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Bitopertin

产品编号 T6788Cas号 845614-11-1
别名 Paliflutine, 比拓喷丁, RO4917838, 比托派汀, RG1678

Bitopertin (Paliflutine) 是一种有效的甘氨酸转运蛋白 1 (GlyT1) 抑制剂,对人 hGlyT1b 的 Ki 为 8.1 nM。

Bitopertin

Bitopertin

纯度: 100%
产品编号 T6788 别名 Paliflutine, 比拓喷丁, RO4917838, 比托派汀, RG1678Cas号 845614-11-1

Bitopertin (Paliflutine) 是一种有效的甘氨酸转运蛋白 1 (GlyT1) 抑制剂,对人 hGlyT1b 的 Ki 为 8.1 nM。

规格价格库存数量
1 mg¥ 248现货
2 mg¥ 355现货
5 mg¥ 579现货
10 mg¥ 892现货
25 mg¥ 1,820现货
50 mg¥ 2,880现货
100 mg¥ 4,560现货
1 mL x 10 mM (in DMSO)¥ 693现货
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纯度:100%
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产品介绍

生物活性
产品描述
Bitopertin (Paliflutine) (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.
靶点活性
GlyT1:25 nM
体外活性
RG1678在稳定表达hGlyT1b和mGlyT1b的细胞中非竞争性抑制[3H]甘氨酸的摄取,其IC50值分别为25 ± 2 nM和22 ± 5 nM(n = 6),并在来自中国仓鼠卵巢细胞的膜上以8.1 nM的Ki值竞争性置换[3H]ORG24598的结合,针对human hGlyT1b。至30 μM浓度,RG1678对hGlyT2介导的[3H]甘氨酸摄取无影响。基于置换[3H]ORG24598的能力,RG1678的药理学在不同物种之间没有显著差异。在海马CA1锥体细胞中,RG1678在30 nM(213 ± 18%;n=7)、100 nM(269 ± 44%,n=13)时增强NMDA依赖的长期增强效应(LTP),但在300 nM(152 ± 14%;n=9)时则没有这种效果。
体内活性
给予RG1678后,在大鼠的微透析实验和大鼠的脑脊液(CSF)中均可观察到持续时间超过3小时的剂量依赖性胞外甘氨酸水平增加。在小鼠中,RG1678剂量依赖性且显著地减轻了由精神兴奋剂D-安非他明引起的过度活动。此外,RG1678还能阻止长期用苯环已哌啶(一种NMDA受体开放通道阻断剂)处理的大鼠对D-安非他明挑战的过度反应[1]。
激酶实验
Association and dissociation kinetic analysis of [3H]ORG24598 to hGlyT1 and ratforebrain membranes is performed. [3H]ORG24598 binding experiments are performed using membranes from CHO cells expressing hGlyT1b and also in membranes from mouse, rat, monkey, and dogforebrains. Saturation isotherms are determined by adding [3H]ORG24598 to rat, mouse, monkey, and dog forebrain membranes (40 μg/well) and cell membranes (10 μg/well) in a total volume of 500 μL for 3 h at room temperature. Saturation binding experiments are analyzed by an Excel-based curve-fitting program using the Michaelis-Menten equation derived from the equation of a bimolecular reaction and the law of mass action:B=(Bmax×[F])/(Kd+[F]), where B is the amount of ligand bound at equilibrium, Bmax the maximum number of binding sites, [F] the concentration of free ligand, and Kd the ligand dissociation constant. For inhibition experiments, membranes are incubated with 3 nM [3H]ORG24598 and 10 concentrations of Bitopertin for 1 h at room temperature. Schild analysis is performed in the presence of increasing concentrations of [3H]ORG24598 (1-300 nM). IC50 values are derived as described above. Ki values are calculated according to the following equation: Ki=IC50/(1+[L]/Kd)[1].
动物实验
Bitopertin (RG1678) is dissolved in H2O with 0.3% Tween 80 (Mice)[1]. Bitopertin (RG1678) is prepared in Polysorbate 80, HEC, Methyl- and Propylparaben pH 6.0 (Rats)[1].Male NMRI mice (20-30 g) are treated with Bitopertin (0.3, 3, 1, and 10 mg/kg p.o.) or vehicle (p.o.). After 1 min, L-687,414 (50 mg/kg s.c.) or vehicle is given. After 15 min of habituation in the activity chambers, horizontal activity is recorded for 60 min. The time course of Bitopertin effects on L-678,414-induced hyperactivity is also examined; locomotor activity is assessed 2.5, 4.5, and 24 h after administration of Bitopertin (L-678,414 is always given 15 min before the activity procedure). In addition, the effect of subchronic Bitopertin is investigated. Mice receive vehicle or Bitopertin (1 mg/kg p.o.) for 4 consecutive days and L-678,414-induced hyperactivity is evaluated on day 5. Wistar rats receive a 14-day treatment of PCP HC1 (5 mg/kg) or vehicle (NaCl 0.9%, 5 mL/kg i.p.). 24 h following the last injection, rats (6-18 per group) are allowed to individually habituate to the test boxes for 30 min. Rats then received Bitopertin (1, 3, 10 mg/kg p.o.) or vehicle (Polysorbate 80, HEC, Methyl- and Propylparaben pH 6.0; 5 mL/kg p.o.), followed after 1 h by 1 mg/kg D-amphetamine or vehicle i.p. Horizontal activity is recorded directly after the administration of Bitopertin until 120 min after dosing with amphetamine. Data are analyzed by ANOVA supplemented by Fischer's least significant difference post hoc test.
别名Paliflutine, 比拓喷丁, RO4917838, 比托派汀, RG1678
化学信息
分子量543.46
分子式C21H20F7N3O4S
CAS No.845614-11-1
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (92 mM)
H2O: Insoluble
Ethanol: 5 mg/mL
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.8401 mL9.2003 mL18.4006 mL92.0031 mL
5 mM0.3680 mL1.8401 mL3.6801 mL18.4006 mL
10 mM0.1840 mL0.9200 mL1.8401 mL9.2003 mL
20 mM0.0920 mL0.4600 mL0.9200 mL4.6002 mL
50 mM0.0368 mL0.1840 mL0.3680 mL1.8401 mL

计算器

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体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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