Nutrabiotech Teriflunomide 99% 1G Powder, 99% high purity Teriflunomide powder, DHODH inhibitor compound, neuroinflammation regulation raw material, CNS remyelination research powder

98% nutrabiotech powder teriflunomide CAS 108605-62-5

High-purity Teriflunomide powder CAS 108605-62-5, a key pyrimidine synthesis inhibitor and immunomodulatory compound. Widely applied in biochemical research, pharmaceutical raw material development and immunology study. Premium pure Teriflunomide with stable molecular activity and reliable quality for lab and bulk supply.

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Teriflunomide (CAS 108605-62-5) DHODH Inhibitor | FDA-Approved MS Therapy, Leflunomide Metabolite

Teriflunomide CAS 108605-62-5
DHODH Inhibitor & Approved MS Therapy

The pharmacologically active metabolite of leflunomide (A77 1726). Teriflunomide is a reversible inhibitor of dihydroorotate dehydrogenase (DHODH, IC50 262 nM) that blocks de novo pyrimidine synthesis in proliferating lymphocytes. It is FDA-approved (2012, brand Aubagio, Sanofi) for relapsing forms of multiple sclerosis, and at higher concentrations additionally inhibits NF-κB and tyrosine kinases. A validated immunomodulatory tool compound for MS, rheumatology, and antiviral research.

DHODH Inhibitor FDA-Approved (2012) Multiple Sclerosis Immunomodulator Pyrimidine Synthesis NF-κB Inhibitor Leflunomide Metabolite
Request a Quote Technical Specs
270.21
MW (C12H9F3N2O2)
262 nM
DHODH IC50
≥98%
Purity (HPLC)

Molecular Information

Name: Teriflunomide
CAS: 108605-62-5
Formula: C12H9F3N2O2
MW: 270.21 g/mol
SMILES: C/C(O)=C(/C#N)C(=O)
  NC1=CC=C(C=C1)C(F)(F)F
InChIKey: UTNUDOFZCWSZMS
  -YFHOEESVSA-N
MP: ~127-129°C (monohydrate)
Appearance: White to almost white powder
Synonyms: A77 1726 / HMR1726 / Aubagio
Storage: -20°C, dry, dark
🧪
CAS Number
108605-62-5
⚖️
Molecular Weight
270.21
🎯
Primary Activity
DHODH Inhibitor
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for Teriflunomide (CAS 108605-62-5)

📋 Physicochemical Properties

  • Product NameTeriflunomide
  • IUPAC Name(Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide
  • CAS Number108605-62-5
  • Code NamesA77 1726 / HMR1726
  • Molecular FormulaC12H9F3N2O2
  • Molecular Weight270.21 g/mol
  • SMILESC/C(O)=C(/C#N)C(=O)NC1=CC=C(C=C1)C(F)(F)F
  • InChIKeyUTNUDOFZCWSZMS-YFHOEESVSA-N
  • Melting Point~127-129°C (monohydrate)
  • BCS ClassII (low sol., high perm.)
  • Brand NameAubagio (Sanofi)
  • PubChem CID10155739

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormPowder
  • ColorWhite to almost white
  • Storage Condition-20°C, dry, dark
  • Protein Binding>99%
  • Half-life18-19 days
  • SolubilityDMSO ~32 mg/mL, ethanol 1 mg/mL; practically insoluble in water
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Pathway Profile

Teriflunomide's trifluoromethylphenyl scaffold targets pyrimidine biosynthesis and downstream immune and inflammatory signaling

🧬 DHODH (IC50 262 nM) 🛡️ NF-κB ⚡ Tyrosine Kinases 🧫 Pyrimidine Synthesis 🩸 Lymphocyte Proliferation 🔥 Mitochondrial ETC 🧠 CNS Immune 💊 Immunomodulation 🦠 Antiviral (research) 🦴 Osteoclast Regulation

How Teriflunomide Works: DHODH-Driven Immunomodulation

Teriflunomide acts through a coordinated sequence from pyrimidine blockade to selective lymphocyte suppression

1

Reversible DHODH Inhibition

Teriflunomide (IC50 262 nM) binds and reversibly inhibits dihydroorotate dehydrogenase, the fourth enzyme of de novo pyrimidine biosynthesis and a component of the mitochondrial electron transport chain, halting orotate-to-uridine conversion.

