Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a noncompetitive glycine reuptake inhibitor and inhibits glycine uptake at human GlyT1 (IC50: 25 nM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 5,380 | 6-8周 | ||
50 mg | ¥ 6,990 | 6-8周 | ||
100 mg | ¥ 10,600 | 6-8周 |
Bitopertin (R enantiomer) 的其他形式现货产品:
产品描述 | Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a noncompetitive glycine reuptake inhibitor and inhibits glycine uptake at human GlyT1 (IC50: 25 nM). |
靶点活性 | GlyT1:25 nM |
体外活性 | Bitopertin (RG1678) competitively blocks [3H]ORG24598 binding sites at human GlyT1b in membranes from Chinese hamster ovary cells. In cells stably expressing hGlyT1b and mGlyT1b, Bitopertin potently inhibits [3H]glycine uptake (IC50s: 25 nM and 22 nM). Conversely, Bitopertin has no effect on hGlyT2-mediated glycine uptake up to 30 μM concentration. Bitopertin has a high affinity for the recombinant hGlyT1b transporter. Under equilibrium conditions (1 h at room temperature), Bitopertin displaces [3H]ORG24598 binding (Ki: 8.1 nM). In hippocampal CA1 pyramidal cells, Bitopertin enhances NMDA-dependent long-term potentiation at 100 nM but not at 300 nM [1]. Bitopertin has an excellent selectivity profile against the GlyT2 isoform (IC50>30 μM) and toward a panel of 86 targets including transmembrane and soluble receptors, enzymes, ion channels, and monoamine transporters (<41% inhibition at 10 μM is measured for all targets) [2]. |
体内活性 | Bitopertin dose-dependently increases cerebrospinal fluid and striatal levels of glycine measured by microdialysis in rats. Additionally, Bitopertin attenuates hyperlocomotion induced by the psychostimulant D-amphetamine or the NMDA receptor glycine site antagonist L-687,414 in mice. Bitopertin also prevents the hyper-response to the D-amphetamine challenge in rats treated chronically with phencyclidine. The administration of vehicle has no effect on extracellular levels of striatal glycine, which remained constant throughout the experiment. In contrast, p.o. administration of Bitopertin (1-30 mg/kg) produced a dose-dependent increase in extracellular glycine levels. Bitopertin (30 mg/kg) produces glycine levels 2.5 times higher than pretreatment levels. A similar dose-dependent increase in glycine concentration is observed in the CSF of rats treated p.o. with Bitopertin (1-10 mg/kg) compared with vehicle-treated animals, 3 h after drug administration [1]. In vivo pharmacokinetic studies in rat and monkey reveals that Bitopertin has, in both species, a low plasma clearance, an intermediate volume of distribution, a good oral bioavailability (78% for rat, 56% for monkey), and a favorable terminal half-life (5.8 h for rat, 6.4 h for monkey). The plasma protein binding is high in the two preclinical species (97%) and in human (98%). The CNS penetration of Bitopertin in rat (brain/plasma=0.7) is better than that in mouse (brain/plasma=0.5) [2]. |
别名 | RO4917838 (R enantiomer), RG1678 (R enantiomer), Bitopertin R enantiomer |
分子量 | 543.46 |
分子式 | C21H20F7N3O4S |
CAS No. | 845614-12-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Bitopertin (R enantiomer) 845614-12-2 Neuroscience GlyT RG-1678 RO 4917838 RO-4917838 RO4917838 (R enantiomer) RG1678 (R enantiomer) RG1678 RG 1678 Bitopertin Bitopertin R enantiomer RO4917838 Inhibitor inhibitor inhibit