| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
S1PR1 0.19 nM (EC50) S1PR5 32.8 nM (EC50)
Sphingosine-1-phosphate receptor 1 (S1PR1) is the primary target, with an EC50 of 0.19 nM. RP101988 also shows activity against S1PR5 (EC50=32.8 nM). It is also a substrate for drug transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). These interactions influence the compound's disposition and bioavailability. |
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| ln Vitro |
RP101988 is a drug transporter substrate for P-gp and breast cancer resistance protein (BCRP)[2].
In vitro, RP101988 functions as a potent S1PR1 agonist, activating receptor-mediated signaling pathways. RP101988 is a drug transporter substrate for P-gp and breast cancer resistance protein (BCRP), indicating involvement in cellular efflux mechanisms. It is the major bioactive metabolite of Ozanimod and contributes to the pharmacological effects of the parent drug. |
| ln Vivo |
As the major active metabolite of Ozanimod, RP101988 contributes significantly to the parent drug"s in vivo efficacy. Following oral administration of Ozanimod, RP101988 circulates in plasma and acts on S1PR1 receptors to modulate lymphocyte trafficking. The metabolite shares similar biological activity with the parent drug and plays a key role in achieving therapeutic effects in autoimmune conditions such as multiple sclerosis and ulcerative colitis.
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| Enzyme Assay |
S1PR1 binding and functional assay protocol: CHO-K1 cells stably expressing human S1PR1 are seeded in 96-well plates and incubated with increasing concentrations of RP101988 (0.001-1000 nM) for 60 min at 37degC. GTPgammaS binding is measured using scintillation proximity assay with [35S]GTPgammaS (0.1 nM) in assay buffer (20 mM HEPES, 100 mM NaCl, 10 mM MgCl2, pH 7.4). Non-specific binding is determined in the presence of 10 uM unlabeled GTPgammaS. EC50 values are calculated using non-linear regression analysis. Each point is measured in duplicate or triplicate.
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| Cell Assay |
Cell-based functional assay protocol: Jurkat T cells (expressing endogenous S1PR1) or S1PR1-transfected HEK293 cells are serum-starved for 4 hours. Cells are treated with RP101988 (0-1000 nM) for 15 min at 37degC. S1PR1 activation is assessed by measuring receptor internalization via flow cytometry using fluorescently labeled anti-S1PR1 antibodies. Alternatively, downstream signaling is evaluated by Western blotting for phosphorylated ERK1/2 (Thr202/Tyr204) and Akt (Ser473). EC50 is calculated by densitometry analysis from dose-response curves.
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| Animal Protocol |
In vivo pharmacokinetic study protocol: Male SD rats (or cynomolgus monkeys) receive RP101988 at 0.1-1 mg/kg via intravenous injection or oral gavage. Blood samples are collected from jugular vein at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose. Plasma is separated and stored at -80degC until LC-MS/MS analysis. PK parameters (Cmax, Tmax, AUC0-∞, t1/2, clearance, volume of distribution) are calculated by non-compartmental analysis using WinNonlin software.
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| ADME/Pharmacokinetics |
Following oral administration of Ozanimod, RP101988 is generated as a major active metabolite. Clinical pharmacokinetic studies show that after repeated oral administration of Ozanimod (1 mg, day 10), RP101988 achieves mean Cmax of 266 pg/mL and AUC0-∞ of 5960 pg·h/mL, with Tmax of 6 hours. The metabolite is transported by P-gp and BCRP and its systemic exposure is consistent with contributing to the overall pharmacological response of Ozanimod therapy.
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| Toxicity/Toxicokinetics |
Toxicity data for RP101988 as a standalone compound are limited. As the major active metabolite of Ozanimod, its toxicity profile is expected to be consistent with the parent drug. Ozanimod has demonstrated an acceptable safety profile in clinical trials with common adverse events including headache, hypertension, and elevated liver enzymes. Careful patient monitoring for bradyarrhythmia, respiratory effects, and infections is required. RP101988 is intended for research use only.
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| References |
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| Additional Infomation |
RP101988 is the principal bioactive metabolite of Ozanimod, an FDA-approved drug for relapsing forms of multiple sclerosis and ulcerative colitis. Its mechanism involves S1PR1 agonism leading to lymphocyte retention in lymph nodes, reducing autoimmune-mediated inflammation. RP101988 is also a substrate for P-gp and BCRP. The compound has not been independently approved as a therapeutic agent but is used in research to understand active metabolite pharmacology.
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| Molecular Formula |
C23H22N4O4
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|---|---|
| Molecular Weight |
418.45
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| CAS # |
2990018-57-8
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| Appearance |
Off-white to light yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~125 mg/mL (~298.72 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3898 mL | 11.9489 mL | 23.8977 mL | |
| 5 mM | 0.4780 mL | 2.3898 mL | 4.7795 mL | |
| 10 mM | 0.2390 mL | 1.1949 mL | 2.3898 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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