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S1P1

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93

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5

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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 S1P1-5 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 .
    Sphingosine-1-phosphate
  • HY-12288
    Ozanimod
    4 Publications Verification

    RPC-1063

    LPL Receptor Neurological Disease Inflammation/Immunology
    Ozanimod (RPC-1063) is a CNS-penetrant sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
    Ozanimod
  • HY-12355
    Siponimod
    5+ Cited Publications

    BAF-312

    LPL Receptor Neurological Disease Inflammation/Immunology
    Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research - .
    Siponimod
  • HY-12789
    Etrasimod
    1 Publications Verification

    APD334

    LPL Receptor Inflammation/Immunology
    Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
    Etrasimod
  • HY-115831
    SAR247799
    2 Publications Verification

    S1P1 agonist 3

    LPL Receptor Cardiovascular Disease
    SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .
    SAR247799
  • HY-10569
    Ponesimod
    5+ Cited Publications

    ACT-128800

    LPL Receptor Inflammation/Immunology
    Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
    Ponesimod
  • HY-W008947
    SEW​2871
    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 .
    SEW​2871
  • HY-12288A
    Ozanimod hydrochloride
    4 Publications Verification

    RPC-1063 hydrochloride

    LPL Receptor Neurological Disease Inflammation/Immunology
    Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
    Ozanimod hydrochloride
  • HY-17606

    ACT-334441

    LPL Receptor Inflammation/Immunology
    Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous .
    Cenerimod
  • HY-16734A

    MT-1303 hydrochloride

    LPL Receptor Cardiovascular Disease Inflammation/Immunology
    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 .
    Amiselimod hydrochloride
  • HY-10968
    CYM5442
    3 Publications Verification

    LPL Receptor Neurological Disease
    CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS) .
    CYM5442
  • HY-18166

    LPL Receptor Inflammation/Immunology
    NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ 35S assays .
    NIBR0213
  • HY-108494

    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 .
    CYM50260
  • HY-117213

    S1P1-IN-Ex26

    LPL Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    Ex26 (S1P1-IN-Ex26) is a potent and selective sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach .
    Ex26
  • HY-110291

    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 .
    A-971432
  • 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 .
    CYM50308
  • HY-19511
    GSK2018682
    1 Publications Verification

    LPL Receptor Inflammation/Immunology
    GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
    GSK2018682
  • HY-101265

    S1p receptor agonist 1

    LPL Receptor Inflammation/Immunology
    Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
    Icanbelimod
  • HY-108496S

    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 .
    Sphingosine-1-phosphate-d7
  • HY-12835

    LPL Receptor Inflammation/Immunology
    S1P1 agonist III is an orally active hS1P1 agonist with an EC50 value of 18 nM. S1P1 agonist III shows limited activity against hS1P3. S1P1 agonist III can be used in the research of multiple sclerosis .
    S1P1 agonist III
  • HY-108490

    LPL Receptor Inflammation/Immunology
    VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively) .
    VPC 23019
  • HY-104069

    LPL Receptor Inflammation/Immunology
    S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.
    S1P1 agonist 1
  • HY-12355A
    Siponimod hemifumarate
    5+ Cited Publications

    BAF-312 hemifumarate

    LPL Receptor Potassium Channel Neurological Disease Inflammation/Immunology
    Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis .
    Siponimod hemifumarate
  • HY-101939A

    LPL Receptor Neurological Disease
    RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
    RP-001 hydrochloride
  • HY-148198

    LPL Receptor Neurological Disease Inflammation/Immunology
    S1P5 receptor agonist-1 (Example 6) is an effective and selective S1P5 receptor (S1P5 receptor) agonist. The EC50 values for S1P5 and S1P1 receptors are 20 nM and > 3 μM, respectively. S1P5 receptor agonist-1 can be used in studies on neuroprotection and immune regulation .
    S1P5 receptor agonist-1
  • HY-175984

    LPL Receptor Inflammation/Immunology
    S1P1 agonist 7 is a potent, orally active, and β-arrestin-biased S1P1 agonist (EC50(G‑protein) = 12.7 nM and EC50(β‑arrestin) = 3.23 nM). S1P1 agonist 7 demonstrates potent immunomodulatory activity and a favorable safety profile. S1P1 agonist 7 exhibits excellent metabolic stability, minimal to moderate CYP inhibition, and S1P3-sparing selectivity. S1P1 agonist 7 shows pharmacokinetics, effectively reduces circulating lymphocytes, and significantly alleviates disease severity in experimental autoimmune encephalomyelitis (EAE) mouse models under both prophylactic and therapeutic regimens. S1P1 agonist 7 can be used for multiple sclerosis (MS) research .
    S1P1 agonist 7
  • HY-108493

