1006378-90-0

Basic information

• Product Name: p38 MAPK-IN-1
• Synonyms: p38 MAPK-IN-1
• CAS NO: 1006378-90-0
• Molecular Formula: C21H14F2N2O
• Molecular Weight: 348.3454664
• Mol File: 1006378-90-0.mol

Chemical Properties

• Boiling Point: 527.0±50.0 °C(Predicted)
• Appearance: /
• Density: 1.27±0.1 g/cm3(Predicted)
• PKA: 0.26±0.40(Predicted)
• CAS DataBase Reference: p38 MAPK-IN-1(CAS DataBase Reference)
• NIST Chemistry Reference: p38 MAPK-IN-1(1006378-90-0)
• EPA Substance Registry System: p38 MAPK-IN-1(1006378-90-0)

Safety Data

• Hazardous Substances Data: 1006378-90-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Research and Development:
p38 MAPK-IN-1 is used as a research tool for studying the role of p38α MAP kinase in cellular signaling pathways. Its potential in the development of therapeutic treatments makes it a promising candidate for diseases such as rheumatoid arthritis, inflammatory bowel disease, and cancer.
Used in Preclinical Research:
p38 MAPK-IN-1 is used as a selective inhibitor in preclinical research to investigate its effects on cell proliferation, survival, and differentiation. The promising results obtained from these studies could lead to the development of novel drugs for various medical conditions.

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Relevant articles and documents

1,7-naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase

The design, synthesis, and ability to inhibit p38 MAP kinase by a novel series of naphthyridine N-oxides will be described. Some of these compounds showed a significant reduction in the LPS-induced TNF production in human whole blood. Structure-activity relationship studies revealed that N-oxide oxygen was essential for activity and was probably a determinant factor for its marked selectivity against other related kinases. After an extensive SAR exercise, several compounds from this series were identified as very potent p38 inhibitors. In vivo efficacy of some derivatives was demonstrated to reduce TNF levels in an acute murine model of inflammation (ED50 = 0.5 mg/kg in LPS-induced TNF production when dosed orally 1.5 h prior to LPS administration). The oral efficacy was further demonstrated in a chronic model of adjuvant arthritis in rats with established disease when administered orally (ED 50 1 mg/kg).

1, 7-NAPHTHYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS

This invention is directed to new inhibitors of the p38 mitogen-activated protein kinas having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.