| 产品描述: | 磷酸酶抑制剂;phosphatase Inhibitors;;InformationKY-226 KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively.TargetsPTP1B (Cell-free assay) 0.28 μM |
| 靶点: |
IC50: 0.25 μM (Protein tyrosine phosphatase 1B (PTP1B)) |
| 体内研究: |
KY-226 (10-30 mg/kg/天;口服给药;每天;持续 4 周;雄性 db/db 小鼠) 处理可显著降低血浆葡萄糖和甘油三酯水平以及血红蛋白 A1c 值,而无需增加体重。 KY-226 可减轻口服葡萄糖耐量试验中的血浆葡萄糖升高。KY-226 还会增加肝脏和股骨肌肉中的 pIR 和磷酸化 Akt。 |
| 参考文献: |
1. Ito Y, et al. Therapeutic effects of the allosteric protein tyrosine phosphatase 1B inhibitor KY-226 on experimental diabetes and obesity via enhancements in insulin and leptin signaling in mice. J Pharmacol Sci. 2018 May;137(1):38-46. 2. Sun M, et al. KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia. Neuroscience. 2019 Feb 10;399:89-102. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.076 ml |
10.381 ml |
20.761 ml |
| 5 mM |
0.415 ml |
2.076 ml |
4.152 ml |
| 10 mM |
0.208 ml |
1.038 ml |
2.076 ml |
| 50 mM |
0.042 ml |
0.208 ml |
0.415 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |