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Sphingosine-1-phosphate receptor agonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (4) Drug Isomer (1) Drug Metabolite (3) Endogenous Metabolite (2) ERK (2) GSK-3 (2) JAK (2) LPL Receptor (21) Mitochondrial Metabolism (1) Reactive Oxygen Species (ROS) (2) Reference Standards (2) SphK (1) STAT (2)
By Research Areas:	Cancer (4) Cardiovascular Disease (4) Endocrinology (2) Inflammation/Immunology (15) Metabolic Disease (4) Neurological Disease (6)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108496

Sphingosine-1-phosphate 15+ Cited Publications S1P	Endogenous Metabolite LPL Receptor	Inflammation/Immunology Endocrinology Cancer
Sphingosine-1-phosphate (S1P) is an agonist of S1P_1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca ²⁺ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids . Sphingosine-1-phosphate stimulates the DNA synthesis, cell proliferation and migration .

HY-W008947

SEW2871 5+ Cited Publications	LPL Receptor ERK Akt	Neurological Disease Metabolic Disease Inflammation/Immunology
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC₅₀ of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .

HY-108494

CYM50260	LPL Receptor	Cardiovascular Disease
CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P₄-R) agonist with an EC₅₀ of 45 nM. CYM50260 displays no activity against S1P₁-R, S1P₂-R, S1P₃-R and S1P₅-R .

HY-110291

A-971432	LPL Receptor	Neurological Disease
A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC₅₀s of .362, >10, 0.006 μM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .

HY-108495

CYM50308 1 Publications Verification ML248	LPL Receptor	Cardiovascular Disease
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P₄-R) agonist with an EC₅₀ of 56 nM. CYM50308 displays 37-fold more selective for S1P₄-R than S1P₅-R. CYM50308 has no activity at S1P₁-R, S1P₂-R and S1P₃-R subtypes at concentrations up to 25 μM .

HY-13660

Mocravimod hydrochloride 2 Publications Verification KRP-203	LPL Receptor Reactive Oxygen Species (ROS) Akt GSK-3 JAK STAT	Metabolic Disease Inflammation/Immunology Cancer
Mocravimod (hydrochloride) is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod (hydrochloride) preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod (hydrochloride) significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod (hydrochloride) retains T cell effector function. Mocravimod (hydrochloride) can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI) .

HY-109038

Mocravimod 2 Publications Verification KRP-203 free base	LPL Receptor Reactive Oxygen Species (ROS) Mitochondrial Metabolism Akt GSK-3 JAK STAT	Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
Mocravimod (KRP-203 free base) is a sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod retains T cell effector function. Mocravimod can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI) .

HY-108496S

Sphingosine-1-phosphate-d7 S1P-d₇	Endogenous Metabolite LPL Receptor	Endocrinology
Sphingosine-1-phosphate-d₇ is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .

HY-136578

RP101988	LPL Receptor Drug Metabolite	Inflammation/Immunology Cancer
RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC₅₀s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely .

HY-136576

RP101075 1 Publications Verification	LPL Receptor Drug Metabolite	Inflammation/Immunology
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC₅₀ of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC₅₀=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile .

HY-164964

TRV045	LPL Receptor	Neurological Disease
TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity .

HY-119221

AUY954	LPL Receptor	Neurological Disease Inflammation/Immunology
AUY954 is an oral active and selective sphingosine-1-phosphate receptor 1 agonist with the EC₅₀ values of 1.2 nM, 0.9 nM >10,000 nM, 1,210 nM, >1,000 nM, and 340 nM for hS1P2, mS1P2, S1P2, S1P3, S1P4, and S1P5 receptors, respectively. AUY954 can be used for study of experimental autoimmune neuritis .

HY-139555

Zectivimod	LPL Receptor	Inflammation/Immunology
Zectivimod is a **sphingosine-1-phosphate receptor** agonist. Zectivimod can be used for the research of autoimmune diseases，chronic inflammatory diseases and immunoregulation disorders .

