RN-1 dihydrochloride

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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

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50 mg ¥8900 In-stock
100 mg ¥14500 In-stock
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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.

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