[CAS NO. 845614-11-1] Bitopertin

Name: Bitopertin
Brand: Arctom Scientific
SKU: SLK-S8219

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PRODUCTS SPECIFICATIONS [845614-11-1]

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Catalog

SLK-S8219

Brand

Selleck

CAS

845614-11-1

DESCRIPTION [845614-11-1]

Overview

MDL	MFCD18251496
Molecular Weight	543.46
Molecular Formula	C21H20F7N3O4S
SMILES	C(=O)(C1=C(O[C@H](C(F)(F)F)C)C=CC(S(C)(=O)=O)=C1)N2CCN(CC2)C3=C(F)C=C(C(F)(F)F)C=N3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8401 mL	9.2003 mL	18.4006 mL
5 mM	0.3680 mL	1.8401 mL	3.6801 mL
10 mM	0.1840 mL	0.9200 mL	1.8401 mL
50 mM	0.0368 mL	0.1840 mL	0.3680 mL

Description

Bitopertin (RG1678,RO-4917838) is a potent inhibitor of , with of 8.1 nM for human hGlyT1b and of 22-25 nM in Chinese hamster ovary cells.

Targets

GlyT1 ^[1] (in cells stably expressing mGlyT1b)	GlyT1 ^[1] (in cells stably expressing hGlyT1b)
22 nM	25nM

In vitro

RG1678 noncompetitively inhibits [3H]glycine uptake in cells stably expressing hGlyT1b and mGlyT1b, with IC50 values of 25 ± 2 nM and 22 ± 5 nM, respectively (n = 6) and competitively displaces [3H]ORG24598 binding with a Ki of 8.1 nM at human hGlyT1b in membranes from Chinese hamster ovary cells. RG1678 has no effect on hGlyT2-mediated [3H]glycine uptake up to 30 μM concentration. There is no significant species difference in the pharmacology for RG1678 based on the ability of the compound to displace [3H]ORG24598. In hippocampal CA1 pyramidal cells, RG1678 enhances NMDA-dependent long-term potentiation (LTP) at 30 nM (213 ± 18%; n=7), 100 nM (269 ± 44%, n=13) but not at 300 nM (152 ± 14%; n = 9).

In vivo

Administration of RG1678 produces a long-lasting (>3h) dose-dependent increase in extracellular glycine levels both in microdialysis experiments conducted in rats and CSF of rats. In mice, RG1678 dose-dependently and significantly attenuates hyperlocomotion induced by the psychostimulant D-amphetamine. RG1678 also prevents the hyper-response to D-amphetamine challenge in rats treated chronically with phencyclidine, an NMDA receptor open-channel blocker.

References

[1] Alberati D, et al. Neuropharmacology. 2012, 62(2):1152-1161.
[2] Bugarski-Kirola D, et al. Eur Neuropsychopharmacol. 2014, 24(7):1024-1036.

Synonyms

Methanone, [4-[3-fluoro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl][5-(methylsulfonyl)-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]phenyl]-

Piperazine, 1-[3-fluoro-5-(trifluoromethyl)-2-pyridinyl]-4-[5-(methylsulfonyl)-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]benzoyl]-

[4-[3-Fluoro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl][5-(methylsulfonyl)-2-[(1S)-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

(S)-[4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-(methanesulfonyl)-2-(2,2,2-trifluoro-1-methylethoxy)phenyl]methanone

R 1678

Bitopertin

Ro 4917939

RG 1678

[4-[3-Fluoro-5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]-[5-methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanone