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Chemical Structure : Iclepertin
CAS No.: 1421936-85-7
Catalog No.: PC-38397Not For Human Use, Lab Use Only.
Iclepertin (BI 425809) is a potent, selective and oral glycine transporter 1 (GlyT1) inhibitor with IC50 of 5.2 nM in rat primary neurons and 5.0 nM in human SK‐N‐MC cells (3H‐glycine uptake).
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|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $548 | In stock | |
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| 100 mg | Get quote |
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Iclepertin (BI 425809) is a potent, selective and oral glycine transporter 1 (GlyT1) inhibitor with IC50 of 5.2 nM in rat primary neurons and 5.0 nM in human SK‐N‐MC cells (3H‐glycine uptake).
BI 425809 displays no activity of BI 425809 against the related glycine transporter GlyT2, nor against other off‐targets.
Oral administration of BI 425809 in rats induced a dose‐dependent increase of glycine CSF levels from 30% (0.2 mg/kg, not significant) to 78% (2 mg/kg, P < 0.01), relative to vehicle.
Iclepertin (BI 425809) has been developed for the treatment of cognitive impairment associated with schizophrenia and AD.
| M.Wt | 512.423 | |
| Formula | C20H18F6N2O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
[5-(methanesulfonyl)-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}phenyl]{(1R,5R)-1-[5-(trifluoromethyl)-1,2-oxazol-3-yl]-3-azabicyclo[3.1.0]hexan-3-yl}methanone |
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1. Moschetti V, et al. Clin Drug Investig. 2018 Aug;38(8):737-750.
2. Rosenbrock H, et al. Clin Transl Sci. 2018 Nov;11(6):616-623.
3. Moschetti V, et al. Eur J Drug Metab Pharmacokinet. 2018 Apr;43(2):239-249.
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