Bitopertin (R enantiomer) NEW
| Price | Get Latest Price | ||
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-08-22 |
Product Details
| Product Name: Bitopertin (R enantiomer) | CAS No.: 845614-12-2 |
| Supply Ability: 10g | Release date: 2025/08/22 |
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
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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