HY-143865

S1PR1 agonist 2	LPL Receptor	Inflammation/Immunology
S1PR1 agonist 2 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 2 has the potential for the research of autoimmune diseases (extracted from patent WO2021175225A1, compound 1) .

HY-147660

IMMH001	LPL Receptor	Inflammation/Immunology
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 .

HY-W008947R

SEW2871 (Standard)	Reference Standards LPL Receptor ERK Akt	Neurological Disease Metabolic Disease Inflammation/Immunology
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .

HY-16621

PPI-4955	SphK	Inflammation/Immunology
PPI-4955 is a subtype 1 (S1P₁) agonist of sphingosine-1-phosphate receptor with an EC₅₀ of 1.62 nM. PPI-4955-P (the active phosphorylated form) exhibits excellent receptor selectivity and affinity, and the IC₅₀ values for hS1P₁, hS1P₃, hS1P₄, and hS1P₅ are 0.23, 2000, 6.5, and 184 nM respectively. PPI-4955 has significantly improved in vivo phosphorylation efficiency, which can reduce lymphocytes and improve cardiovascular risk. PPI-4955 can be used in immunomodulation research .

HY-50692

CAY10734	LPL Receptor	Inflammation/Immunology
CAY10734 is the agonist for sphingosine-1-phosphate receptor 1 (S1P1) with an IC₅₀ of 1.3 nM. CAY10734 promotes the recirculation of peripheral blood lymphocytes, and is a potential immunosuppressant .

HY-136577

RP101442	LPL Receptor Drug Metabolite	Inflammation/Immunology
RP101442, an active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC₅₀s of 2.6 nM and 171 nM for S1PR1 and S1PR5, respectively .

HY-143864

S1PR1 agonist 1	LPL Receptor	Inflammation/Immunology
S1PR1 agonist 1 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 1 has the potential for the research of autoimmune diseases (extracted from patent WO2021175223A1, compound 22) .

HY-119221A

AUY 954 hydrochloride	LPL Receptor	Neurological Disease
AUY 954 hydrochloride is a potent and selective sphingosine-1-phosphate (S1P(1)) receptor agonist, exhibiting significant immunomodulatory activity. AUY 954 hydrochloride induces a profound and reversible reduction of circulating lymphocytes upon oral administration. AUY 954 hydrochloride has demonstrated efficacy in prolonging cardiac allograft survival when used in combination with RAD001 in a stringent transplantation model. AUY 954 hydrochloride effectively prevents experimental autoimmune neuritis in rats, showcasing its therapeutic potential in autoimmune conditions.

HY-113040B

(±)-(17S,18R)-Epoxyeicosatetraenoic acid (±)-17(S),18(R)-EETeTr	Drug Isomer	Others
(±)-(17S,18R)-Epoxyeicosatetraenoic acid ((±)-17 (S),18 (R)-EETeTr) is one of the constituent enantiomers of (±) 17 (18)-EpETE. (±) 17 (18)-EpETE is an active metabolite of the ω-3 fatty acid eicosapentaenoic acid, and also an agonist of sphingosine-1-phosphate receptor 1 (S1P1) .

HY-108495R

CYM50308 (Standard) ML248 (Standard)	Reference Standards LPL Receptor	Cardiovascular Disease
CYM50308 (Standard) is the analytical standard of CYM50308 (HY-108495). This product is intended for research and analytical applications. CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC₅₀ of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-108496

Sphingosine-1-phosphate 15+ Cited Publications S1P	Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Endogenous Metabolite LPL Receptor
Sphingosine-1-phosphate (S1P) is an agonist of S1P_1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca ²⁺ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids . Sphingosine-1-phosphate stimulates the DNA synthesis, cell proliferation and migration .

Cat. No.	Product Name	Chemical Structure

HY-108496S

Sphingosine-1-phosphate-d7
Sphingosine-1-phosphate-d₇ is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .

Sphingosine-1-phosphate-d7

Sphingosine-1-phosphate-d₇ is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .

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