2. GPCR/G Protein
  3. LPL Receptor
  4. S1P1 agonist 7

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.

For research use only. We do not sell to patients.

S1P1 agonist 7

S1P1 agonist 7 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

S1P1 agonist 7 Related Antibodies

Top Publications Citing Use of Products

View All LPL Receptor Isoform Specific Products:

View All Isoforms
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

In Vitro

S1P1 agonist 7 (compound 28) shows a 4.51-fold β-arrestin bias relative to Fingolimod (HY-11063) in docking studies, with an EC50 values of 12.7 nM for G-protein signaling and 3.23 nM for β-arrestin recruitment[1].
S1P1 agonist 7 (1-10 µM, 15-60 min) displays high stability across all microsomal species (human, rat, and mouse), and shows no significant inhibition against most CYP isozymes at 10 µM[1].
S1P1 agonist 7 (serial dilution starting from 100 μM, 90 min) demonstrates high selectivity for S1P1 in Chem-4/G₁₅ and CHO-K1 EDG1 cells, exhibiting EC50 values of 0.014 μM in G-protein signaling and 0.0023 μM in β-arrestin recruitment, with only low additional activity at S1P₅[1].
S1P1 agonist 7 (0.041-10 μM, 2 min) does not induce any observable changes in peak frequency or beat rate, even at the highest tested concentrations in human induced pluripotent stem cells (iPSC)-derived cardiomyocytes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

S1P1 agonist 7 Related Antibodies
In Vivo

S1P1 agonist 7 (1, 3, and 10 mg/kg, i.g., single dose) reduces peripheral blood lymphocyte count (PLC) in C57BL/6N mice[1].
S1P1 agonist 7 (10 mg/kg, i.g., daily for 23 days) confers robust protection against EAE in MOG35−55 (HY-P1240) induced EAE mice, moderating its onset, progression, and associated pathological damage[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6N mice (8 weeks old) immunized with MOG/CFA emulsion and received PTX on two consecutive days to induce EAE[1]
Dosage: 10 mg/kg
Administration: i.g., daily for 23 days
Result: Delayed disease onset and reduced symptom severity, as indicated by lower cumulative and mean maximum clinical scores.
Maintained its prophylactic effect until the peak of disease severity, which occurred around 17 dpi.
Prevented body weight loss and lowered disease incidence in EAE mice, indicating a protective effect.
Moderated disease progression, and led to a steady reduction in symptom severity until 34 dpi, demonstrating a moderate therapeutic effect comparable to that of Siponimod (HY-12355).
Significantly reduced the cumulative clinical score from 19 dpi (the peak of EAE) to 34 dpi.
Prevented body weight loss compared to the vehicle-treated group.
Markedly reduced demyelination in the spinal cord's dorsal column and ventral white matter.
Reduced immune cell infiltration and partially preserved myelin integrity.
Animal Model: Female C57BL/6N mice (8 weeks old)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: i.g., single dose
Result: Reduced PLC to 24.4 % of baseline at 4 h post administration, outperforming Fingolimod (36.3 %).
Promoted a rapid recovery of PLCs to 70.8 % of baseline within 28 hours, in contrast to Fingolimod (HY-11063), which causes prolonged lymphopenia.
Produced a rapid reduction in lymphocyte counts to approximately 40 % of baseline at 3 h post administration and achieved maximal suppression at the 3 and 10 mg/kg doses by 6 h post administration, while triggering an early rebound in the 1 mg/kg group by the same time, suggesting the onset of recovery.
Elicited a stronger pharmacodynamic response at 3 and 10 mg/kg, and permitted full lymphocyte recovery in all groups within 24 hours.
Molecular Weight

406.43

Formula

C23H22N2O5
SMILES

O=C(O)CCC(N1C=CC2=C1C=CC(OCC3=CC=C(OC(C)C)C(C#N)=C3)=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

S1P1 agonist 7 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

S1P1 agonist 7LPL ReceptorLysophospholipid Receptorβ-arrestin-biasedS1P1immunomodulatory activitymetabolic stabilityCYP inhibitionEAE mouse modelMSiPSC-derived cardiomyocytesmicrosomalPLCInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
S1P1 agonist 7
Cat. No.:
HY-175984
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.