RN-1 dihydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RN-1 dihydrochloride  纯度: 99.75%

RN-1 dihydrochloride 是一种有效的、可透过血脑屏障、不可逆的、选择性的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂，IC50 为 70 nM。RN-1 dihydrochloride 对 LSD1 的选择性高于 MAO-A 和 MAO-B，IC50 值分别为 0.51 μM 和 2.785 μM。

RN-1 dihydrochloride

RN-1 dihydrochloride Chemical Structure

CAS No. : 1781835-13-9

规格 价格 是否有货 数量
5 mg ￥1400 In-stock
10 mg ￥2400 In-stock
50 mg ￥8900 In-stock
100 mg ￥14500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

RN-1 dihydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Anti-Cardiovascular Disease Compound Library

生物活性

RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. 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[1][2].

IC50 & Target

IC50: 70 nM (LSD1), 0.51 μM (MAO-A) and 2.785 μM (MAO-B)[1]
体外研究
(In Vitro)

RN-1 dihydrochloride shows cytotoxic for ovarian cancer cells (SKOV3, OVCAR3, A2780 and cisplatin-resistant A2780cis), with IC50 values of ≈100-200 μM[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

RN-1 (3-10 mg/kg; i.p.; daily; for 2 or 4 consecutive weeks) dihydrochloride effectively induces fetal hemoglobin (HbF) levels in red blood cells and reduces disease pathology in SCD mice[2].
In C57BL/6 male mice, after intraperitoneal administration of RN-1 dihydrochloride (10 mg/kg), concentrations are detectable up to 24 h post dose in both plasma and brain tissues. The brain/plasma exposure ratio is 88.9. RN-1 dihydrochloride significantly impairs long-term memory, but not short-term memory[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sickle cell disease (SCD) mice[2]
Dosage: 3 mg/kg or 10 mg/kg
Administration: i.p.; daily; for 2 or 4 consecutive weeks
Result: Effectively induced HbF levels in red blood cells and reduced disease pathology in SCD mice.

分子量

452.42

Formula

C23H31Cl2N3O2
CAS 号

1781835-13-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 20 mg/mL (44.21 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 2.2103 mL 11.0517 mL 22.1034 mL
5 mM 0.4421 mL 2.2103 mL 4.4207 mL
10 mM 0.2210 mL 1.1052 mL 2.2103 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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Ramesh Neelamegam, et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. ACS Chem Neurosci. 2012 Feb 15;3(2):120-128.

    [2]. Shuaiying Cui, et al. The LSD1 inhibitor RN-1 induces fetal hemoglobin synthesis and reduces disease pathology in sickle cell mice. Blood. 2015 Jul 16;126(3):386-96.

    [3]. Sergiy Konovalov, et al. Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines. J Ovarian Res. 2013 Oct 29;6(1):75.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务