Upadacitinib(1310726-60-3)

Upadacitinib Product Information

Density: 1.56±0.1 g/cm³ (Predicted)

Storage Conditions: Store at -20°C

Solubility:

DMSO: 42.67 (maximum concentration mg/mL); 112.17 (maximum concentration mM)

DMSO:PBS (pH 7.2) (1:1): 0.5 (maximum concentration mg/mL); 1.31 (maximum concentration mM)

DMF: 30.0 (maximum concentration mg/mL); 78.87 (maximum concentration mM)

Ethanol: 76.0 (maximum concentration mg/mL); 199.8 (maximum concentration mM)

Introduction:Upadacitinib is a JAK1 inhibitor that has demonstrated excellent efficacy in clinical trials for the treatment of various autoimmune and inflammatory disorders.

Efficacy:Upadacitinib has shown remarkable efficacy in clinical trials for treating a variety of autoimmune diseases and inflammatory diseases. Developed by AbbVie, a leading international biopharmaceutical company, this oral small-molecule targeted drug was approved last year for the treatment of atopic dermatitis (AD), rheumatoid arthritis (RA), and psoriatic arthritis (PsA) in adults and adolescents aged 12 years and older. It is currently the selective JAK1 inhibitor with the most covered indications in China.

Uses:Upadacitinib is an oral JAK1 inhibitor used for the treatment of diseases such as rheumatoid arthritis and psoriatic arthritis. JAK kinases belong to a family of non-receptor tyrosine kinases, with four identified members: JAK1, JAK2, JAK3, and TYK1. The substrate of JAK is STAT (Signal Transducer and Activator of Transcription). After being phosphorylated by JAK, STAT dimerizes, then crosses the nuclear membrane and enters the nucleus to regulate the expression of related genes. This signaling pathway is known as the JAK-STAT pathway. Therefore, JAK plays a crucial role in the pathophysiological processes of immune-mediated diseases and can be used to treat certain autoimmune diseases, including atopic dermatitis, rheumatoid arthritis, psoriasis, and ulcerative colitis. In 2017, Tofacitinib, the first oral targeted JAK kinase inhibitor for rheumatoid arthritis, was launched in China. As the first JAK kinase inhibitor approved for the treatment of rheumatoid arthritis, it can block the signal transduction of inflammatory cytokines in cells that contribute to rheumatoid arthritis.

Applications:Upadacitinib (ABT-494) is a highly potent, orally active, and selective Janus kinase 1 (JAK1) inhibitor (IC50 = 43 nM). It exhibits approximately 74-fold selectivity for JAK1 over JAK2 (200 nM). Upadacitinib (ABT-494) is used in the treatment of various autoimmune diseases.