1208319-26-9

Basic information

• Product Name: Oclacitinib
• Synonyms: PF-03394197 (oclacitinib);Oclacitinib PF-03394197;JAKi;trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanemethanesulfonamide;CyclohexaneMethanesulfonaMide, N-Methyl-4-(Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMino)-, trans-;N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide;N-Methyl-1-(trans-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide;Oclacitinib
• CAS NO: 1208319-26-9
• Molecular Formula: C15H23N5O2S
• Molecular Weight: 337.44042
• Product Categories: Inhibitors
• Mol File: 1208319-26-9.mol

Chemical Properties

• Appearance: /
• Density: 1.316±0.06 g/cm3(Predicted)
• Vapor Pressure: 0Pa at 20-25℃
• Storage Temp.: Refrigerator, Under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly, Sonicated)
• PKA: 11.59±0.40(Predicted)
• CAS DataBase Reference: Oclacitinib(CAS DataBase Reference)
• NIST Chemistry Reference: Oclacitinib(1208319-26-9)
• EPA Substance Registry System: Oclacitinib(1208319-26-9)

Safety Data

• Hazardous Substances Data: 1208319-26-9(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
Oclacitinib is used as an anti-allergy medication for the treatment of various allergic conditions. Its primary application is in managing moderate to severe allergic reactions, particularly in cases where other treatments have been ineffective or poorly tolerated.
Used in Allergy Treatment:
Oclacitinib is used as a therapeutic agent for the treatment of allergic diseases, such as atopic dermatitis, asthma, and allergic rhinitis. It works by inhibiting the JAK enzymes, which are involved in the signaling pathways of cytokines that contribute to allergic inflammation. This inhibition helps to reduce the severity of allergy symptoms and improve the overall quality of life for patients suffering from these conditions.
Used in Immunology Research:
Oclacitinib is also used as a research tool in immunology to study the role of JAK enzymes in immune responses and allergic reactions. By understanding the mechanisms of action of Oclacitinib, researchers can gain valuable insights into the development of new therapeutic strategies for the treatment of various immune-related disorders.

Biological Activity

janus kinase (jak) enzymes are involved in cell signaling pathways activated by cytokines dysregulated in allergy. pf-03394197 (oclacitinib) is a novel janus kinase inhibitor.

in vitro

pf-03394197 inhibited jak family members by 50% at concentrations ranging from 10 to 99 nm and did not inhibit a panel of 38 non-jak kinases. pf-03394197 was most potent at inhibiting jak1. pf-03394197 also inhibited the function of jak1-dependent cytokines involved in allergy and inflammation as well as pruritus. pf-03394197 had minimal effects on cytokines which did not activate the jak1 enzyme in cells [1].

in vivo

pf-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily was safe and efficacious in controlling the pruritus associated with allergic dermatitis. pf-03394197 provided itch relief within 24 h that persisted through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7 [2].

IC 50

10 nm for jak1