1. GPCR/G Protein
  2. LPL Receptor
  3. Icanbelimod

Icanbelimod  (Synonyms: S1p receptor agonist 1)

Cat. No.: HY-101265 Purity: 99.95%
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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.

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Icanbelimod Chemical Structure

Icanbelimod Chemical Structure

CAS No. : 1514888-56-2

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 176 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

EC50: 9.83 nM (S1P1 internalization)[1]

In Vivo

Icanbelimod (oral administration; 0.01 mg/kg-1 mg/kg) at all dose is active, and only a dose of 0.01 mg/kg is required to observe a decrease in the number of peripheral blood lymphocytes by more than 50% and a decrease in the 1 mg/kg dose. Besides, this compound is lymphocyte-specific, which dose not significantly alter the number of peripheral monocytes and other white blood cells in SD rats[1].
Icanbelimod (oral administration; 3 mg/kg; 12 days) is has been proved to block lymphocyte efflux. In the development of type II collagen-induced arthritis in rat model, compound 2 is effective in inhibiting the development of joint swelling in arthritis and joint structure destruction[1].
Icanbelimod (oral administration; 0.3-1mg/kg; 30 days; once daily) inhibits the development of experimental autoimmune encephalitis (EAE) as a dose-dependent manner in mice model[1].

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

Animal Model: Lewis rats[1]
Dosage: 3 mg/kg
Administration: Oral administration
Result: Decreased the severity score of arthritis in the four-legged rats.
Animal Model: Female C57BL/6 mice[1] 
Dosage: 0.03, 0.1, and 1 mg/kg
Administration: Oral administration
Result: Decreased the severity score of EAE in MOG 35-55 induced mice.
Molecular Weight

409.45

Formula

C23H24FN3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1CN(CC2=CC=C(C3=NOC(C4=CC=C(CC(C)C)C=C4)=N3)C=C2F)C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 6.8 mg/mL (16.61 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4423 mL 12.2115 mL 24.4230 mL
5 mM 0.4885 mL 2.4423 mL 4.8846 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

=
Concentration (final)

C2

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V2

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

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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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4423 mL 12.2115 mL 24.4230 mL 61.0575 mL
5 mM 0.4885 mL 2.4423 mL 4.8846 mL 12.2115 mL
10 mM 0.2442 mL 1.2212 mL 2.4423 mL 6.1058 mL
15 mM 0.1628 mL 0.8141 mL 1.6282 mL 4.0705 mL
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Icanbelimod 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:
Icanbelimod
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HY-101265
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