2

Pyrimidine Depletion

Blocked DHODH depletes pyrimidine nucleotide pools (UTP/dTTP) required for rapid DNA and RNA synthesis. Because replicating cells need de novo pyrimidines, proliferating lymphocytes are selectively starved of building blocks.

3

Selective Lymphocyte Suppression

Activated T and B cells — which depend heavily on de novo pyrimidine synthesis — are preferentially inhibited, dampening autoimmune and inflammatory responses. At higher concentrations, NF-κB and tyrosine-kinase pathways are also inhibited.

Research Applications & Disease Models

Teriflunomide's dual immunomodulatory and antiviral profile spans neurology, rheumatology, oncology and infectious disease

🧠

Multiple Sclerosis

FDA/EMA-approved disease-modifying therapy for relapsing forms of MS (brand Aubagio). The pivotal TEMSO Phase III trial showed reduced annualized relapse rate and slowed lesion accrual and brain-volume loss versus placebo.

TEMSO Phase III
🧬

DHODH Biology

A gold-standard reversible inhibitor of dihydroorotate dehydrogenase, widely used as a chemical probe to study the pyrimidine biosynthesis pathway, mitochondrial electron transport, and nucleotide-dependent proliferation.

Pathway Tool
🛡️

Immunomodulation

Selectively inhibits the proliferation of activated lymphocytes via pyrimidine depletion, making it a model compound for studying autoimmune regulation, tolerogenic signaling, and lymphocytic suppression mechanisms.

Lymphocyte
🦠

COVID-19 & Antiviral Research

DHODH inhibitors are investigated as host-targeted antiviral and anti-inflammatory agents. By limiting pyrimidine-dependent viral replication and cytokine storm, teriflunomide is explored in viral-infection models.

Host-Targeted
⚔️

Cancer Immunotherapy

DHODH inhibition reshapes the tumor microenvironment by modulating T-cell metabolism and pyrimidine availability. Studied as a combination strategy to enhance anti-tumor immunity and sensitize resistant tumors.

Tumor Microenv.
🦴

Rheumatoid Arthritis

The parent prodrug leflunomide is approved for RA; teriflunomide represents the active moiety used to dissect the immunomodulatory mechanism underlying disease control in inflammatory arthritis.

Leflunomide
🤝

Transplant Rejection

Pyrimidine-depletion-mediated lymphocyte suppression is studied as a strategy to prevent graft rejection and graft-versus-host disease, leveraging selective control of proliferating immune cells.

Transplant
🔥

NF-κB Signaling

At higher concentrations, teriflunomide inhibits NF-κB activation and certain tyrosine kinases, providing an additional axis for studying inflammatory transcription and cytokine signaling.

Transcription
⏳

Pharmacokinetics & Half-Life

With a terminal half-life of 18-19 days and >99% protein binding, teriflunomide is a model for studying long-residence small molecules, enterohepatic recirculation, and washout/cholestyramine procedures.

