RN-1 dihydrochloride

Modify Date: 2024-02-05 12:17:54

RN-1 dihydrochloride Structure
RN-1 dihydrochloride structure
Common Name RN-1 dihydrochloride
CAS Number 1781835-13-9 Molecular Weight 452.42
Density N/A Boiling Point N/A
Molecular Formula C23H31Cl2N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of RN-1 dihydrochloride


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].

 Names

Name RN-1
Synonym More Synonyms

 RN-1 dihydrochloride Biological Activity

Description 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].
Related Catalog
Target

IC50: 70 nM (LSD1), 0.51 μM (MAO-A) and 2.785 μM (MAO-B)[1]

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].
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]. 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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C23H31Cl2N3O2
Molecular Weight 452.42
Exact Mass 451.179321

 Synonyms

Ethanone, 1-(4-methyl-1-piperazinyl)-2-[[(1S,2R)-2-[4-(phenylmethoxy)phenyl]cyclopropyl]amino]-, hydrochloride (1:2)
2-({(1S,2R)-2-[4-(Benzyloxy)phenyl]cyclopropyl}amino)-1-(4-methyl-1-piperazinyl)ethanone dihydrochloride
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: RN-1
  • Price: $500.0/100mg $900.0/250mg $1800.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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