BI-425809


Catalog No. Size PriceQuantity
M17591-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

BI-425809 is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. BI-425809 is inactive against GlyT2. BI-425809 can be used for Alzheimer disease and schizophrenia research.

Product information

CAS Number: 1421936-85-7

Molecular Weight: 512.42

Formula: C20H18F6N2O5S

Chemical Name: (1R, 5R)-3-(5-methanesulfonyl-2-{[(2R)-1, 1, 1-trifluoropropan-2-yl]oxy}benzoyl)-1-[5-(trifluoromethyl)-1, 2-oxazol-3-yl]-3-azabicyclo[3.1.0]hexane

Smiles: C[C@@H](OC1=CC=C(C=C1C(=O)N1C[C@@H]2C[C@@]2(C1)C1C=C(ON=1)C(F)(F)F)S(C)(=O)=O)C(F)(F)F

InChiKey: MYHDQTVHHMSLEF-DDBGAENHSA-N

InChi: InChI=1S/C20H18F6N2O5S/c1-10(19(21,22)23)32-14-4-3-12(34(2,30)31)5-13(14)17(29)28-8-11-7-18(11,9-28)15-6-16(33-27-15)20(24,25)26/h3-6,10-11H,7-9H2,1-2H3/t10-,11+,18+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BI 425809 inhibits GlyT1 with the IC50 values of 5.2 nM in rat primary neurons and 5.0 nM in human SK-N-MC cells.

In Vivo:

Single oral administration of BI 425809 induced a dose-dependent increase of glycine cerebrospinal fluid (CSF) levels. 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), relative to vehicle.

Products are for research use only. Not for human use.

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