PK Model

Key Literature & Landmark Publications

Seminal papers on teriflunomide's DHODH mechanism, MS efficacy, and leflunomide pharmacology

O'Connor P, Wolinsky JS, Confavreux C, et al. Randomized trial of oral teriflunomide for relapsing multiple sclerosis (TEMSO). New England Journal of Medicine. 2011;365(14):1293-1303.
doi: 10.1056/NEJMoa1014656
Cherwinski HM, McCarley D, Schatzman R, et al. The immunosuppressant leflunomide interferes with phospholipase C-dependent Ca2+ mobilization and phosphatidylinositol turnover. Journal of Pharmacology and Experimental Therapeutics. 1995;272(1):460-468.
A77 1726 / leflunomide DHODH characterization
Fox RI, Herrmann ML, Frangou CG, et al. Mechanism of action for leflunomide in rheumatoid arthritis. Seminars in Arthritis and Rheumatism / Journal of Rheumatology. 1998;27 Suppl 53:39-45.
A77 1726 DHODH / pyrimidine synthesis mechanism

Available Sizes & Ordering

Research-grade Teriflunomide (CAS 108605-62-5) with full QC documentation; research packs and bulk custom quantities supported

TierPack SizeStock StatusSuitable ForLead Time
Standard1 gIn StockBiochemical / cell-based assaysSame/next-day ship
Medium5 gIn StockIn vivo pharmacology, long-term studiesSame/next-day ship
Large10 gIn StockMulti-lab collaborations, HTSSame/next-day ship
Bulk100 gIn StockProcess development, scale-upQuote to confirm
Industrial1 KGMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is Teriflunomide (CAS 108605-62-5), and what makes it unique?
Teriflunomide (code names A77 1726, HMR1726) is the pharmacologically active metabolite of the prodrug leflunomide, with molecular formula C12H9F3N2O2 and MW 270.21. It is a reversible inhibitor of dihydroorotate dehydrogenase (DHODH, IC50 262 nM) that blocks de novo pyrimidine synthesis. Uniquely, it is one of the few DHODH inhibitors with a clinically approved indication — FDA-approved (2012, brand Aubagio, Sanofi) for relapsing forms of multiple sclerosis.
How does Teriflunomide differ from leflunomide?
Leflunomide is a prodrug rapidly converted in vivo to teriflunomide, the species responsible for activity. Using teriflunomide directly bypasses the need for hepatic conversion and provides the active moiety used in the approved MS therapy. Teriflunomide also has a long terminal half-life (~18-19 days), clinically relevant for washout procedures.
What is Teriflunomide's mechanism as a DHODH inhibitor?
Teriflunomide reversibly inhibits DHODH (IC50 262 nM), the fourth enzyme in de novo pyrimidine biosynthesis and part of the mitochondrial electron transport chain. Blocking DHODH depletes pyrimidine nucleotides (UTP/dTTP) required for rapid DNA/RNA synthesis, selectively impairing proliferation of activated lymphocytes. At higher concentrations it additionally inhibits NF-κB and certain tyrosine kinases.
What clinical evidence supports Teriflunomide in multiple sclerosis?
Teriflunomide is FDA- and EMA-approved for relapsing forms of MS. The pivotal TEMSO Phase III trial (O'Connor P et al., N Engl J Med 2011) demonstrated a statistically significant reduction in annualized relapse rate and slowed MRI lesion accrual and brain-volume loss versus placebo. These disease-modifying effects reflect its immunomodulatory DHODH inhibition.
Why is Teriflunomide's long half-life clinically significant?
Teriflunomide has an unusually long terminal half-life of ~18-19 days due to enterohepatic recirculation and high plasma protein binding (>99%). Effects therefore persist for weeks after discontinuation, and a plasma washout procedure (activated charcoal / cholestyramine) may be required when rapid elimination is needed (e.g., before pregnancy or in toxicity).
How should Teriflunomide be dissolved and stored for research use?
Teriflunomide is soluble in DMSO (~32 mg/mL) and ethanol (1 mg/mL), and practically insoluble in water. Prepare a concentrated DMSO stock for assays, keeping final DMSO ≤0.1% v/v. Store powder at -20°C, dry and dark. Always research-use-only; not for human or clinical consumption.
Is QC documentation provided with each batch?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity (≥98%), NMR structural confirmation, and MS data. MSDS/SDS, solubility datasheets, and Certificates of Origin are available on request. Qualified institutions may request sample evaluation — please contact us for details.

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