Baricitinib

• Background:

  Baricitinib is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (IC50 = 5.9nM) and JAK2 (IC50 = 5.7nM) and inhibits Tyk2 (IC50 = 53nM) . It displays >100-fold selectivity for JAK1/2 over JAK3 (IC50 > 400nM) . Janus kinases (JAKs) are non-receptor kinases and play important roles in the proinflammatory signaling pathways that are frequently over-activated in autoimmune disorders such as rheumatoid arthritis. Upon binding of extracellular cytokines and growth factors, JAKs are phosphorylated and activate signal transducers and activators of transcription (STATs) . Via these signaling cascades, inflammatory cytokine and chemokine transcription is induced to form inflammatory mediators including IL-2, IL-6, IL-12, IL-15, IL-23. Baricitinib inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50nM. It inhibits IL-6 receptor signaling, IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T cells and displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. It also has been shown to block MSU-induced inflammasome activation. Baricitinib has potential application in various inflammatory disorders, including rheumatoid arthritis and systemic lupus erythematosus (SLE) . The majority of viruses enter cells through receptor mediated endocytosis. Baricitinib potently inhibits AP-2 associated protein kinase 1 (AAK1) and also binds cyclin G-associated kinase, both regulators of endocytosis. Inhibiting AAK1 might interrupt the passage of the SARS-CoV-2 virus into cells and also the intracellular assembly of virus particles. In addition the drug’s anti-inflammatory activity is expected to act on the inflammatory cascade associated with COVID-19.

• Type:

  Chemical

• Purity:

  Greater than or equal to 98% (HPLC)

• Shipping Conditions:

  Room Temp

• Storage Conditions:

  Short Term Storage: +4C. Long Term Storage: -20C. Handling Advice: Keep cool and dry. Use/Stability: Stable for at least 2 years after receipt when stored at -20C.

• Calculated Molecular Weight:

  371.4

• Other Product Names:

  LY3009104; INCB28050; 1- (Ethylsulfonyl) -3-[4- (7H-pyrrolo[2,3-d]pyrimidin-4-yl) -1H-pyrazol-1-yl]-3-azetidineacetonitrile

• Physical Properties:

  Lyophilized

• CAS Number:

  1187594-09-7