2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
UK-5099(PF1005023) is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
IC50 value: 50 nM
Target: MCT
The trypanosomal pyruvate carrier was found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki = 17 mM) but could be completely blocked by UK5099 (Ki = 49 microM). Inhibition of pyruvate transport resulted in the retention, and concomitant accumulation, of pyruvate within the trypanosomes, causing acidification of the cytosol and osmotic destabilization of the cells. UK-5099 is more powerful inhibitor than alpha-cyano-4-hydroxycinnamate showing 50% inhibition of pyruvate-dependent O2 consumption by rat heart mitochondria at concentrations of 200, 200 and 50 nM respectively.
For the detailed information about the solubility of UK-5099 (UK5099 ) in water, the solubility of UK-5099 (UK5099 ) in DMSO, the solubility of UK-5099 (UK5099 ) in PBS buffer, the animal experiment（test） of UK-5099 (UK5099 ),the in vivo,in vitro and clinical trial test of UK-5099 (UK5099 ),the cell experiment（test） of UK-5099 (UK5099 ),the IC50, EC50 and Affinity of UK-5099 (UK5099 ), please contact DC Chemicals.
