Nutrabiotech Ozanimod 98% Powder 1G, 98% high purity Ozanimod powder, selective S1P receptor modulator, lymphocyte trafficking regulator, CNS autoimmune inflammation research raw material

Ozanimod RPC‑1063 CAS 1306760‑87‑1 High‑Purity Powder Selective S1PR1 & S1PR5 Receptor Modulator Immunology Biochemical Reagent

High‑purity Ozanimod powder CAS 1306760‑87‑1, also known as RPC‑1063, is a highly‑selective sphingosine‑1‑phosphate receptor modulator targeting S1PR1 and S1PR5 receptor subtypes. This off‑white crystalline small‑molecule compound triggers receptor internalisation, blocks lymphocyte egress out of lymph nodes and restrains autoreactive immune‑cell migration toward central‑nervous‑system and intestinal‑tissue. It is widely used for laboratory‑scale research on relapsing multiple sclerosis, ulcerative colitis, Crohn’s disease, immune‑mediated‑inflammation and lymphocyte‑trafficking mechanism exploration. Every‑batch undergoes strict HPLC purity inspection, bulk‑order service and customizable‑packaging are available for global immunology and neuropharmacology research‑oriented purchasers.

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Ozanimod (CAS 1306760-87-1) S1P1 / S1P5 Receptor Modulator | RPC1063, Zeposia, Lymphocyte Sequestration

Ozanimod CAS 1306760-87-1
Selective S1P1 / S1P5 Receptor Modulator

Ozanimod (development code RPC1063; marketed as Zeposia) is an orally active, next-generation sphingosine-1-phosphate receptor modulator with an EC50 of approximately 0.41 nM at human S1P1 and 11 nM at S1P5, and minimal activity at S1P2, S1P3 or S1P4. It functions as a functional antagonist: sustained S1P1 internalisation renders lymphocytes blind to the egress gradient, sequestering them in lymph nodes and cutting immune infiltration into the central nervous system and intestinal mucosa. Approved for relapsing multiple sclerosis and moderately to severely active ulcerative colitis.

S1P1 Modulator S1P5 Modulator Functional Antagonist Lymphocyte Sequestration Relapsing MS Research Ulcerative Colitis S1P3-Sparing
Request a Quote Technical Specs
404.46
MW (C23H24N4O3)
0.41 nM
EC50 at human S1P1
≥98%
Purity (HPLC)

Molecular Information

Name: Ozanimod
CAS: 1306760-87-1
Formula: C23H24N4O3
MW: 404.46 g/mol
Purity: ≥98% (HPLC)
SMILES: CC(C)Oc1ccc(-c2nc
  (-c3cccc4c3CC[C@@H]4
  NCCO)no2)cc1C#N
InChIKey: XRVDGNKRPOAQTN
  -FQEVSTJZSA-N
Appearance: White to off-white powder
Solubility: DMSO
Codes: RPC1063 / Zeposia
HCl salt CAS: 1618636-37-5
Storage: -20°C, sealed, desiccated
🧪
CAS Number
1306760-87-1
⚖️
Molecular Weight
404.46
🎯
Primary Targets
S1P1 / S1P5
✅
Purity
≥98%

Ozanimod Technical Specifications & QC Parameters

Complete physicochemical data and quality-control profile for research-grade ozanimod (CAS 1306760-87-1)

📋 Physicochemical Properties

  • Product NameOzanimod
  • IUPAC Name5-[3-[(1S)-1-(2-Hydroxyethylamino)-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile
  • CAS Number1306760-87-1
  • Hydrochloride CAS1618636-37-5
  • SynonymsRPC1063 / Zeposia
  • Molecular FormulaC23H24N4O3
  • Molecular Weight404.46 g/mol
  • SMILESCC(C)Oc1ccc(-c2nc(-c3cccc4c3CC[C@@H]4NCCO)no2)cc1C#N
  • InChIKeyXRVDGNKRPOAQTN-FQEVSTJZSA-N
  • Stereochemistry(S)-configured indane centre
  • AppearanceWhite to off-white powder
  • Chemical Class1,2,4-Oxadiazole indane benzonitrile
  • Active MetabolitesCC112273 / CC1084037

