OSS-128167

中文名称:

OSS-128167

中文同义词:

英文名称:

OSS-128167

英文同义词:

OSS-128167;OSS 128167;OSS128167;OSS-128167(SIRT6-IN-1);OSS-128167;SIRT6-IN-1;Benzoic acid, 5-[[3-[(2-furanylcarbonyl)amino]benzoyl]amino]-2-hydroxy-

CAS号:

887686-02-4

分子式:

C19H14N2O6

分子量:

366.32

EINECS号:

604-604-1

相关类别:

API

Mol文件:

887686-02-4.mol

储存条件 

Sealed in dry,2-8°C

生物活性

OSS_128167 (SIRT6-IN-1)是一种特异性的 SIRT6 抑制剂，对SIRT6, SIRT1和SIRT2的IC50分别为89, 1578和751 μM。OSS_128167 在HBV的转录和复制中起到抗病毒的作用。

靶点

Target Value SIRT6 (Cell-free) 89 μM SIRT2 (Cell-free) 751 μM SIRT1 (Cell-free) 1578 μM

Target

Value

SIRT6 (Cell-free)

89 μM

SIRT2 (Cell-free)

751 μM

SIRT1 (Cell-free)

1578 μM

体外研究

OSS-128167对SIRT6具有特异性，其对SIRT1和SIRT2的IC50s比对SIRT6的高约20倍。它具有细胞渗透性，在培养细胞中具有活性。OSS-128167能够增加H3K9乙酰化和GLUT-1的表达水平。

体内研究

OSS_128167 (50 mg/kg; intraperitoneal injection; every 4 days; for 12 days; male HBV transgenic mice) treatment markedly suppresses the level of HBV DNA and 3.5-Kb RNA in HBV transgenic mice. Animal Model: Male HBV transgenic mice (6-8-week-old) Dosage: 50 mg/kg Administration: Intraperitoneal injection; every 4 days; for 12 days Result: The level of HBV DNA and 3.5-Kb RNA were markedly suppressed in HBV transgenic mice.

Animal Model:

Male HBV transgenic mice (6-8-week-old)

Dosage:

50 mg/kg

Administration:

Intraperitoneal injection; every 4 days; for 12 days

Result:

The level of HBV DNA and 3.5-Kb RNA were markedly suppressed in HBV transgenic mice.