| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
S1PR1 1.03 nM (EC50) S1PR5 8.6 nM (EC50)
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| ln Vitro |
Ozanimod (RPC-1063) hydrochloride exhibits intrinsic activity and potency as S1P receptor modulators for S1P5 across species with [35S]-GTPgS binding. The EC50 values for Human S1P1, Cynomolgus monkey S1P1, Mouse S1P1, Rat S1P1, and Canine S1P1 are 1.03 nM, 1.29 nM, 0.90 nM, 1.02 nM, and 0.61 nM, respectively; for Cynomolgus monkey S1P5, Mouse S1P5, Rat S1P5, and Canine S1P5 are 8.6 nM, 15.9 nM, 957.5 nM, 2032.7 nM, and 1662.0 nM, respectively[1]. By altering the alanine in the mouse sequence, ozanimod hydrochloride recovers the potency with EC50 from 958 nM for mS1P5 to 6.7 nM for mS1P5_A120T, nearly mirroring the EC50 for hS1P5 of 8.6 nM[1]. The binding affinities of ozanimod hydrochloride for hS1P5, mS1P5, and mS1P5 _A120T are 2.0 nM, 59.9 nM, and 5.6 nM, respectively[1]. In addition to having saturation binding for [3H]-A971432 to S1P5D value of 8.75 nM, ozanimod hydrochloride possesses saturation binding of [3H]-ozanimod to hS1P5, and mS1P5_A120T with KD values of 6.56 nM and 7.35 nM, respectively[1].
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| ln Vivo |
Reduced circulating lymphocytes, disease scores, and body weight loss were the outcomes of ozanimod (RPC-1063) hydrochloride (oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days) exposures sufficient to engage S1P1, but not S1P5. Additionally, the spinal cord's levels of inflammation, demyelination, and apoptotic cells were reduced, as was the circulating level of neurofilament light, a marker of neuronal degeneration[1]. During a toxin challenge, ozanimod hydrochloride (oral gavage; 5 mg/kg; once daily) reduced myelin loss and axonal degradation, but it did not promote increased remyelination following intoxication[1]. Mice treated orally with ozanimod hydrochloride (1 or 5 mg/kg for 7 days) exhibit excellent pharmacokinetics[1].
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| Animal Protocol |
Animal/Disease Models: Experimental Autoimmune Encephalomyelitis Model[1]
Doses: 0.05, 0.2, or 1 mg/kg Route of Administration: oral gavage; 0.05, 0.2, or 1 mg/kg; one time/day; for 14 days Experimental Results: Attenuated body weight loss, terminal disease scores were Dramatically attenuated with the 0.2 and 1 mg/kg doses and ALCs were Dramatically decreased in all dose groups. decreased spinal cord inflammation and demyelination, as well as attenuated the number of spinal cord apoptotic cells, and Dramatically decreased the levels of circulating neurofilament light at the top dose of 1 mg/kg. Animal/Disease Models: Cuprizone/Rapamycin Demyelination Model[1] Doses: 5 mg/kg Route of Administration: oral gavage; 5 mg/kg; once-daily Experimental Results: Protected neuronal axons, preventing breakage and ovoid formation in the corpus callosum of CPZ/Rapa treated mice. Dramatically attenuated the extent to which the corpus callosum demonstrated decreased myelin content as visualized by MRI. Did not result in enhanced myelin content. Animal Mode |
| References |
[1]. Julie V Selkirk, et al. Deconstructing the Pharmacological Contribution of Sphingosine-1 Phosphate Receptors to Mouse Models of Multiple Sclerosis Using the Species Selectivity of Ozanimod, a Dual Modulator of Human Sphingosine 1-Phosphate Receptor Subtyp
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| Molecular Formula |
C23H25CLN4O3
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|---|---|
| Molecular Weight |
440.92
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| CAS # |
1618636-37-5
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| Related CAS # |
Ozanimod;1306760-87-1
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| SMILES |
Cl[H].O1C(C2C([H])=C([H])C(=C(C#N)C=2[H])OC([H])(C([H])([H])[H])C([H])([H])[H])=NC(C2C([H])=C([H])C([H])=C3C=2C([H])([H])C([H])([H])[C@]3([H])N([H])C([H])([H])C([H])([H])O[H])=N1
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| Solubility (In Vitro) |
DMSO: 200 mg/mL (453.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (11.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (11.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2680 mL | 11.3399 mL | 22.6799 mL | |
| 5 mM | 0.4536 mL | 2.2680 mL | 4.5360 mL | |
| 10 mM | 0.2268 mL | 1.1340 mL | 2.2680 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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