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Product details

名称

HS-276

英文名称

HS-276

货号

H656696-1ml

包装规格

1ml

浓度

10mM in DMSO

储存温度

-80℃储存

运输条件

超低温冰袋运输

产品介绍

HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a K i of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2 , MAP4K5, IRAK1 , NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC 50 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 In Vitro HS-276 reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC 50 values of 138, 201, and 234 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 C max of 3.68 μM and %F of 98.1% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IRAK1 264 nM (IC 50 ) IRAK4 2500 nM (IC 50 )

生化机理

HS-276 是一种口服活性、强效、高选择性 TAK1 抑制剂，其 K i 为 2.5 nM。HS-276 对 TAK1、CLK2、GCK、ULK2、MAP4K5、IRAK1、NUAK、CSNK1G2、CAMKKβ-1 和 MLK1 具有明显的抑制作用，IC 50 值分别为 8.25、29、33、63、125、264。

CAS号

2767422-72-8(DMSO)

分子式

C24H29N5O2

分子量

419.52 g/mol

Smiles

O=C(C1=CC=CC(C(NC2=NC3=C(N2CCC)C=C(CN4CCCCC4)C=C3)=O)=C1)N

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

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