RO4917838

Name	Bitopertin
Synonyms	RG1678 RG1679 RO4917838 Bitopertin Paliflutine Palufidine,RG-1678 (S)-[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-(methanesulfonyl)-2-(2,2,2-trifluoro-1-methylethoxy)phenyl]methanone [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone
CAS	845614-11-1

Molecular Formula	C21H20F7N3O4S
Molar Mass	543.46
Density	1.444
Solubility	DMSO
Storage Condition	-20℃
Use	RG1678 (Bitopertin) is a non-competitive glycine reabsorption (GlyT1) inhibitor.
In vitro study	RG1678 noncompetitively inhibited the uptake of [3H] glycine in cells stably expressing hGlyT1b and mGlyT1b with an IC50 of 25±2 nM and 22±5 nM, respectively. RG1678 competitively substituted [3H]ORG24598 for binding to human hGlyT1b in CHO cells with a Ki of 8.1 nM. Even at a concentration of 30 μm, RG1678 had no effect on hGlyT2-mediated [3H] glycine uptake. There was no significant difference in the ability of RG1678 to competitively displace [3H] org 24598 across species. In hippocampal CA1 pyramidal cells, 30nM, 100nM RG1678 enhanced NMDA-dependent long-term potentiation, while 300 nM RG1678 did not.
In vivo study	In microdialysis experiments in rats and rat cerebrospinal fluid, RG1678 consistently increased extracellular glycine levels in a dose-dependent manner. In mice, RG1678 significantly reduced the rapid movement induced by d-amphetamine. In the rat, RG1678 will prevent the overreaction due to long-term treatment with Phencyclidine.

Last Update：2024-01-02 23:10:35

biological activity	Bitopertin (RG1678, RO-4917838) is a potent inhibitor of GlyT1(glycine transporter 1) with an IC50 of 25 nM in CHO cells.
target	TargetValue GlyT1 (in cells stable expressing mGlyT1b) 22 nM GlyT1 (in cells stable expressing hGlyT1b) 25nM
Target	Value
GlyT1 (in cells stably expressing mGlyT1b)	22 nM
GlyT1 (in cells stably expressing hGlyT1b)	25nM
In vitro study	RG1678 non-competitively inhibits the absorption of [3H] glycine in cells that stably express hGlyT1b and mGlyT1b, and its IC50 is 25±2 nM and 22±5 nM, respectively. RG1678 competitively replaces [3H]ORG24598 and binds human hGlyT1b in CHO cells with a Ki of 8.1 nM. Even if the concentration is mentioned at 30 μM,RG1678 has no effect on the [3H] glycine uptake mediated by hGlyT2. There was no significant difference in the ability of RG1678 to competitively replace [3H]ORG24598 among different species. In hippocampal CA1 pyramidal cells, 30nM, 100nM RG1678 enhanced NMDA-dependent long-term potentiation, while 300 nM RG1678 did not.
in vivo study	in the microdialysis experiment of cerebrospinal fluid of rats and rats, RG1678 continuously increases the level of extracellular glycine, which is dose-dependent. In mice, RG1678 significantly reduced the rapid movement induced by dextroamphetamine. In rats, RG1678 will prevent the overreaction caused by long-term treatment of phenzyclidine.

Last Update：2024-04-09 19:43:38

Product Name: Bitopertin Request for quotation
CAS: 845614-11-1
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CAS: 845614-11-1
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Product Name: Bitopertin Request for quotation
CAS: 845614-11-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052

Wechat: 15671228036

Product Name: Bitopertin Visit Supplier Webpage Request for quotation
CAS: 845614-11-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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RO4917838

RO4917838 Request for Quotation