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormCrystalline powder
  • Potency (S1P1)EC50 ≈ 0.41 nM (human)
  • Potency (S1P5)EC50 ≈ 11 nM (human)
  • Receptor SelectivityMinimal activity at S1P2, S1P3, S1P4
  • Functional ClassAgonist-driven functional antagonist (receptor internalisation)
  • SolubilityDMSO; poorly soluble in water
  • Storage Condition-20°C, sealed, desiccated, dark
  • Stock Solution Storage-20°C to -80°C, aliquoted, avoid freeze-thaw
  • QC DocumentationCOA / HPLC / chiral HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human or clinical use

Receptor Target Profile & S1P Subtype Selectivity

Five G-protein-coupled receptors read the sphingosine-1-phosphate signal; ozanimod deliberately engages only the two that govern lymphocyte egress and oligodendrocyte biology

🎯 S1P1 (S1PR1, EDG-1) 🎯 S1P5 (S1PR5, EDG-8) 🚫 S1P2 (spared) 🚫 S1P3 (cardiac-sparing) 🚫 S1P4 (spared) 🧲 Gi/o Coupling 🔄 β-Arrestin Recruitment 🩸 Lymph Node Egress Gradient 🧠 Oligodendrocyte S1P5 🧱 Endothelial Barrier Integrity

Ozanimod Mechanism of Action: Agonism That Behaves Like Antagonism

How persistent S1P1 activation traps lymphocytes in lymph nodes and starves inflamed tissue of autoreactive cells

1

The S1P Egress Gradient

Sphingosine-1-phosphate is abundant in blood and lymph but kept low inside lymphoid tissue by S1P lyase. Lymphocytes sense this gradient through surface S1P1 and use it as the directional cue to exit lymph nodes into the circulation.

2

High-Affinity S1P1 Engagement

Ozanimod binds S1P1 as a full agonist with an EC50 of about 0.41 nM, triggering Gi/o signalling and β-arrestin recruitment. Its selectivity for S1P1 and S1P5 leaves S1P3-mediated cardiac and vascular effects largely untouched.

3

Receptor Internalisation & Degradation

Unlike the natural ligand, which allows rapid recycling, ozanimod drives sustained β-arrestin-dependent internalisation, ubiquitination and proteasomal degradation of S1P1 — converting an agonist into a durable functional antagonist.

4

Lymphocyte Sequestration

Without surface S1P1, the lymphocyte cannot read the egress gradient and remains trapped in the lymph node. Circulating naive and central memory T and B cells fall by roughly 50-65%, while effector memory and tissue-resident immunity is comparatively preserved.

5

Reduced Tissue Infiltration

With fewer autoreactive lymphocytes in circulation, trafficking across the blood-brain barrier into CNS lesions and into inflamed colonic mucosa falls. This is the shared basis of efficacy in relapsing multiple sclerosis and in ulcerative colitis.

6

Central S1P5 Component

S1P5 is expressed on oligodendrocytes, oligodendrocyte precursors and astrocytes. Because ozanimod and its major active metabolite CC112273 are CNS-penetrant, a direct glial contribution to remyelination and neuroprotection is an active research question.

Research Applications of the S1P1/S1P5 Modulator Ozanimod

A best-in-class chemical tool for lymphocyte trafficking, autoimmune inflammation and sphingolipid GPCR pharmacology

🧠

Relapsing-Remitting Multiple Sclerosis

The RADIANCE and SUNBEAM phase 3 programmes established ozanimod against interferon beta-1a on annualised relapse rate and MRI lesion burden. In the laboratory it is the reference S1P modulator in experimental autoimmune encephalomyelitis, cuprizone demyelination and blood-brain-barrier trafficking models.

