| 产品描述: | MIPS-21335 is a PI3KC2α inhibitor with an IC50 of 7 nM. MIPS-21335 also inhibits PI3KC2β, p110α, p110β and p110δ, with IC50 values of 43, 140, 386 and 742 nM, respectively. MIPS-21335 has antithrombotic effect. MIPS-21335 can be used for the researches of cardiovascular disease and metabolic disease, such as thrombosis and hyperlipidemia. |
| 靶点: |
PI3KC2α:7 nM (IC50);PI3KC2β:43 nM (IC50);p110α:140 nM (IC50);p110β:386 nM (IC50);p110δ:742 nM (IC50) |
| 体外研究: |
MIPS-21335 (1 mg/kg,静脉注射,尾部切断前 10 分钟) 在血栓形成小鼠模型中显著延迟并最终阻止了血栓形成[1]。 |
| 体内研究: |
MIPS-21335 (10 μM, 10 mins) 会阻碍血液中胶原表面上血小板依赖性血栓的生长。 MIPS-21335 (0.1-10 μM, 10 mins) 可减少高胆固醇血症小鼠中分离出的血液中的血栓形成。 |
| 参考文献: |
1. Selvadurai MV, et al. Disrupting the platelet internal membrane via PI3KC2α inhibition impairs thrombosis independently of canonical platelet activation. Sci Transl Med. 2020 Jul 22;12(553):eaar8430. 2. Setiabakti NM, et al. PI3KC2α inhibition is antithrombotic in blood from hypercholesterolemic mice. J Thromb Haemost. 2024 Jan;22(1):249-254. |
| 保存条件: |
-80°C 12个月; -20°C 6个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.051 ml |
10.257 ml |
20.514 ml |
| 5 mM |
0.41 ml |
2.051 ml |
4.103 ml |
| 10 mM |
0.205 ml |
1.026 ml |
2.051 ml |
| 50 mM |
0.041 ml |
0.205 ml |
0.41 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。 |