ND-630 是有效的乙酰辅酶A羧化酶 (ACC) 抑制剂,抑制人类 ACC1 和 ACC2 的IC50分别为2.1和6.1 nM。
产品描述
ND-630 is an inhibitor of acetyl-CoA carboxylase (ACC) dimerization that inhibits human ACC1 and ACC2 activity (IC50s of 2.1 and 6.1 nM, respectively)
体外活性
ND-630 inhibited hACC1 with an IC50 of 2.1 ± 0.2 nM and hACC2 with an IC50 of 6.1 ± 0.8 nM .?Inhibition was reversible and highly specific for ACC, as evidenced by the absence of an effect of ND-630 on the activity of 101 enzymes, receptors, growth factors, transporters, and ion channels of the Ricerca DrugMatrix Panel at 10 μM .?In addition, because the ACC dimerization site is not conserved among the mammalian carboxylases , ND-630 lacks the ability to inhibit any of these mechanistically related enzymes and therefore exhibits absolute specificity for ACC inhibition relative to other mammalian carboxylases.
体内活性
ND-630 reduces hepatic steatosis in a rat model of diet-induced obesity and in Zucker diabetic rats. It also improves insulin secretion stimulated by glucose and reduces hemoglobin A1c levels by 0.9% in Zucker diabetic rats.
Cas No.
1434635-54-7
分子式
C28H31N3O8S
分子量
569.63
别名
ND-630;NDI-010976;GS-0976
储存和溶解度
DMSO:50 mg/mL (87.78 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years