O-GlcNAcase-IN-6
O-GlcNAcase-IN-6 is an orally active, blood-brain barrier-permeable O-GlcNAcase (OGA) inhibitor with an IC50 of 5.4 nM. O-GlcNAcase-IN-6 inhibits OGA activity, thereby increasing the level of O-GlcNAc glycosylation in brain tissues. O-GlcNAcase-IN-6 can be used for the research of Alzheimer's disease.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2407072-65-3
- Formule: C20H25N5O
- Masse moléculaire:351.45
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
In Vitro
O-GlcNAcase-IN-6 (Compound 24) potently inhibits human OGA by directly binding to the active site of the enzyme, with an IC50 value of 5.4 nM[1].
O-GlcNAcase-IN-6 inhibits OGA activity in HEK293 cells with an IC50 of 26 nM[1].
O-GlcNAcase-IN-6 exhibits low in vitro MDR1-MDCK permeability of 0.7 × 10-6 cm/s, a high P-glycoprotein (PgP) efflux ratio (> 28), a free plasma protein binding rate of 0.61, and a free brain tissue binding rate of 0.24[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CD1 mice (male)[1]
-
Dosage:100 mg/kg
-
Administration:p.o.; single dose
-
Result:Induced a transient elevation of brain O-GlcNAcylation levels, peaking at 8 hours post-administration.
Reached a peak increase similar to the 3-3.5-fold increase observed with the reference compound Thiamet-G (500 mg/kg).
Showed measurable brain exposure, with an AUC(brain)/AUC(plasma) ratio of 0.16 and an unbound brain-to-plasma partition coefficient (Kp,uu) of 0.07.
Chemical Information
-
CAS No. 2407072-65-3
-
Masse moléculaire 351.45
-
Formule C20H25N5O
-
SMILES
CC1=C(C(C(C)C)=NC=C1)NC2=C3C=CN(C3=CC=N2)CC(N(C)C)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
O-GlcNAcase-IN-6 Related Classifications
HY-183557 Related Classifications
Powered by Bioz