Bitopertin (R enantiomer) NEW
| Price | Get Latest Price | ||
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-07-18 |
Product Details
| Product Name: Bitopertin (R enantiomer) | CAS No.: 845614-12-2 |
| Supply Ability: 10g | Release date: 2025/07/18 |
Product Introduction
Bioactivity
| Name | Bitopertin (R enantiomer) |
| Description | Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin, a noncompetitive glycine reuptake inhibitor that inhibits glycine uptake at human GlyT1 (IC50: 25 nM). |
| In vitro | Bitopertin (RG1678) competitively blocks [3H]ORG24598 binding sites at human GlyT1b in membranes from Chinese hamster ovary cells. In cells stably expressing hGlyT1b and mGlyT1b, Bitopertin potently inhibits [3H]glycine uptake (IC50s: 25 nM and 22 nM). Conversely, Bitopertin has no effect on hGlyT2-mediated glycine uptake up to 30 μM concentration. Bitopertin has a high affinity for the recombinant hGlyT1b transporter. Under equilibrium conditions (1 h at room temperature), Bitopertin displaces [3H]ORG24598 binding (Ki: 8.1 nM). In hippocampal CA1 pyramidal cells, Bitopertin enhances NMDA-dependent long-term potentiation at 100 nM but not at 300 nM [1]. Bitopertin has an excellent selectivity profile against the GlyT2 isoform (IC50>30 μM) and toward a panel of 86 targets including transmembrane and soluble receptors, enzymes, ion channels, and monoamine transporters (<41% inhibition at 10 μM is measured for all targets) [2]. |
| In vivo | Bitopertin dose-dependently increases cerebrospinal fluid (CSF) and striatal glycine levels measured by microdialysis in rats, attenuates hyperlocomotion induced by D-amphetamine or NMDA receptor glycine site antagonist L-687,414 in mice, and prevents hyper-response to D-amphetamine in rats chronically treated with phencyclidine. Vehicle administration has no effect on extracellular striatal glycine levels. Oral administration of Bitopertin (1-30 mg/kg) dose-dependently increases extracellular glycine levels, with a 30 mg/kg dose resulting in a 2.5-fold increase. Similar dose-dependent increases in CSF glycine concentration are observed in rats treated with Bitopertin (1-10 mg/kg) compared to vehicle-treated animals, 3 hours post-administration [1]. In vivo pharmacokinetic studies reveal that Bitopertin has low plasma clearance, intermediate volume of distribution, good oral bioavailability (78% in rats, 56% in monkeys), favorable terminal half-life (5.8 h in rats, 6.4 h in monkeys), high plasma protein binding (97% in preclinical species, 98% in humans), and better CNS penetration in rats (brain/plasma=0.7) than in mice (brain/plasma=0.5) [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | RO-4917838 | RO4917838 | RO 4917838 | RG-1678 | RG1678 | RG 1678 | GlyT1 | Bitopertin (R enantiomer) | Bitopertin |
| Inhibitors Related | Sarcosine | Opiranserin hydrochloride | ASP2535 | Tilapertin | Iclepertin | Org 25543 hydrochloride | Opiranserin | LY2365109 hydrochloride | Bitopertin | PF-03463275 | ALX-1393 | Amoxapine |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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