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  2. LPL Receptor
  3. Ozanimod

Ozanimod (Synonyms: RPC-1063)

Cat. No.: HY-12288 Purity: 99.81%
Handling Instructions

Ozanimod (RPC-1063) is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410 pM and 11 nM in [35S]-GTPγS binding, respectively.

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

Ozanimod Chemical Structure

Ozanimod Chemical Structure

CAS No. : 1306760-87-1

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Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 158 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 144 In-stock
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10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
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100 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Ozanimod (RPC-1063) is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410 pM and 11 nM in [35S]-GTPγS binding, respectively.

IC50 & Target

EC50: 410±160 pM (S1P1 receptor), 11±4.3 nM (S1P5 receptor)[1]

In Vitro

Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1) and receptor-5 (S1P5) agonist. The EC50 values are subnanomolar for S1P1 receptors whether measuring inhibition of cAMP generation (160±60 pM) or [35S]-GTPγS binding (410±160 pM). The EC50 value for S1P5 receptor whether measuring inhibition [35S]-GTPγS binding (11±4.3 nM). Ozanimod demonstrates agonist activity at the S1P5 receptor [11±4.3 nM and 83% Emax (percentage of maximum stimulation)]. To determine whether Ozanimod induces sustained S1P1 receptor internalization, S1P1 receptor-HEK293T cells are incubated with different doses of Ozanimod in the presence of 10 μM cycloheximide to prevent translation of new S1P1 receptor protein. Cells are analysed after 1 h treatment, or, after the 1 h treatment washed thoroughly to remove Ozanimod and incubated with 1 μM Cycloheximide for a further 24 h. After a 1 h treatment Ozanimod induces significant loss of S1P1 receptor cell surface expression, similar in magnitude and potency to that seen with FTY720-P-treated cells. Following 1 h of treatment and a 24 h washout period, Ozanimod demonstrates a dose-dependent effect on S1P1 receptor re-expression on the cell surface, with near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM[1].

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

In Vivo

Ozanimod (RPC1063) is specific for S1P1 and S1P5 receptors, induces S1P1 receptor internalization and induces a reversible reduction in circulating B and CCR7+ T lymphocytes in vivo. Ozanimod shows high oral bioavailability and volume of distribution, and a circulatory half-life that supports once daily dosing. Oral Ozanimod reduces inflammation and disease parameters in all three autoimmune disease models[1].

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

Clinical Trial
Molecular Weight

404.46

Formula

C₂₃H₂₄N₄O₃

CAS No.
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 : ≥ 29 mg/mL (71.70 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4724 mL 12.3622 mL 24.7243 mL
5 mM 0.4945 mL 2.4724 mL 4.9449 mL
10 mM 0.2472 mL 1.2362 mL 2.4724 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Representative histograms of transfected HEK293T cells expressing S1P1 receptors incubated with vehicle control or 1 μM RPC1063. HEK293T cells are incubated with increasing doses of Ozanimod (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM and 10 μM) for 1 h, or for 1 h followed by extensive washing to remove compound, then a 24 h recovery period and cell surface receptor expression is monitored[1].

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

Animal Administration
[1]

Mice[1]
Female C57BL/6 mice (60 total, 10 weeks of age) are immunized with Myelin Oligodendrocyte Glycoproteins (MOG) 35-55 peptide with complete Freund's adjuvant on day 0, and pertussis toxin is administered 2 h and 24 h later. At the first instance of clinical symptoms of EAE (limp tail), mice are randomized into treatment groups (n=10 per group) and administered the test compound, p.o., once daily for 14 days. Mice that develop disease earlier than 9 days post-immunization are not enrolled, as these often develop fulminant disease that does not respond to therapy. Test compounds are 0.2 and 0.6 mg/kg Ozanimod, 3 mg/kg FTY720 or vehicle (5% DMSO, 5% Tween-20, 90% 0.1 N HCl). Animals are monitored daily for body weight and clinical symptoms and scored

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

References

Purity: 99.81%

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