Ozanimod (RPC-1063)

Ozanimod (RPC-1063)

$80.00$550.00

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$80.00$550.00

RPC-1063 (CAS No.: 11306760-87-1), a Potent and Selective S1P1 and S1P5 Receptor Agonist with EC50s of 410 pM and 11 nM in [35S]-GTPγS Binding, Respectively. >98% Purity.

Synonyms: Ozanimod, RPC1063, sphingosine-1-phosphate receptor subtypes 1, sphingosine-1-phosphate receptor subtypes 5, S1P1, S1P5

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Description

APIM050408: Ozanimod (RPC-1063) is an oral agonist of the sphingosine-1-phosphate receptor subtypes 1 (S1P1) and 5 (S1P5) that induces peripheral lymphocyte sequestration.

CAS No.: 11306760-87-1
IUPAC/Chemical Name: (S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile
Molecular Formula: C23H24N4O3
Molecular Weight: 404.46
Purity: >98% Purity
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report
Solubility: Soluble in DMSO
Storage: Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Note: Please contact us for COA, Spectra, and SDS information.

Background Information:

Ozanimod (RPC-1063) (CAS No. 11306760-87-1) is a once-daily sphingosine 1-phosphate receptor modulator for the treatment of relapsing Multiple Sclerosis (MS) and inflammatory bowel disease. It was developed by Celgene (now acquired by Bristol-Myers Squibb) and was approved by the FDA on March 26, 2020. In November 2021, ozanimod was also approved by the European Commission for the treatment of adults with relapsing remitting multiple sclerosis.

MS is a devastating inflammatory disease that often progresses and causes severe neurological, physical, and cognitive effects. Inflammatory bowel disease also a chronic inflammatory condition and can cause persistent abdominal pain, diarrhea, bloody stools, and vomiting.

In clinical trials, Ozanimod has been shown to be well-tolerated and has resulted in a higher decrease in the rate of MS relapses than with intramuscular interferon beta-1a, a current standard in MS therapy. Studies involving patients with inflammatory bowel disease have also shown promising results.

Target: S1P5 receptor, S1P1 receptor

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

In Vitro: Ozanimod (RPC-1063) (CAS No. 11306760-87-1) 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 (RPC-1063) 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]

What is the solubility of Ozanimod (RPC-1063) in vitro?
DMSO: > 29 mg/mL

What is the solubility of Omaveloxolone (RTA-408) in vivo?
1. DMSO, PEG300, Tween-80, and saline
Please add 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline in order, solubility ≥ 2.5 mg/mL.
2. DMSO and corn oil
Please add 10% DMSO and 90% corn oil in order, solubility ≥ 2.5 mg/mL.

Reference:
[1]. Scott, F. L. et al. “Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity”, Br. J. Pharmacol., 2016, 173, 1778-1792
[2]. Sandborn, W. J. et al. “Ozanimod Induction and Maintenance Treatment for Ulcerative Colitis”, N. Engl. J. Med. 2016, 374, 1754-1762
[3]. Timony, G. et al. “Pharmacokinetics and Pharmacodynamics of RPC1063 and Its Metabolites in Healthy Adult Volunteers (P1.211)”, Neurology 2014, 82, P1.211
[4]. Meadows, K. R. T. et al. “Ozanimod (RPC1063), a selective S1PR1 and S1PR5 modulator, reduces chronic inflammation and alleviates kidney pathology in murine systemic lupus erythematosus”, Plos ONE 2018, 13, e0193236.

Frequent questions related to “Ozanimod (RPC-1063) (CAS No. 11306760-87-1), a Potent and Selective S1P1 and S1P5 Receptor Agonist”:

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