Iclepertin (BI 425809) | GlyT1 inhibitor | Probechem Biochemicals

Chemical Structure : Iclepertin

CAS No.: 1421936-85-7

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Iclepertin (BI 425809, BI-425809)

货号: 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	￥3580	In stock
10 mg	￥5480	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	512.423
分子式	C20H18F6N2O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

Iclepertin (BI 425809, BI-425809)

生物&药学活性

物理化学性质&存储条件

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Iclepertin (BI 425809, BI-425809)

生物&药学活性

物理化学性质&存储条件

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