Bitopertin (RG1678, RO4917838) | GlyT1 inhibitor, Nrf2 activator

Chemical Structure : Bitopertin

CAS No.: 845614-11-1

Catalog No.: PC-42706Not For Human Use, Lab Use Only.

Bitopertin (RG1678, RO4917838) is a potent and selective glycine uptake GlyT1 inhibitor with EC50 of 30 nM, also is an Nrf2 activator.

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Biological Activity

Bitopertin (RG1678, RO4917838) is a potent and selective glycine uptake GlyT1 inhibitor with EC50 of 30 nM, also is an Nrf2 activator.

Bitopertin shows no activity for GlyT2, hERG, CYP450 enzymes above 10 uM.

Bitopertin shows brain penetratione and excellent pharmacokinetic in vivo.

Bitopertin suppresses osteoclast differentiation and ameliorates ovariectomy-induced bone loss by activating Nrf2.

Bitopertin interacts with the Keap1 Kelch domain and decreases Keap1-Nrf2 binding, leading to reduced Nrf2 ubiquitination and degradation.

M.Wt	543.455
Formula	C21H20F7N3O4S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Methanone, [4-[3-fluoro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl][5-(methylsulfonyl)-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]phenyl]-

1. Pinard E, et al. J Med Chem. 2010 Jun 24;53(12):4603-14.

2. Alberati D, et al. Neuropharmacology. 2012 Feb;62(2):1152-61

3. Martin-Facklam M, et al. Neuropsychopharmacology. 2013 Feb;38(3):504-12.