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Cat. No.: HY-183557

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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.

For research use only. We do not sell to patients.

CAS No.: 2407072-65-3
Formula: C₂₀H₂₅N₅O
Molecular Weight:351.45

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

O-GlcNAcase-IN-6 Chemical Structure

CAS No.: 2407072-65-3

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Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Bioz

Biological Activity

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

Species	Dose	Route	C₀	T_1/2	V_dss	CL	AUC_0-inf	C_max	T_max	Bioavailability
Mice^[1]	1 mg/kg	i.v.	794 ng/mL	1.02 h	2.1 L/kg	50 mL/min/kg	338 ng·h/mL	/	/	/
Mice^[1]	5 mg/kg	p.o.	/	1.7 h	/	/	1793 ng·h/mL	697 ng/mL	0.5 h	100 %

In Vivo

O-GlcNAcase-IN-6 (Compound 24) (100 mg/kg; p.o.; single dose) induces a transient, significant elevation of brain O-GlcNAcylation levels in male CD1 mice, confirming in vivo OGA target engagement^[1].

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
Molecular Weight 351.45
Formula C₂₀H₂₅N₅O
SMILES

CC1=C(C(C(C)C)=NC=C1)NC2=C3C=CN(C3=CC=N2)CC(N(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bouton J, et al. Discovery of 5‑Azaindole Inhibitors of O‑GlcNAcase for the Treatment of Alzheimer's Disease and Related Tauopathies. ACS Med Chem Lett. 2026;17(5):1096-1105. Published 2026 Apr 23. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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