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Alfa Chemistry Materials Tofacitinib citrate

Alfa Chemistry Materials Tofacitinib citrate chemically named as (3R,4R)-3-[4-methyl-3-[N-methyl-N-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropionitrile citrate, is a white or almost white powder, which is lightly soluble in water, very slightly soluble in methanol, and practically insoluble in acetone. Tofacitinib citrate is a novel, oral Janus kinase (JAK) inhibitor for the treatment of rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis.

Chemical Name: Tofacitinib citrate

Functions: API Intermediate

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Knowde Enhanced TDS

Identification & Functionality

Chemical Name

Tofacitinib citrate

Pharma & Nutraceuticals Functions

API Intermediate

CAS No.
540737-29-9
EC No.
638-826-4
Technologies

Pharmaceuticals & Nutraceuticals

Product Families

Pharmaceuticals & Nutraceuticals — Pharmaceutical Actives & Precursors

Active Pharmaceutical Ingredients (APIs),

Intermediates & Precursors

Chemical Structure

Alfa Chemistry Materials Tofacitinib citrate - Chemical Structure

Applications & Uses

Markets

Healthcare & Pharma

Applications

Healthcare & Pharma — Drug Delivery & Care Solutions

Other Drug & Care Solutions

Used as a Janus kinase (JAK) Inhibitor

Introduction of Janus kinase:

Janus kinase (JAK) is a family of intracellular, non-receptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. The JAK family is comprised of several different subtypes, notably JAK1, JAK2, JAK3 and TYK2 in addition to a multitude of STAT proteins, STAT 1, STAT2, STAT3, STAT4, STAT5a, STAT5b and STAT6. The pathway is initiated by a ligand/cytokine acting as an extracellular signal and binding to a receptor on the cell membrane which in turn causes a structural or conformational change and thus consequent activation of the implicated JAK isoforms that are either homodimers or heterodimers.Alfa Chemistry Materials Tofacitinib citrate - Used As A Janus Kinase (Jak) Inhibitor

Signaling pathway 1 in figure above: Ligand binding to the extra-cellular domain of the homodimer or heterodimer cytokines receptor, the latter is activated and auto-phosphorylation occurs, signaling pathway 2: STAT proteins bind to the activated receptor, signaling pathway 3: STAT proteins are phosphorylated followed by nucleus translocation and protein synthesis.

It’s reported that STAT4 SNPs are associated with rheumatoid arthritis, polymorphisms of STAT3 are associated with psoriatic arthritis, JAK1&JAK2&JAK3 are associated with ulcerative colitis.

Mechanism of Action:

Tofacitinib citrate inhibits the phosphorylation and activation of JAKs. JAKs cannot phosphorylate the cytokine receptors. Consequently, the receptors cannot contact with STATS. These latter are not phosphorylated and activated. Therefore, they cannot translocate to the nucleus. Gene transcription and cytokine production are inhibited. Figure below shows the simplified action mechanism diagram.Alfa Chemistry Materials Tofacitinib citrate - Used As A Janus Kinase (Jak) Inhibitor - 1

Properties

Physical Form

Powder,

Solid

Safety & Health

Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur.

  • Common side effects:
    • headache
    • upper respiratory tract infection
    • cold-like symptoms
    • diarrhea
    • skin rash
    • vomiting
  • Serious side effects:
    • blood clots
    • pneumonia
    • cancer
    • gastrointestinal perforations
    • infection
    • cellulitis
    • shingles
    • high blood pressure

Alfa Chemistry offers high quality of tofacitinib citrate which meets the CP.