RN-1 (hydrochloride)
- Product Name
- RN-1 (hydrochloride)
- CAS No.
- 1781835-13-9
- Chemical Name
- RN-1 (hydrochloride)
- Synonyms
- RN1; RN 1;RN-1 (hydrochloride);RN 1 dihydrochloride;1-(4-methyl-1-piperazinyl)-2-[[(1R*,2S*)-2-[4-phenylmethoxy)phenyl]cyclopropyl]amino]ethanone dihydrochloride;disease,RN1,RN 1 dihydrochloride,Histone Demethylase,inhibit,hemoglobin,fetal,RN1 dihydrochloride,brain-penetrant,LSD1,Inhibitor,HbF,sickle,RN 1,cell,RN-1,irreversible
- CBNumber
- CB83152731
- Molecular Formula
- C23H30ClN3O2
- Formula Weight
- 415.96
- MOL File
- 1781835-13-9.mol
RN-1 (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- insoluble in EtOH; ≥2.7 mg/mL in DMSO with ultrasonic; ≥8.47 mg/mL in H2O
- form
- crystalline solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 18124
- Product name
- RN-1 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 18124
- Product name
- RN-1 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 18124
- Product name
- RN-1 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $216
- Updated
- 2024/03/01
- Product number
- 4977
- Product name
- RN1dihydrochloride
- Purity
- ≥97%(HPLC)
- Packaging
- 10
- Price
- $223
- Updated
- 2021/12/16
- Product number
- 4977
- Product name
- RN1dihydrochloride
- Purity
- ≥97%(HPLC)
- Packaging
- 50
- Price
- $936
- Updated
- 2021/12/16
RN-1 (hydrochloride) Chemical Properties,Usage,Production
Uses
RN-1 Hydrochloride is a potent, irreversible inhibitor of LSD1. It blocks long-term but not short-term memory in mice following intraperitoneal administration. RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.
Biological Activity
rn-1 (hydrochloride) is a brain-penetrant, potent and irreversible lsd1 inhibitor with ic50 values of 10-70 nm [1].lysine-specific demethylase 1 (lsd1) is a flavin-dependent monoamine oxidase that demethylate mono- and di-methylated lysines, specifically histone 3, lysines 4 and 9 (h3k4 and h3k9) [2].rn-1 (hydrochloride) is a potent and irreversible lsd1 inhibitor with ic50 values of 10-70 nm. however, rn-1 is much less effective against mao-a and mao-b with ic50 values of 0.51 and 2.785 μm, respectively [1]. in ovarian cancer lines, rn-1 also induced cytotoxicity, which was correlated with the lsd1 inhibitory potential [3].following intraperitoneal administration in mice, rn-1 penetrated the blood-brain barrier and the brain/plasma exposure ratio was 88.9. in mice, rn-1 significantly impaired long-term memory but not short-term memory. and long-term memory impairment was due to a brain-specific effect [1]. in a sickle cell disease (scd) mouse model, rn-1 induced hbf synthesis and increased frequencies of hbf-positive cells and mature erythrocytes, as well as reduced reticulocytes and sickle cells. and the rn-1 treated mice did not exhibit the necrotic lesions in the liver and spleen [4].
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. |
storage
Store at -20°C
References
[1]. neelamegam r, ricq el, malvaez m, et al. brain-penetrant lsd1 inhibitors can block memory consolidation. acs chem neurosci. 2012 feb 15;3(2):120-128.
[2]. shi y, lan f, matson c, et al. histone demethylation mediated by the nuclear amine oxidase homolog lsd1. cell. 2004 dec 29;119(7):941-53.
[3]. konovalov s, garcia-bassets i. 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.
[4]. cui s, lim kc, shi l, 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.
RN-1 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
RN-1 (hydrochloride) Suppliers
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6003
- Advantage
- 61
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4768
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8000
- Advantage
- 62
- Tel
- 18081075745
- chemflowtech@sina.com
- Country
- China
- ProdList
- 1886
- Advantage
- 58
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- +86-0371-86658258 +8613203830695
- Fax
- 0371-86658258
- laboratory@coreychem.com
- Country
- China
- ProdList
- 30229
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 021-38015121 18438616290
- lanwu@univ-bio.com
- Country
- China
- ProdList
- 24731
- Advantage
- 58