| 产品描述: | SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5 |
| 靶点: |
IC50: 0.022 μM (HepG2/14C-Citrate Uptake Assay); 0.056 μM (recombinant hSLC3A5/14C-Citrate Uptake Assay);Stearoyl-CoADesaturase(SCD) |
| 体外研究: |
SLC13A5-IN-1 exhibits an IC50 of 0.022 μM in HepG2/14C-Citrate Uptake Assay. HepG2 cells endogenously express hSLC13A5 transporter which is responsible for the uptake of citrate into these cells. Uptake of 14C-citrate can be completely blocked by SLC13A5-IN-1 and the signal can be competed with unlabelled citrate. T.
SLC13A5-IN-1 exhibits an IC50 of 0.056 μM in recombinant hSLC3A5/14C-Citrate Uptake Assay.
SLC13A5-IN-1 exhibits an IC50 of 100 μM in recombinant Human GlyT2/3H-Glycine Uptake Assay. The human embryonic kidney 293 cells are used that stably over-express the human GlyT2 receptor which is responsible for the uptake of glycine into these cells. Uptake of 3H-glycine can be completely blocked by SLC13A5-IN-1. |
| 体内研究: |
MEISi-2 (10 µM; i.p.; at day 1, day 4 and day 7) functionally inhibits MEIS in vivo, thus they induces c-Kit+ cell, Sca1+ cell, CD150+ cell, LSK HSPCs, LSKCD34low HSC content and LSKCD150+CD48- HSC content.
MEISi-2 down-regulates Meis1 expression, Hif-2α, and key CDKI gene expression including p16, p19, p19ARF. |
| 参考文献: |
1. Joerg Kley, et al. Sulfonamides as inhibitors of the uptake of extracellular citrate. Patent WO2018104220A1 |
| 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 |
2.165 ml |
10.827 ml |
21.655 ml |
| 5 mM |
0.433 ml |
2.165 ml |
4.331 ml |
| 10 mM |
0.217 ml |
1.083 ml |
2.165 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.433 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。 |