生物活性 | |||
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描述 | G0/G1 switch 2 (G0s2) may aggravate renal dysfunction in the context of CKD (chronic kidney disease) through mechanisms involving increased renal expression of the Clock gene making G0s2 a promising therapeutic target in the treatment of CKD. NS-3-008 HCl is an orally active G0s2 transcriptional inhibitor with an IC50 of 2.25 μM. Treatment of wild-type 5/6Nx mice with NS-3-008 (5 mg/kg, P.O.) resulted in decreased levels of G0s2 and Ccl2 mRNA in the kidneys. Furthermore, the phosphorylation of Stat5 and p65 protein was decreased in wild-type 5/6Nx mice treated with NS-3-008, and serum urea nitrogen (SUN) concentrations and renal caspase 3/7 activity decreased as well. Finally, the F4/80-positive area and F4/80 protein levels were decreased in 5/6Nx mice treated with NS-3-008[1]. | ||
作用机制 | NS-3-008 bound to Hsd17b4[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.71mL 0.74mL 0.37mL |
18.53mL 3.71mL 1.85mL |
37.06mL 7.41mL 3.71mL |
参考文献 |
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