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
- 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.
- 更新日期：2024/04/30
- 产品编号：HY-120327
- 产品名称：KY-226
- CAS编号：
- 包装：1 mg
- 价格：920元
- 更新日期：2024/04/30
- 产品编号：HY-120327
- 产品名称：抑制剂 KY-226
- CAS编号：1621673-53-7
- 包装：5mg
- 价格：2300元
- 公司名称：InvivoChem
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