抑制剂

生物活性靶点体外研究体内研究抑制剂试剂级价格

抑制剂

CAS号:1621673-53-7
英文名:KY-226
中文名:抑制剂
CBNumber:CB14668126
分子式:C27H31NO3S2
分子量:481.67
MOL File:1621673-53-7.mol

抑制剂化学性质

密度 :1.186±0.06 g/cm3(Predicted)
储存条件 :-20°
溶解度 :Soluble in DMSO (>25 mg/ml).
形态 :solid
酸度系数(pKa) :3.91±0.40(Predicted)
颜色 :Off-white
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

抑制剂性质、用途与生产工艺

生物活性 KY-226 是一种有效的、口服活性的 protein tyrosine phosphatase 1B (PTP1B) 的选择性变构抑制剂，对人PTP1B的IC50值为0.28 μM。KY-226 通过增强 insulin 和 leptin 信号传导来发挥抗糖尿病和抗肥胖的作用。
靶点
Target Value
PTP1B
(Cell-free assay) 0.28 μM

体外研究

In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin.
KY-226 (1 μM; 24 hours; bEnd.3 cells) treatment rescues lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. KY-226 treatment restores phosphorylation of pAkt (T308) and its downstream target forkhead box protein O1 (FoxO1) (S256) in bEnd.3 cells.

Western Blot Analysis

Cell Line:	bEnd.3 cells stimulated with LPS
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Rescued lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1.

体内研究

KY-226 (10-30 mg/kg/day; oral administration; daily; for 4 weeks; male db/db mice) treatment significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
KY-226 attenuates plasma glucose elevations in the oral glucose tolerance test. KY-226 also increases pIR and phosphorylated Akt in the liver and femoral muscle.

Animal Model:	Male db/db mice (8-11 weeks old)
Dosage:	10 mg/kg and 30 mg/kg
Administration:	Oral administration; daily; for 4 weeks
Result:	Significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.