RN-1 dihydrochloride 是血脑屏障通透性的、不可逆的赖氨酸特异性脱甲基酶 1 (LSD1) 选择性抑制剂,IC50为 70 nM,对 LSD1 的选择性高于 MAO-A 和 MAO-B,IC50分别为 0.51 μM 和 2.785 μM。
产品描述
RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).
体外活性
RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively[3].
体内活性
In sickle cell disease (SCD) mice, RN-1 dihydrochloride (3-10 mg/kg; i.p.) effectively induces fetal hemoglobin (HbF) levels in red blood cells and reduces disease pathology[1]. In C57BL/6 male mice, after administration of RN-1 dihydrochloride (10 mg/kg, i.p.), concentrations are detectable up to 24 h post dose in both plasma and brain tissues. RN-1 dihydrochloride significantly impairs long-term memory, but not short-term memory. The brain/plasma exposure ratio is 88.9[3].
Cas No.
1781835-13-9
分子量
452.417
储存和溶解度
H2O:18 mg/mL (39.79 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years