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  • 比托派汀|T6788|TargetMol

比托派汀|T6788|TargetMol

Bitopertin
845614-11-1
￥248 1mg 起订
￥355 2mg 起订
￥579 5mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
比托派汀
英文名称：
Bitopertin
CAS号：
845614-11-1
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
100%
产品类别：
抑制剂
货号：
T6788

Product Introduction

Bioactivity

名称Bitopertin
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.
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.
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]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 50 mg/mL (92 mM)
H2O : Insoluble
Ethanol : 5 mg/mL
关键字inhibit | Bitopertin | GlyT | Inhibitor | RO 4917838 | RG-1678 | RG 1678 | Glycine transporters | RO-4917838
相关产品Opiranserin | ALX-1393 | Bitopertin (R enantiomer) | Org 25543 hydrochloride | Opiranserin hydrochloride | PF-03463275 | Tilapertin | Amoxapine | Sarcosine | Iclepertin | ASP2535 | LY2365109 hydrochloride
相关库抑制剂库 | 经典已知活性库 | 已知活性化合物库 | NO PAINS 化合物库 | 神经退行性疾病化合物库 | 药物功能重定位化合物库 | 人代谢物化合物库
比拓喷丁|||比托派汀|||RO4917838|||RG1678|||Paliflutine|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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