Bitopertin

製品コードS8219 バッチS821901

印刷

化学情報

Chemical Structure Synonyms RG1678, RO-4917838 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H20F7N3O4S
分子量 543.46 CAS No. 845614-11-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (184.0 mM)
Ethanol 100 mg/mL (184.0 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 Bitopertin (RG1678,RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.
in vitro RG1678 noncompetitively inhibits [3H]glycine uptake in cells stably expressing hGlyT1b and mGlyT1b, with IC50 values of 25 ± 2 nM and 22 ± 5 nM, respectively (n = 6) and competitively displaces [3H]ORG24598 binding with a Ki of 8.1 nM at human hGlyT1b in membranes from Chinese hamster ovary cells. RG1678 has no effect on hGlyT2-mediated [3H]glycine uptake up to 30 μM concentration. There is no significant species difference in the pharmacology for RG1678 based on the ability of the compound to displace [3H]ORG24598. In hippocampal CA1 pyramidal cells, RG1678 enhances NMDA-dependent long-term potentiation (LTP) at 30 nM (213 ± 18%; n=7), 100 nM (269 ± 44%, n=13) but not at 300 nM (152 ± 14%; n = 9)[1].
in vivo Administration of RG1678 produces a long-lasting (>3h) dose-dependent increase in extracellular glycine levels both in microdialysis experiments conducted in rats and CSF of rats. In mice, RG1678 dose-dependently and significantly attenuates hyperlocomotion induced by the psychostimulant D-amphetamine. RG1678 also prevents the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker[1].

プロトコル(参考用のみ)

キナーゼアッセイ [3H]glycine uptake assay
Assays are performed at 22 °C in uptake buffer in quadruplicate. Uptake is started by adding 25 μM nonradioactive glycine and 60 nM [3H]glycine or 200 nM [3H]glycine (hGlyT2). Nonspecific uptake is determined with 10 μM ORG24598, a potent and specific GlyT1 inhibitor (hGlyT1b and mGlyT1b) or 5 μM ORG25543, a potent and specific GlyT2 inhibitor (hGlyT2). After 15 (hGlyT1b) or 30 (mGlyT1b and hGlyT2) min, plates are washed three times with ice-cold uptake buffer. Radioactivity is measured by liquid scintillation in a PerkinElmer TopCount scintillation plate reader with quenching correction after adding 50 μl Microscint 40 and shaking for 1 h. Influence of RG1678 on the uptake of [3H]glycine is assessed by analyzing the kinetics of recombinant hGlyT1b in the presence of increasing concentrations of the inhibitor. Non-linear regression analysis (Michaelis–Menten equation) is used to determine kinetic parameters (Km and Vmax). Linear regression analysis (Linear-Burk plot) is used to confirm the nature of RG1678 competition versus glycine.
動物実験 動物モデル Mice
投薬量 0.3-30 mg/kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Glycine Enhances Satellite Cell Proliferation, Cell Transplantation, and Oligonucleotide Efficacy in Dystrophic Muscle. [ Mol Ther, 2020, 6;28(5):1339-1358] PubMed: 32209436

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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