[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone
- CAS No.
- 845614-11-1
- Chemical Name:
- [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone
- Synonyms
- RG1678;RG1679;R-1678;RO4917838;DISC-1459;Bitopertin;RO-4927838;Paliflutine;RG1678, RO-4917838;Palufidine,RG-1678
- CBNumber:
- CB12546501
- Molecular Formula:
- C21H20F7N3O4S
- Molecular Weight:
- 543.46
- MDL Number:
- MFCD18251496
- MOL File:
- 845614-11-1.mol
- MSDS File:
- SDS
[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone Properties
Boiling point | 635.1±55.0 °C(Predicted) |
---|---|
Density | 1.444 |
storage temp. | Store at -20°C |
solubility | insoluble in H2O; ≥17.94 mg/mL in EtOH; ≥88.9 mg/mL in DMSO with ultrasonic |
form | crystalline solid |
pka | 3.57±0.39(Predicted) |
color | White to off-white |
FDA UNII | Q8L6AN59YY |
[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone price More Price(25)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 19896 | Bitopertin ≥98% | 845614-11-1 | 10mg | $121 | 2024-03-01 | Buy |
Cayman Chemical | 19896 | Bitopertin ≥98% | 845614-11-1 | 25mg | $287 | 2024-03-01 | Buy |
Cayman Chemical | 19896 | Bitopertin ≥98% | 845614-11-1 | 50mg | $543 | 2024-03-01 | Buy |
Cayman Chemical | 19896 | Bitopertin ≥98% | 845614-11-1 | 100mg | $961 | 2024-03-01 | Buy |
TRC | B591450 | Bitopertin | 845614-11-1 | 50mg | $5225 | 2021-12-16 | Buy |
[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone Chemical Properties,Uses,Production
Uses
Bitopertin is a potent and noncompetitive glycine reuptake inhibitor (GRI). Bitopertin is an investigational agent for the treatment of schizophrenia.
in vivo
Bitopertin (RG1678) dose-dependently increases cerebrospinal fluid and striatal levels of glycine measured bymicrodialysis in rats. Additionally Bitopertin attenuates hyperlocomotion induced by the psychostimulant D-amphetamine or the NMDA receptor glycine site antagonist L-687,414 in mice. Bitopertin also prevents the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker. Administration of vehicle has no effect on extracellular levels of striatal glycine, which remained constant throughout the experiment. In contrast, p.o. administration of Bitopertin (1-30 mg/kg) produced a dose-dependent increase in extracellular glycine levels. Bitopertin 30 mg/kg produces glycine levels 2.5 times higher than pretreatment levels. A similar dose-dependent increase in glycine concentration is observed in the CSF of rats treated p.o. with Bitopertin (1-10 mg/kg) compared with vehicle-treated animals, 3 h after drug administration. Interestingly, the level of CSF glycine increase 3 h after Bitopertin dosing is very similar to the increase in the microdialysis experiment at the same time point[1]. In vivo pharmacokinetic studies in rat and monkey reveals that Bitopertin (RG1678) has, in both species, a low plasma clearance, an intermediate volume of distribution, a good oral bioavailability (78% for rat, 56% for monkey), and a favorable terminal half-life (5.8 h for rat, 6.4 h for monkey). The plasma protein binding is high in the two preclinical species (97%) and in human (98%). The CNS penetration of Bitopertin in rat (brain/plasma=0.7) is better than that in mouse (brain/plasma=0.5)[2].
IC 50
GlyT1
[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49732 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9911 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
Hefei TNJ Chemical Industry Co.,Ltd. | +86-0551-65418684 +8618949823763 | sales@tnjchem.com | China | 25356 | 58 |
LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24727 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
Seasons Biotechnology Co., Ltd. | +86-0576-89232655 +86-13566878689 | info@seasonsbio.com | China | 47 | 58 |
View Lastest Price from [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-Methylsulfonyl-2-[((S)-2,2,2-trifluoro-1-methylethyl)oxy]phenyl]methanone manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2025-04-30 | Bitopertin
845614-11-1
|
US $35.00-89.00 / mg | 98.57% | 10g | TargetMol Chemicals Inc. |
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- Bitopertin
845614-11-1
- US $35.00-89.00 / mg
- 98.57%
- TargetMol Chemicals Inc.