845614-12-2

Basic information

• Product Name: RO4917838 (R enantioMer)
• Synonyms: Bitopertin (R enantioMer);RG 1678 (R enantioMer);RG1678 (R enantioMer);RG-1678 (R enantioMer);RO4917838 (R enantioMer);[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((R)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone
• CAS NO: 845614-12-2
• Molecular Formula: C₂₁H₂₀F₇N₃O₄S
• Molecular Weight: 543.4550224
• Mol File: 845614-12-2.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• CAS DataBase Reference: RO4917838 (R enantioMer)(CAS DataBase Reference)
• NIST Chemistry Reference: RO4917838 (R enantioMer)(845614-12-2)
• EPA Substance Registry System: RO4917838 (R enantioMer)(845614-12-2)

Safety Data

• Hazardous Substances Data: 845614-12-2(Hazardous Substances Data)

Usage

General Description

RO4917838 (R enantioMer) is a selective and potent inhibitor of the histone lysine methyltransferase G9a, a critical regulator of gene expression. It has been shown to effectively reduce G9a-dependent H3K9me2 levels in cells, leading to the suppression of cancer cell growth and proliferation. The compound exhibits high selectivity for G9a, with minimal off-target effects. It also has potential to be a promising therapeutic agent in cancer treatment, as it can effectively inhibit the growth of various cancer cell lines in vitro. Additionally, it is being investigated for its role in modulating immune response and as a potential treatment for neurodegenerative diseases.

Relevant articles and documents

Selective GlyT1 inhibitors: Discovery of [4-(3-fluoro-5- trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2, 2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia

The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine class of GlyT1 inhibitors to improve hERG channel selectivity and brain penetration. This effort culminated in the discovery of compound 10a (RG1678), the first potent and selective GlyT1 inhibitor to have a beneficial effect in schizophrenic patients in a phase II clinical trial.