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S1P1 agonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Drug Intermediate (1) Drug Isomer (1) Endogenous Metabolite (3) ERK (2) Isotope-Labeled Compounds (2) LPL Receptor (62) Reference Standards (7) SphK (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (9) Endocrinology (3) Infection (1) Inflammation/Immunology (45) Metabolic Disease (2) Neurological Disease (17)

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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-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 ^- .

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 .

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-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 .

HY-16734A

Amiselimod hydrochloride 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 .

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) .

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-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.

HY-101265

Icanbelimod 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.

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-108490

VPC 23019	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 (pK_i= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC₅₀= 6.58 and 7.07, respectively) .

HY-101939A

RP-001 hydrochloride	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 .

HY-148198

S1P5 receptor agonist-1	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 .

HY-12835

S1P1 agonist III	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 .

HY-108493

CS-2100	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 .

HY-32854

4-Bromo-3-(trifluoromethyl)aniline 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) .

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 .

HY-12355A

Siponimod hemifumarate 5+ Cited Publications BAF-312 hemifumarate	LPL Receptor	Neurological Disease Inflammation/Immunology
Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC₅₀s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research .

HY-104069

S1P1 agonist 1	LPL Receptor	Inflammation/Immunology
S1P1 Agonist 1 is a *S1P1* agonist with immunomodulatory activities.

HY-132847

Vibozilimod 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 .

HY-135432

Etrasimod arginine 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 .

HY-175984

S1P1 agonist 7	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 .

HY-120633A

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

HY-16622

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

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-101939

RP-001	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 .

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-145362

S1P1 agonist 4	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).

HY-14977

CS-0777-P	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) .

HY-10968A

CYM5442 hydrochloride	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) .

HY-16622A

GSK 1842799 TFA	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 .

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-120615

BMS-520	LPL Receptor	Neurological Disease Inflammation/Immunology
BMS-520 is a potent, orally active and selective sphingosine-1-phosphate 1 (S1P₁) agonist with an EC₅₀ of 0.47nM. BMS-520 shows ~3400-fold selectivity over S1P₃. BMS-520 demonstrates impressive efficacy in a rat model of arthritis and in a mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis. BMS-520 can be used for arthritis and EAE research .

HY-16734

Amiselimod MT-1303	LPL Receptor	Cardiovascular Disease Inflammation/Immunology
Amiselimod (MT-1303) is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod 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 inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimodis promising for research of autoimmune diseases .

HY-144126

S1P1 agonist 5	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) .

HY-156565

S1P1 agonist 6	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 .

HY-156565A

Sumonerimod hemicalcium 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 .

HY-120468

GSK2263167	LPL Receptor	Inflammation/Immunology
GSK2263167 is a S1P1 receptor agonist

HY-118919

CYM5181	LPL Receptor	Others
CYM5181 is a novel *S1P1* agonist with a pEC₅₀ value of -8.47 .

HY-14433A

(S)-PF-462991 (S)-PF-991	LPL Receptor	Inflammation/Immunology
(S)-PF-462991 is a direct-acting S1P_1,5 agonist .

HY-10569R

Ponesimod (Standard) ACT-128800 (Standard)	Reference Standards LPL Receptor	Inflammation/Immunology
Ponesimod (Standard) is the analytical standard of Ponesimod. This product is intended for research and analytical applications. 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 .

HY-120611A

BMS-960	LPL Receptor	Cardiovascular Disease Inflammation/Immunology
BMS-960 is a potent and selective *S1P₁* receptor agonist containing isoxazole, which can be used in the research of immune diseases and vascular diseases .

HY-157787

Ginkgolic acid 2-phosphate	LPL Receptor	Neurological Disease
Ginkgolic acid 2-phosphate is a potent sphingosine 1-phosphate agonist. Ginkgolic acid 2-phosphate induces ERK phosphorylation. Ginkgolic acid 2-phosphate interactes with S1P1 .

HY-120611

BMS-960 free base	LPL Receptor	Cardiovascular Disease Inflammation/Immunology
BMS-960 free base is a potent and selective *S1P₁* receptor agonist containing isoxazole, which can be used in the research of immune diseases and vascular diseases .

HY-10569S

Ponesimod-d4 ACT-128800-d₄	Isotope-Labeled Compounds LPL Receptor	Others
Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569) . 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 .

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-10569S1

Ponesimod-d7 ACT-128800-d₇	Isotope-Labeled Compounds	Others
Ponesimod-d₇ (ACT-128800-d₇) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d₇ (ACT-128800) is a potent, selective and orally active agonist of *S1P₁, with an IC₅₀* of 6 nM in a radioligand binding assay. Ponesimod-d₇ activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod-d₇ can protect against lymphocyte-mediated tissue inflammation .

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 .

HY-10569S

Ponesimod-d4

Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569) . 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 .

HY-10569S1

Ponesimod-d7

Ponesimod-d₇ (ACT-128800-d₇) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d₇ (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod-d₇ activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod-d₇ can protect against lymphocyte-mediated tissue inflammation .

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