1. GPCR/G Protein
  2. LPL Receptor
  3. S1P1 agonist 1

S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.

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S1P1 agonist 1 Chemical Structure

S1P1 agonist 1 Chemical Structure

CAS No. : 1220973-37-4

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Based on 1 publication(s) in Google Scholar

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Description

S1P1 Agonist 1 is a S1P1 agonist with immunomodulatory activities.

IC50 & Target

S1P1[1]

In Vitro

S1P1 Agonist 1 binds to S1P1 is internalized and activates intracellular AKT and ERKs cellular signaling pathways. S1P1 Agonist 1 mediated S1P1 downregulation is independent of sphingosine kinase activity indicating it to be a direct agonist of S1P1. S1P1 Agonist 1 decreases cell surface expression of S1P1 in in vitro cell culture model[1].

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

In Vivo

S1P1 Agonist 1 (1.3mg/kg) attenuates EAE disease. EAE is the animal model of multiple sclerosis which is extensively used for investigating clinical studies for multiple sclerosis drugs. S1P1 Agonist 1 treatment reduces peripheral total blood lymphocyte and T lymphocyte counts significantly. The reduction in total lymphocytes and T cells are 48% and 41% in AKP-11 treated animals, respectively. The reduction in the CD4+ and CD8+ T cell populations are 41% and 40% in S1P1 Agonist 1 treated animals, respectively. S1P1 Agonist 1 treatment reduces CNS infiltration of T cells and Cytokines and enhances neuroprotection. S1P1 Agonist 1 treatment has little effect on the heart rate of animals. The decrease in blood pressure is also smaller with S1P1 Agonist 1 treatment as compared animals treated with FTY720[1].

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

Molecular Weight

443.88

Formula

C22H22ClN3O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC(C1=CC2=CC(C3=NOC(C4=CC=C(OCCC)C(Cl)=C4)=N3)=CC=C2O1)(N)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (281.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2529 mL 11.2643 mL 22.5286 mL
5 mM 0.4506 mL 2.2529 mL 4.5057 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

Rats: EAE is induced in female Lewis rats with guinea pig MBP (25 μg/rat). EAE developed rats are divided into 3 groups on day 11 or 12 after immunization and administered vehicle or S1P1 Agonist 1 (3 or 1.3 mg/kg) or FTY720 (1 mg/kg) orally every day until day 26. Rats are administrated orally with 1.3 mg/kg S1P1 Agonist 1, 1 mg/kg FTY720 and vehicle. After post administration, heart rates are measured at 1, 2, 4, 6, 12, and 24 hr[1].

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2529 mL 11.2643 mL 22.5286 mL 56.3215 mL
5 mM 0.4506 mL 2.2529 mL 4.5057 mL 11.2643 mL
10 mM 0.2253 mL 1.1264 mL 2.2529 mL 5.6322 mL
15 mM 0.1502 mL 0.7510 mL 1.5019 mL 3.7548 mL
20 mM 0.1126 mL 0.5632 mL 1.1264 mL 2.8161 mL
25 mM 0.0901 mL 0.4506 mL 0.9011 mL 2.2529 mL
30 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8774 mL
40 mM 0.0563 mL 0.2816 mL 0.5632 mL 1.4080 mL
50 mM 0.0451 mL 0.2253 mL 0.4506 mL 1.1264 mL
60 mM 0.0375 mL 0.1877 mL 0.3755 mL 0.9387 mL
80 mM 0.0282 mL 0.1408 mL 0.2816 mL 0.7040 mL
100 mM 0.0225 mL 0.1126 mL 0.2253 mL 0.5632 mL
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S1P1 agonist 1 Related Classifications

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.

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Product Name:
S1P1 agonist 1
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