HS-276 |
| カタログ番号GC65941 |
HS-276 は、2.5 nM の Ki を持つ、経口活性で強力かつ選択性の高い TAK1 阻害剤です。 HS-276 は、TAK1、CLK2、GCK、ULK2、MAP4K5、IRAK1、NUAK、CSNK1G2、CAMKKβ-1、および MLK1 の有意な阻害を示し、IC50 値は 8.25、29、33、63、125、264、270、810 です。 、1280、および 5585 nM、それぞれ。 HS-276 は、関節リウマチ (RA) の研究に使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2767422-72-8
Sample solution is provided at 25 µL, 10mM.
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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[1].
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[1].
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[1].
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%[1].
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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