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  3. Ozanimod

Ozanimod  (Synonyms: RPC-1063)

Cat. No.: HY-12288 Purity: 99.83%
COA Handling Instructions

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

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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10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
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25 mg USD 370 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

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

IC50 & Target

S1PR1

1.03 nM (EC50)

S1PR5

8.6 nM (EC50)

In Vitro

Ozanimod (RPC-1063) has potency and intrinsic activity of S1P receptor modulators for S1P5 across species with [35S]-GTPgS binding, and the EC50 values of 1.03 nM, 1.29 nM, 0.90 nM, 1.02 nM and 0.61 nM for Human S1P1, Cynomolgus monkey S1P1, Mouse S1P1, Rat S1P1 and Canine S1P1, respectively; and the EC50 values of 8.6 nM, 15.9 nM, 957.5 nM, 2032.7 nM and 1662.0 nM for Human S1P5, Cynomolgus monkey S1P5, Mouse S1P5, Rat S1P5 and Canine S1P5, respectively[1].
Ozanimod restores the potency with EC50 from 958 nM for mS1P5 to 6.7 nM for mS1P5_A120T to closely mirror the EC50 for hS1P5 of 8.6 nM by mutating the alanine in the mouse sequence[1].
Ozanimod has binding affinity with Ki values of 2.0 nM, 59.9 nM and 5.6 nM for hS1P5, mS1P5 and mS1P5 _A120T, respectively[1].
Ozanimod has saturation binding of [3H]-ozanimod to hS1P5, and mS1P5_A120T with KD values of 6.56 nM, 7.35 nM, respectively and also has saturation binding for [3H]-A971432 to S1P5D value of 8.75 nM[1].

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

In Vivo

Ozanimod (RPC-1063) (oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days) exposures sufficient to engage S1P1, but not S1P5, resulted in reduced circulating lymphocytes, disease scores, and body weight loss; reduced inflammation, demyelination, and apoptotic cell counts in the spinal cord; and reduced circulating levels of the neuronal degeneration marker, neurofilament light[1].
Ozanimod (oral gavage; 5 mg/kg; once-daily) prevented axonal degradation and myelin loss during toxin challenge but did not facilitate enhanced remyelination after intoxication[1].
Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice[1].

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

Animal Model: Experimental Autoimmune Encephalomyelitis Model[1]
Dosage: 0.05, 0.2, or 1 mg/kg
Administration: oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days
Result: Attenuated body weight loss, terminal disease scores were significantly attenuated with the 0.2 and 1 mg/kg doses and ALCs were significantly reduced in all dose groups.
Reduced spinal cord inflammation and demyelination, as well as attenuated the number of spinal cord apoptotic cells, and significantly reduced the levels of circulating neurofilament light at the top dose of 1 mg/kg.
Animal Model: Cuprizone/Rapamycin Demyelination Model[1]
Dosage: 5 mg/kg
Administration: oral gavage; 5 mg/kg; once-daily
Result: Protected neuronal axons, preventing breakage and ovoid formation in the corpus callosum of CPZ/Rapa treated mice.
Significantly attenuated the extent to which the corpus callosum demonstrated reduced myelin content as visualized by MRI.
Did not result in enhanced myelin content.
Animal Model: C57BL/6J mice[1]
Dosage: 1 or 5 mg/kg
Administration: oral, 1 or 5 mg/kg, for 7 days
Result:
Dose Terminal body weight % versus day 1 Spinal cord inflammation Foci per 20 cells Spinal cord demyelination Score 0–5 Spinal cord apoptotic cells Count per section Plasma NfL pg/ml
Vehicle (5% DMSO, 5%Tween 20, 90% water) 86.4 ± 3.2 8.50 ± 1.21 2.00 ± 0.15 2.25 ± 0.53 4.37 ± 0.89
Ozanimod (0.05 mg/kg) 85.8 ± 2.7 5.00 ± 1.03* 0.91 ± 0.21*** 1.08 ± 0.23* 3.53 ± 0.46
Ozanimod (0.2 mg/kg) 95.7 ± 3.1* 3.54 ± 0.49*** 0.73 ± 0.14 *** 0.91 ± 0.28* 2.62 ± 0.46
Ozanimod (1 mg/kg) 102.8 ± 1.8* 2.67 ± 0.56*** 0.33 ± 0.14 *** 0.60 ± 0.19** 1.91 ± 0.34**
Clinical Trial
Molecular Weight

404.46

Formula

C23H24N4O3

CAS No.
SMILES

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

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 available by MCE.
Purity & Documentation

Purity: 99.83%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ozanimod
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