Neuroimmunology
🩺

Ulcerative Colitis & IBD

TOUCHSTONE and the pivotal TRUE NORTH trial demonstrated induction and maintenance of clinical remission in moderately to severely active ulcerative colitis. Widely used in DSS colitis, T-cell transfer colitis and mucosal-healing studies as an oral alternative to anti-integrin biologics.

Gastroenterology
🔬

S1P Receptor Pharmacology & GPCR Biology

An essential selectivity benchmark in S1P1-S1P5 panels: GTPγS binding, cAMP inhibition, β-arrestin recruitment (PathHunter/Tango), receptor internalisation imaging and BRET-based conformational assays. Frequently paired with fingolimod-phosphate and siponimod as comparators.

Receptor Pharmacology
🚦

Lymphocyte Trafficking & Egress

Used to acutely and reversibly block lymph node egress in vivo, allowing researchers to separate the contribution of newly recruited circulating lymphocytes from that of tissue-resident populations in infection, transplantation and tumour immunology models.

Immune Cell Trafficking
🧬

Crohn's Disease & Mucosal Immunology

Explored beyond ulcerative colitis into Crohn's disease and other mucosal inflammatory conditions, where reducing lymphocyte recruitment to the gut wall is the therapeutic goal. Useful for studying gut-homing integrin biology and epithelial barrier restoration.

Mucosal Immunity
🫀

Vascular Barrier & Cardiac Safety Pharmacology

S1P1 maintains endothelial adherens junctions while S1P3 mediates bradycardia. Ozanimod's S1P3-sparing profile makes it the standard tool for dissecting which S1P subtype drives which vascular or cardiac phenotype in safety pharmacology research.

Safety Pharmacology
🧫

Remyelination & Oligodendrocyte Biology

Because S1P5 is expressed on oligodendrocyte lineage cells and ozanimod is CNS-penetrant, it is applied in oligodendrocyte precursor differentiation assays, myelin sheath formation co-cultures and neuroprotection paradigms.

Glial Biology
💊

Metabolism, DDI & Active-Metabolite Research

Ozanimod is a rich case study in complex metabolism: alcohol/aldehyde dehydrogenases, MAO-B, CYP3A4 and gut microflora generate the major circulating active metabolites CC112273 and CC1084037, with CC112273 cleared by CYP2C8 — the basis of its rifampin, gemfibrozil and MAO-inhibitor interactions.

DMPK / ADME
🛡️

Broader Autoimmune & Inflammatory Models

Applied across psoriasis, rheumatoid arthritis, lupus, graft-versus-host disease, transplant rejection and acute lung injury models where lymphocyte egress blockade or endothelial barrier stabilisation is the mechanistic hypothesis under test.

Autoimmunity

Key Publications on Ozanimod (RPC1063)

Discovery pharmacology and the pivotal multiple sclerosis and ulcerative colitis trials

Scott FL, Clemons B, Brooks J, et al. Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1) and receptor-5 (S1P5) agonist with autoimmune disease-modifying activity. British Journal of Pharmacology. 2016;173(11):1778-1792. [Discovery pharmacology]
doi: 10.1111/bph.13476
Comi G, Kappos L, Selmaj KW, et al. Safety and efficacy of ozanimod versus interferon beta-1a in relapsing multiple sclerosis (SUNBEAM): a multicentre, randomised, minimum 12-month, phase 3 trial. Lancet Neurology. 2019;18(11):1009-1020.
doi: 10.1016/S1474-4422(19)30239-X
Cohen JA, Comi G, Selmaj KW, et al. Safety and efficacy of ozanimod versus interferon beta-1a in relapsing multiple sclerosis (RADIANCE): a multicentre, randomised, 24-month, phase 3 trial. Lancet Neurology. 2019;18(11):1021-1033.
doi: 10.1016/S1474-4422(19)30238-8
Sandborn WJ, Feagan BG, D'Haens G, et al. Ozanimod as induction and maintenance therapy for ulcerative colitis (TRUE NORTH). New England Journal of Medicine. 2021;385(14):1280-1291. [Pivotal UC trial]
doi: 10.1056/NEJMoa2033617
Sandborn WJ, Feagan BG, Wolf DC, et al. Ozanimod induction and maintenance treatment for ulcerative colitis (TOUCHSTONE). New England Journal of Medicine. 2016;374(18):1754-1762.
doi: 10.1056/NEJMoa1513248
Cohen JA, Arnold DL, Comi G, et al. Safety and efficacy of the selective sphingosine 1-phosphate receptor modulator ozanimod in relapsing multiple sclerosis (RADIANCE): a randomised, placebo-controlled, phase 2 trial. Lancet Neurology. 2016;15(4):373-381.
doi: 10.1016/S1474-4422(16)00018-1

