D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.
体外研究
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.
体内研究
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.
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)
溶解性数据
In Vitro:
DMSO : 80 mg/mL (230.39 mM; ultrasonic and warming and heat to 60°C)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.8799 mL
14.3993 mL
28.7985 mL
5 mM
0.5760 mL
2.8799 mL
5.7597 mL
10 mM
0.2880 mL
1.4399 mL
2.8799 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: