Bitopertin | RG1678;RO4917838;R-1678 | 比拓喷丁 | Glycine transporter

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比托派汀 /Bitopertin {[allProObj[0].p_purity_real_show]}

货号：A514249 同义名： 比拓喷丁 / RG1678;RO4917838

Bitopertin is a noncompetitive inhibitor of glycine reuptake with IC50 of 25 nM.

Bitopertin 化学结构
CAS号：845614-11-1

Bitopertin 3D分子结构
CAS号：845614-11-1

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Bitopertin 纯度/质量文件产品仅供科研

货号：A514249 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

Bitopertin 生物活性

靶点	GlyT1 GlyT1, IC50:22 nM
描述	Bitopertin is a potent and noncompetitive glycine reuptake inhibitor targeting on GlyT1 (glycine transporter type 1), with IC50 value of 25nM. Bitopertin enhanced NMDA-dependent long-term potentiation at 100 nM but not at 300 nM in hippocampal CA1 pyramidal cells. It dose-dependently increased cerebrospinal fluid and striatal levels of glycine measured by microdialysis in rats. Also, it attenuated hyperlocomotion induced by the psychostimulant D-amphetamine or the NMDA receptor glycine site antagonist L-687,414 in mice. Additionally, it prevented the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker. Bitopertin is usually used in study of schizophrenia. It can modulate both glutamatergic and dopaminergic neurotransmission in animal experiments that model aspects of schizophrenia.
作用机制	Bitopertin could competitively block [³H]ORG24598 binding sites at human GlyT1b.^[1]

Bitopertin 动物研究

Dose

Mice: 0.1 mg/kg - 10 mg/kg^[3] (i.p.); 0.3 mg/kg - 10 mg/kg^[1] (p.o.) Rat: 0.3 mg/kg - 3 mg/kg^[4] (p.o.), 1 mg/kg - 10 mg/kg^[1] (p.o.)

Administration

i.p., p.o.

Pharmacokinetics

Animal	Rats^[5]	Monkeys^[5]
Dose	2 mg/kg (i.v.) 3 mg/kg (p.o.)	0.5 mg/kg (i.v.) 2.8 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.
F	78% (p.o.)	56% (p.o.)
PPB % unbound		3
T_1/2	5.8 h (p.o.)	6.4 h (p.o.)
T_max	1 h (p.o.)	5.5 h (p.o.)
CL	4.32 ml/min/kg (i.v.)	3.62 ml/min/kg (i.v.)
C_max	721 ng/ml (p.o.)	517 ng/ml (p.o.)
Vd_ss	3.58 L/kg (i.v.)	1.98 L/kg (i.v.)
AUC_0→∞	8670 ng·h/ml (p.o.)	7230 ng·h/ml (p.o.)
Protein binding (free drug %)	3

Bitopertin 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01192906	Schizophrenia	Phase 3	Completed	-	-
NCT01234779	Schizophrenia	Phase 2	Completed	-	-
NCT01235559	Schizophrenia	Phase 3	Completed	-	-

Bitopertin 参考文献

[1]Alberati D, Moreau JL, et al. Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia. Neuropharmacology. 2012 Feb;62(2):1152-61.

[2]Bugarski-Kirola D, Wang A, et al. A phase II/III trial of bitopertin monotherapy compared with placebo in patients with an acute exacerbation of schizophrenia - results from the CandleLyte study. Eur Neuropsychopharmacol. 2014 Jul;24(7):1024-36.

[3]Armbruster A, Neumann E, et al. The GlyT1 Inhibitor Bitopertin Ameliorates Allodynia and Hyperalgesia in Animal Models of Neuropathic and Inflammatory Pain. Front Mol Neurosci. 2018 Jan 10;10:438.

[4]Effects of Clozapine, Aripiprazole and Bitopertin in Rats Social Withdrawal Assessed in an Automatic Social Interaction Test

[5]Pinard E, Alanine A, et al. 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. J Med Chem. 2010 Jun 24;53(12):4603-14.

Bitopertin 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.20mL

1.84mL

0.92mL

18.40mL

3.68mL

1.84mL

Bitopertin 技术信息

CAS号	845614-11-1
分子式	C₂₁H₂₀F₇N₃O₄S
分子量	543.455

别名	比拓喷丁 ;RG1678;RO4917838;R-1678
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(92 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

动物实验配方

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01192906	Schizophrenia	Phase 3	Completed	-	-
NCT01234779	Schizophrenia	Phase 2	Completed	-	-
NCT01235559	Schizophrenia	Phase 3	Completed	-	-
NCT01235585	Schizophrenia	Phase 3	Completed	-	-
NCT01636492	Healthy Volunteer	Phase 1	Completed	-	New Zealand ... 展开 >> Christchurch, New Zealand, 8011 收起 <<
NCT01192880	Schizophrenia	Phase 3	Completed	-	-
NCT03271541	Beta-Thalassemia	Phase 2	Completed	-	Italy ... 展开 >> Centro della Microcitemia e delle Anemie Congenite - Ospedale Galliera; Oncologia /Cardiologia Genova, Liguria, Italy, 16128 Ospedale Maggiore di Milano; Cardio-Metabolic Diseases Milano, Lombardia, Italy, 20122 Lebanon Chronic Care Center Baabda, Lebanon, 1003 Thailand Siriraj Hospital; Division of Haematology-Oncology Bangkok Noi, Thailand, 10700 收起 <<
NCT01674361	Obsessive-Compulsive Disorder	Phase 2	Completed	-	-
NCT02019290	Healthy Volunteer	Phase 1	Withdrawn	March 31, 2014	-

比托派汀 /Bitopertin {[allProObj[0].p_purity_real_show]}

Bitopertin 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Bitopertin 质控信息

Bitopertin 生物活性

Bitopertin 动物研究

Bitopertin 临床研究

Bitopertin 参考文献

Bitopertin 实验方案

Bitopertin 技术信息

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靶点

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比托派汀 /Bitopertin {[allProObj[0].p_purity_real_show]}

Bitopertin 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Bitopertin 质控信息

Bitopertin 生物活性

Bitopertin 动物研究

Bitopertin 临床研究

Bitopertin 参考文献

Bitopertin 实验方案

Bitopertin 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Bitopertin 纯度/质量文件产品仅供科研