1. GPCR/G Protein
  2. LPL Receptor

Ozanimod (Synonyms: RPC-1063)

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

Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
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Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
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10 mg USD 228 In-stock
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25 mg USD 420 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
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100 mg USD 1020 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 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].

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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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.
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]

Ozanimod is preprared in vehicle (5% DMSO, 5% Tween-20, 90% 0.1 N HCl)[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. At the end of the study, mice are anaesthetized via inhalation of isoflurane bubbled with oxygen at 10-20 kPa, blood drawn via cardiac puncture to exsanguination and analysed by a veterinary haemoanalyser.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

404.46

Formula

C₂₃H₂₄N₄O₃

CAS No.

1306760-87-1

SMILES

N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[[email protected]@H]4NCCO)=NO2)=CC=C1OC(C)C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 29 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.81%

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Product Name:
Ozanimod
Cat. No.:
HY-12288
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