产品
编 号:F741805
分子式:C24H29N5O2
分子量:419.52
产品类型
结构图
CAS No: 2767422-72-8
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产品详情
生物活性:
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research.
体内研究:
HS-276 (CIA mouse model of inflammatory arthritis, 50 mg/kg, IP, daily for 6 days) reduces inflammation, pannus, cartilage damage (CD), bone resorption (BR), and periosteal bone formation (PBF) histological manifestations.HS-276 (CD-1 mice, 30 mg/kg, Oral gavage, once) shows excellent bioavailability in mice with a Cmax of 3.68 μM and %F of 98.1%.
体外研究:
HS-276 reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC50 values of 138, 201, and 234 nM, respectively.