    LPL Receptor Inflammation/Immunology
    CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR .
    CS-2100
  • HY-32854

    5-Amino-2-bromobenzotrifluoride

    Drug Intermediate Neurological Disease Inflammation/Immunology
    4-Bromo-3-(trifluoromethyl)aniline (5-Amino-2-bromobenzotrifluoride) can be used for synthesis of AUY954 (HY-119221) (a S1P1 receptor agonist) .
    4-Bromo-3-(trifluoromethyl)aniline
  • HY-111021
    ASP-4058
    1 Publications Verification

    LPL Receptor Inflammation/Immunology
    ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
    ASP-4058
  • HY-119245

    BMS-986166

    LPL Receptor Inflammation/Immunology
    Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases .
    Udifitimod
  • HY-145362

    LPL Receptor Others
    S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
    S1P1 agonist 4
  • HY-18164

    LPL Receptor Inflammation/Immunology
    TASP0277308 is a highly selective S1P1 antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice .
    TASP0277308
  • HY-156565

    LPL Receptor Inflammation/Immunology
    S1P1 agonist 6 (Compound I) is a S1P1 agonist that reduces autoimmune ability by blocking the transportation of lymphocytes. S1P1 agonist 6 can be used as an immunosuppressive agent in the study of various autoimmune diseases research .
    S1P1 agonist 6
  • HY-144126

    LPL Receptor Inflammation/Immunology
    S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
    S1P1 agonist 5
  • HY-132847

    SCD-044

    LPL Receptor Inflammation/Immunology
    Vibozilimod (SCD-044) is an oral S1P1/EDG1 receptor-selective agonist with an EC50 of <1 nM. Vibozilimod promotes S1P1/EDG1 receptor internalization, inhibits lymphocyte migration, induces lymphopenia and reduces lymphocyte counts. Vibozilimod is used for the research of inflammatory diseases such as psoriasis and atopic dermatitis .
    Vibozilimod
  • HY-156565A

    S1P1 agonist 6 hemicalcium

    LPL Receptor Inflammation/Immunology
    S1P1 agonist 6 hemicalcium (Compound I) is a S1P1 agonist that reduces autoimmune ability by blocking the transportation of lymphocytes. S1P1 agonist 6 hemicalcium can be used as an immunosuppressive agent in the study of various autoimmune diseases research .
    Sumonerimod hemicalcium
  • HY-RS12391

    Small Interfering RNA (siRNA) LPL Receptor Others

    S1PR1 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    S1PR1 Human Pre-designed siRNA Set A
    S1PR1 Human Pre-designed siRNA Set A
  • HY-135432
    Etrasimod arginine
    1 Publications Verification

    APD334 arginine

    LPL Receptor Inflammation/Immunology
    Etrasimod arginine is an orally available S1P receptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4 +CD45RB high T cell-transferred mouse colitis model .
    Etrasimod arginine
  • HY-12789S

    APD334-d9

    Isotope-Labeled Compounds LPL Receptor Inflammation/Immunology
    Etrasimod-d9 (APD334-d9) is a deuterium labeled Etrasimod (HY-12789). Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells. .
    Etrasimod-d9
  • HY-120633A

    LPL Receptor Inflammation/Immunology
    BMS-986104 hydrochloride is a selective S1P1 receptor partial agonist, and can be used for research of autoimmune diseases .
    BMS-986104 hydrochloride
  • HY-12355S

    BAF-312-d11

    LPL Receptor Isotope-Labeled Compounds Neurological Disease Inflammation/Immunology
    Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research .
    Siponimod-d11
  • HY-16622

    LPL Receptor Cardiovascular Disease
    GSK1842799 is an orally active selective S1P1 receptor agonist prodrug. GSK1842799 is promising for research of multiple sclerosis .
    GSK1842799
  • HY-10968A

    LPL Receptor Neurological Disease
    CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS) .
    CYM5442 hydrochloride
  • HY-104069R

    Reference Standards LPL Receptor Inflammation/Immunology
    S1P1 agonist 1 (Standard) is the analytical standard of S1P1 agonist 1 (HY-104069). This product is intended for research and analytical applications. S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.
    S1P1 agonist 1 (Standard)
  • HY-101939

    LPL Receptor Neurological Disease
    RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
    RP-001
  • HY-W008947R

    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 .
    SEW​2871 (Standard)
  • HY-119221

    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 .
    AUY954
  • HY-14977

    LPL Receptor Inflammation/Immunology
    CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
    CS-0777-P
  • HY-12355R

    BAF-312 (Standard)

    Reference Standards LPL Receptor Neurological Disease Inflammation/Immunology
    Siponimod (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research - .
    Siponimod (Standard)
  • HY-16622A

    LPL Receptor Others
    GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
    GSK 1842799 TFA

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