| 产品描述: | Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus |
| 靶点: |
SGLT2;SGLT |
| 体内研究: |
Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats |
| 参考文献: |
1. Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60. 2. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. 3. Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20°C;充氩 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.289 ml |
11.445 ml |
22.89 ml |
| 5 mM |
0.458 ml |
2.289 ml |
4.578 ml |
| 10 mM |
0.229 ml |
1.144 ml |
2.289 ml |
| 50 mM |
0.046 ml |
0.229 ml |
0.458 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。 |