Ozanimod Pack Sizes & Ordering Information

Research-grade ozanimod (CAS 1306760-87-1) supplied with full QC documentation — available in 1g / 5g / 10g / 100g / 1KG

TierPack SizeStock StatusTypical Use CaseShipping Notes
Standard1 gIn StockS1P receptor panels, β-arrestin and internalisation assays, EC50 determinationSame/next-day dispatch; amber vial with desiccant
Medium5 gIn StockEAE and DSS colitis cohorts, lymphocyte-count pharmacodynamic studiesSame/next-day dispatch; sealed foil pouch, ambient shipping
Large10 gIn StockChronic in vivo dosing, PK/PD and active-metabolite profiling, multi-site studies1-2 business days; double-sealed, light-protected
Bulk100 gIn StockFormulation development, salt-form and polymorph screening, analytical standardsQuote to confirm; HDPE container, cool-chain option available
Industrial1 KGMade to orderPilot-scale campaigns, CRO/CMO supply agreements, chiral process developmentBatch delivery on campaign schedule; per-lot COA, chiral purity and export documents

💡 Reference pack sizes shown above; for current pricing, lot availability and bulk ozanimod quotations please contact us for a quote. Tiered discounts apply to 100 g and 1 KG orders.

Ozanimod Frequently Asked Questions (FAQ)

