D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.
性状
Solid
体外研究(In Vitro)
D-Cl-amidine (200-400 μM) is effective in significantly decreasing cell viability in MDA-MB-231 cells.D-Cl-amidine increase caspase 3 activity, indicating that inhibition of PAD1 leads to an increase in apoptosis. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
D-Cl-amidine, administered by iv at a dose of 2.5 mg/kg, is still detected after 2 h in serum at a concentration of ~21 nM and at 4 h at ~10 nM. D-Cl-amidine is still observed in the blood serum at a concentration of ~10 nM at 4 h when administered by ip at a dose of 10 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Bicker KL, et al. D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. ACS Med Chem Lett. 2012 Oct 26;3(12):1081-1085.
溶解度数据
In Vitro: DMSO : 80 mg/mL (230.39 mM; ultrasonic and warming and heat to 60°C)H2O : 16.67 mg/mL (48.01 mM; ultrasonic and warming and heat to 60°C)