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TP-040 | TP-040 : Inhibitor of OGA
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
OGA
  • IC50:46 nM
  • EC50:450 nM
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family - HEXB IC50 > 10 µM (> 210-fold). Selectivity outside target family ...

Potency
Cellular
In Vitro

OGA

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c01712

In Vivo Validations

Mouse
Dose: 30 mg/Kg
Route of delivery: Oral
Organ of interest (O): Brain
Target engagement assay: Brain penetrant: Brain-to-plasma unbound concentration ratio (Kp,uu) 0.25 after 30 min and 0.35 after 1 h. Unbound fraction in plasma (fu,plasma) and brain (fu,brain) of 0.53 and 0.14, respectively. after 1 h: c(plasma) 1.9 µg/ml and c(brain) 2.6 µg/ml were observed

DOI Reference: 10.1021/acs.jmedchem.0c01712

Negative Control Compounds

CANSAR3550548
Notes: TP-040n: Human OGA enzymatic assay: IC50 > 10 µM

Chemical Information

Molecular Formula C15H22N6
SMILEs CC1CCN(c2ccnc(NCc3cn(C)cn3)n2)CC1
InChI InChI=1S/C15H22N6/c1-12-4-7-21(8-5-12)14-3-6-16-15(19-14)17-9-13-10-20(2)11-18-13/h3,6,10-12H,4-5,7-9H2,1-2H3,(H,16,17,19)
Molecular weight 286.19 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 43

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Expert Reviews

No SERP comments found for TP-040

Probe TP-040 is in the process of SERP review.

Please continue to check back for new reviews and commentary.