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Ozanimod

Cat. No. M5244
Ozanimod Structure
Synonym:

RPC1063

Size Price Availability Quantity
2mg USD 80  USD80 In stock
5mg USD 110  USD110 In stock
10mg USD 170  USD170 In stock
25mg USD 355  USD355 In stock
50mg USD 560  USD560 In stock
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Quality Control & Documentation
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 (for reference only)
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.
Chemical Information
Molecular Weight 404.46
Formula C23H24N4O3
CAS Number 1306760-87-1
Solubility (25°C) 71 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Sandborn WJ, et al. N Engl J Med. Ozanimod Induction and Maintenance Treatment for Ulcerative Colitis.

[2] Scott FL, et al. Br J Pharmacol. Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.

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Ozanimod hydrochloride

Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .

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  Catalog
Abmole Inhibitor Catalog




Keywords: Ozanimod, RPC1063 supplier, S1P Receptor, inhibitors, activators


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