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Ozanimod

Cat. No. M5244
Ozanimod Structure
Synonym:

RPC1063

Size Price Availability Quantity
2mg USD 81  USD90 In stock
5mg USD 126  USD140 In stock
10mg USD 207  USD230 In stock
25mg USD 441  USD490 In stock
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Quality Control
Biological Activity

In vitro: In S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation. In vivo: In vivo, Ozanimod shows high oral bioavailability and volume of distribution. In a MOG-induced EAE mouse model, Ozanimod (3 mg/kg, p.o.) suppresses clinical symptoms. In a rat TNBS model of inflammatory bowel disease, Ozanimod (1.2 mg/kg, p.o.) inhibits clinical and histological disease scores. In a Naïve CD4+CD45Rbhi T cell adoptive transfer model, Ozanimod (1.2 mg/kg, p.o.) also significantly reduced disease severity as assessed by measuring the degree of inflammation, gland loss, hyperplasia, neutrophil infiltrate and mucosal thickness.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models MOG-induced EAE model in C57Bl6 mice, TNBS model of inflammatory bowel disease in male Sprague Dawley rats, and Na飗e CD4+CD45Rbhi T cell adoptive transfer model in SCID mice
Formulation 5% DMSO, 5% Tween-20, 90% 0.1N HCl
Dosages 0.1-3 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 404.46
Formula C23H24N4O3
CAS Number 1306760-87-1
Purity 99.86%
Solubility 71 mg/mL in DMSO
Storage at -20°C
References

Ozanimod Induction and Maintenance Treatment for Ulcerative Colitis.
Sandborn WJ, et al. N Engl J Med. 2016 May 5;374(18):1754-62. PMID: 27144850.

Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.
Scott FL, et al. Br J Pharmacol. 2016 Jun;173(11):1778-92. PMID: 26990079.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ozanimod, RPC1063 supplier, S1P Receptor, inhibitors

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