly reduced activity against S1P2, S1P3, and S1P4. This compound is essential for investigating therapeutic strategies in multiple sclerosis (MS) and related neurological disorders.
Synonyms: MT-1303
Amiselimod is a selective sphingosine 1-phosphate receptor-1 (S1P1) modulator that is converted to its active metabolite, Amiselimod phosphate, by sphingosine kinases in vivo. Exhibiting oral bioactivity, Amiselimod effectively inhibits chronic colitis by restricting the infiltration of Th1 and Th17 colitogenic cells into the colon. Additionally, it shows potential in the treatment of lupus nephritis by decreasing the presence of autoreactive T cells in the kidneys. This compound is valuable for research into various autoimmune diseases.
Synonyms: VTX002
Tamuzimod is a potent S1P receptor modulator, exhibiting significant immunomodulatory effects. With an EC50 value of less than 1 μM, it effectively influences S1P receptor signaling pathways. This compound is primarily utilized in research applications focused on immune modulation and related disease models.
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Synonyms: APD334 arginine
Etrasimod arginine is an orally bioavailable sphingosine-1-phosphate (S1P) receptor modulator, acting as a potent full agonist at the S1P1 receptor while displaying partial agonist activity at the S1P4 receptor. This compound exhibits significant anti-inflammatory effects, demonstrated in a CD4+CD45RBhigh T cell-transferred mouse model of colitis. Etrasimod arginine is valuable for research applications targeting immune modulation and inflammatory diseases.
Synonyms: BMS-986166
Udifitimod (BMS-986166) is a selective, orally active modulator of the sphingosine-1-phosphate receptor 1 (S1P1R). This compound demonstrates significant potential in the modulation of immune responses, making it valuable for research focused on autoimmune diseases. Its ability to influence lymphocyte egress and migration underscores its relevance in therapeutic investigations.
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RP-1859 is a sphingosine 1-phosphate (S1P) modulator that exhibits anti-inflammatory and immunomodulatory properties. This compound is particularly relevant in the study of iatrogenic autoimmune colitis, facilitating investigations into the underlying mechanisms of this condition and potential therapeutic interventions. RP-1859's modulation of S1P signaling pathways may provide valuable insights into inflammatory responses and immune regulation.
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LX2932 is an orally active modulator of the sphingosine 1-phosphate (S1P) signaling axis, impacting S1PR receptor activity. It demonstrates a dose-dependent reduction in circulating lymphocyte populations, which may aid in the treatment of autoimmune disorders. LX2932 has shown efficacy in improving collagen-induced arthritis, making it a valuable compound for research in immunology and inflammatory disease models.
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