GSK2981278(CAS:1474110-21-8)

GSK2981278 (CAS 1474110-21-8) is a highly selective RORγ inverse agonist small-molecule API independently developed by GlaxoSmithKline (GSK). It specifically targets and regulates the Th17 cell inflammatory pathway and serves as a benchmark research-grade API for autoimmune inflammatory diseases, especially psoriasis. With precise target selectivity, potent anti-inflammatory activity and clear pharmacological mechanism, it has become a core raw material for global immunopharmacological research, innovative anti-inflammatory drug screening and dermatological candidate drug development, widely used in university scientific research, pharmaceutical R&D, pharmacological experiments and compound activity screening. Featuring stable physical and chemical properties, high molecular structure purity and strict impurity control, it delivers excellent batch stability, fully meeting the raw material standards for high-end scientific experiments and pre-IND new drug research, and adapting to various in vitro cell experiments, animal model tests and formulation pre-research.

In terms of pharmacological mechanism, RORγ is the key nuclear receptor regulating Th17 cell differentiation and activation, as well as the core target mediating psoriasis and autoimmune inflammation. Excessive activation of Th17 cells induces massive secretion of pro-inflammatory cytokine IL-17, triggering abnormal proliferation of skin keratinocytes, vasodilation and inflammatory cell infiltration, eventually leading to typical psoriatic pathological lesions such as skin erythema, scales and swelling. As a specific inverse agonist, GSK2981278 accurately binds to RORγ receptors, efficiently blocks the binding of RORγ to target gene DNA, directly inhibits the activation of IL-17 gene promoter, and blocks the synthesis and release of IL-17 and downstream pro-inflammatory factors at the upstream pathway, completely cutting off the inflammatory cascade. Different from traditional broad-spectrum anti-inflammatory raw materials, it features single target specificity and extremely low off-target effects, precisely targeting skin-specific inflammatory pathways without interfering with normal immune metabolism, with outstanding anti-inflammatory accuracy and safety.

In scientific research applications, GSK2981278 is mainly applied to the pathological mechanism research of psoriasis and the development of new topical anti-inflammatory drugs. Preclinical animal experiments have verified that local administration of GSK2981278 significantly relieves skin redness, hyperplasia and scales in psoriasis model mice, effectively inhibits inflammatory infiltration in skin tissues and reduces local inflammation levels, showing excellent local skin anti-inflammatory potential. Although the Phase I clinical trial of systemic administration was terminated due to insufficient local drug exposure, its definite target activity and anti-inflammatory efficacy make it a core tool drug for RORγ target modification, structural optimization and combined medication research. In addition to psoriasis, it is also used for mechanism research of Th17-mediated autoimmune diseases such as rheumatoid arthritis and systemic inflammation, providing core experimental support for the R&D of broad-spectrum anti-inflammatory drugs.

In terms of raw material supply and application advantages, GSK2981278 adopts mature synthetic technology and advanced purification process to stably provide high-purity finished products without impurity interference, ensuring excellent experimental repeatability and meeting high-end scientific research demands such as high-throughput drug screening, in-depth mechanism research and formulation development. It has suitable solubility for in vitro experiments and topical formulation research, stable physical and chemical properties and good storage stability for long-term scientific research use. As a globally recognized tool drug for RORγ targets with clear mechanism and sufficient experimental data, it is an essential core raw material for universities, research institutions and innovative pharmaceutical enterprises to study immune inflammatory pathways and develop innovative dermatological drugs. With the booming R&D of new drugs for autoimmune skin diseases and growing demand for precise targeted anti-inflammatory APIs, GSK2981278 maintains long-term stable market prospects in immunopharmacological research and innovative drug development due to its irreplaceable research value and practicability.