DAPORINAD | DAPORINAD : Inhibitor of NAMPT
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NAMPT
  • Ki:0.3 nM
  • IC50:1-3 nM
  • IC50:1.6 nM
  • IC50:7.4 nM
Inhibitor
up to 100 nM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
Clonogenic Assay in a Selection of Cancer Cell Lines shows little selectivity for DAPORINAD DOI: 10 ...

Potency
Cellular
In Vitro

NAMPT

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

PMID Reference: 14612543

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 52.9 min
Systemic clearance: 29.29 mL/min/kg
Cmax: 5476.2 ng/mL
Area Under the Curve:: 171,690 min∙ng/mL
Volume of Distribution at Steady-State: 897.1 mL/Kg

DOI Reference: 10.3390/molecules27062011

Dose: 10 mg/Kg
Route of delivery: Intravenous
Plasma half life: 50.5 min
Systemic clearance: 28.1 mL/min/kg
Cmax: 14,872 ng/mL
Area Under the Curve:: 357,205 min∙ng/mL
Volume of Distribution at Steady-State: 646.6 mL/Kg

DOI Reference: 10.3390/molecules27062011

Dose: 30 mg/Kg
Route of delivery: Intravenous
Plasma half life: 40.8 min
Systemic clearance: 17.9 mL/min/kg
Cmax: 48,059 ng/mL
Area Under the Curve:: 1,763,266 min∙ng/mL
Volume of Distribution at Steady-State: 535.8 mL/Kg

DOI Reference: 10.3390/molecules27062011

Chemical Information

Molecular Formula C24H29N3O2
SMILEs O=C(/C=C/c1cccnc1)NCCCCC1CCN(C(=O)c2ccccc2)CC1
InChI InChI=1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+
Molecular weight 391.23 Da
AlogP 3.9337000000000035
HBond acceptors 5
HBond donors 1
Atoms 58

References

Cross References

Vendors

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Expert Reviews


No SERP comments found for DAPORINAD

Probe DAPORINAD is in the process of SERP review.

Please continue to check back for new reviews and commentary.