Bitopertin
Bitopertin
CAS: 845614-11-1
Molecular Formula: C21H20F7N3O4S
Bitopertin - Names and Identifiers
Bitopertin - Physico-chemical Properties
| 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. |
Bitopertin - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.84 ml | 9.2 ml | 18.401 ml |
| 5 mM | 0.368 ml | 1.84 ml | 3.68 ml |
| 10 mM | 0.184 ml | 0.92 ml | 1.84 ml |
| 5 mM | 0.037 ml | 0.184 ml | 0.368 ml |
Last Update：2024-01-02 23:10:35
Bitopertin - Reference Information
Open Data Unverified Data
| 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
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