2. Neuronal Signaling
  3. OGA
  4. 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.

O-GlcNAcase-IN-6

O-GlcNAcase-IN-6 Chemical Structure

CAS No. : 2407072-65-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

O-GlcNAcase-IN-6 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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.

O-GlcNAcase-IN-6 Related Antibodies
Parmacokinetics
Species Dose Route C0 T1/2 Vdss CL AUC0-inf Cmax Tmax 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.
Molecular Weight

351.45

Formula

C20H25N5O
CAS No.
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

O-GlcNAcase-IN-6 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

O-GlcNAcase-IN-62407072-65-3OGAO-GlcNAc hydrolaseO-GlcNAcasebrain tissuemurine modelsMDR1-MDCKhuman liver microsomesmouse liver microsomesHEK293 cellsalzheimer’s diseasemale CD1 miceInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
O-GlcNAcase-IN-6
Cat. No.:
HY-183557
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.