What is ozanimod (CAS 1306760-87-1)?
Ozanimod, development code RPC1063 and marketed as Zeposia, is an orally active small molecule that selectively modulates sphingosine-1-phosphate receptors 1 and 5. Molecular formula C23H24N4O3, molecular weight 404.46 g/mol. It activates human S1P1 with an EC50 of about 0.41 nM and S1P5 at about 11 nM, with minimal activity at S1P2, S1P3 and S1P4. It is approved for relapsing forms of multiple sclerosis and for moderately to severely active ulcerative colitis.
How does the S1P1 mechanism actually work?
Lymphocytes exit lymph nodes by following a sphingosine-1-phosphate gradient that is high in blood and lymph and low in lymphoid tissue, sensed through surface S1P1. Ozanimod binds S1P1 as an agonist but, unlike the endogenous ligand, drives sustained β-arrestin-dependent internalisation, ubiquitination and degradation of the receptor. The lymphocyte loses its compass, cannot egress, and remains sequestered in the lymph node. Circulating naive and central memory T and B cells drop by roughly 50-65%. This is why S1P1 modulators are called functional antagonists even though they are pharmacological agonists.
How does ozanimod differ from fingolimod?
Fingolimod is a sphingosine analogue prodrug that must be phosphorylated by sphingosine kinase 2, after which it engages S1P1, S1P3, S1P4 and S1P5. Its S1P3 activity is linked to first-dose bradycardia and AV block. Ozanimod is selective for S1P1 and S1P5 and largely spares S1P3, which is why it uses a 7-day dose-escalation regimen instead of routine first-dose cardiac monitoring. Ozanimod also has a shorter functional washout, so lymphocyte counts recover more quickly after discontinuation — a practical advantage in study design.
How does ozanimod compare with siponimod and ponesimod?
All three are second-generation, subtype-selective S1P modulators developed to avoid fingolimod's S1P3 liability. Siponimod targets S1P1/S1P5 and is cleared largely by CYP2C9, so genotyping is required before dosing. Ponesimod is S1P1-selective with a very short half-life and rapid lymphocyte recovery. Ozanimod is S1P1/S1P5-selective, is not CYP2C9-dependent, and is unique in having major long-lived active metabolites (CC112273, CC1084037) that carry most of the systemic exposure.
How is ozanimod metabolised, and which drug interactions matter?
Ozanimod is extensively metabolised through alcohol and aldehyde dehydrogenases, monoamine oxidase B, CYP3A4 and gut microflora, generating the major active metabolite CC112273 plus CC1084037; these metabolites account for most circulating activity. CC112273 is cleared predominantly by CYP2C8. Consequently strong CYP2C8 inducers such as rifampin sharply reduce active metabolite exposure, CYP2C8 inhibitors such as gemfibrozil increase it, and co-administration of monoamine oxidase inhibitors is contraindicated. Note that ozanimod is not a CYP2C9 or CYP1A2 driven drug — that pattern belongs to siponimod and to other agent classes.
Why does the same drug work in multiple sclerosis and in ulcerative colitis?
Both diseases depend on the continuous recruitment of circulating autoreactive lymphocytes into a target tissue — the CNS in MS and the colonic mucosa in ulcerative colitis. Sequestering those cells in secondary lymphoid organs starves both tissues of new inflammatory infiltrate, so a single trafficking-directed mechanism serves both indications. The S1P5 arm adds a CNS-specific dimension via oligodendrocyte and astrocyte expression, which is relevant to MS but not to UC.
Is ozanimod CNS-penetrant?
Yes. Ozanimod and its major active metabolite CC112273 distribute into the central nervous system, which is mechanistically important because S1P5 is expressed on oligodendrocytes, oligodendrocyte precursor cells and astrocytes. Whether direct glial S1P5 engagement contributes to remyelination and neuroprotection over and above peripheral lymphocyte sequestration remains an active and interesting research question, and is one reason the compound is popular in demyelination models.
What assays is ozanimod suitable for?
It performs well as a reference agonist/modulator in: GTPγS binding and cAMP inhibition assays on recombinant S1P1-S1P5; β-arrestin recruitment platforms such as PathHunter and Tango; receptor internalisation imaging using tagged S1P1 constructs; flow-cytometric lymphocyte-count pharmacodynamics in whole blood; and in vivo EAE, cuprizone and DSS colitis models. It is commonly benchmarked side by side with fingolimod-phosphate, siponimod and the endogenous ligand S1P.
How should ozanimod be prepared and stored?
Prepare concentrated stocks in DMSO; aqueous solubility is poor. Dilute into buffer or medium immediately before use and keep final DMSO ≤0.1% v/v for cell work. The molecule contains a chiral (S)-indane centre and a secondary amine, so avoid strongly acidic or basic conditions and prolonged heating that could risk epimerisation or degradation. Store the solid at -20 °C, sealed, desiccated and protected from light; store DMSO stocks aliquoted at -20 °C or -80 °C and avoid repeated freeze-thaw cycles.
What QC documentation is supplied, and are bulk quantities available?
Every lot ships with a Certificate of Analysis (COA) reporting HPLC purity (≥98%), chiral purity for the (S)-enantiomer, 1H NMR structural confirmation and MS identity data. MSDS/SDS, residual-solvent data and Certificates of Origin are available on request. Pack sizes run 1 g, 5 g, 10 g, 100 g and 1 KG, with the 1 KG tier manufactured to order on a campaign basis; hydrochloride salt conversion can be discussed for bulk programmes. For custom specifications or repeat-supply agreements please contact our technical sales team.

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