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ROLAPITANT | ROLAPITANT : Antagonist of TACR1
RATINGS:
Cellular Use: (0 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
TACR1
  • Ki:0.66 nM
Antagonist
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: >1000-fold for the human NK1 receptor compared to the human NK2 an ...

Potency
Cellular
In Vitro

TACR1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.pbb.2012.03.021

In Vivo Validations

Gerbils
Dose: 0.3 mg/kg, 1.0 mg/Kg IV, o.3 mg/Kg PO
Route of delivery: Intravenous, Oral
Target engagement assay: Intravenous rolapitant (0.3 and 1 mg/kg) dose-dependently blocked the foot tapping induced byGR-73632 with complete blockade observed at 1 mg/kg, iv.

DOI Reference: 10.1016/j.pbb.2012.03.021

Chemical Information

Molecular Formula C25H26F6N2O2
InChI InChI=1S/C25H26F6N2O2/c1-16(17-11-19(24(26,27)28)13-20(12-17)25(29,30)31)35-15-23(18-5-3-2-4-6-18)10-9-22(14-32-23)8-7-21(34)33-22/h2-6,11-13,16,32H,7-10,14-15H2,1H3,(H,33,34)/t16-,22-,23-/m1/s1
Molecular weight 500.19 Da
AlogP 0.0
HBond acceptors 4
HBond donors 2
Atoms 61

References

Publications

Cross References

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Expert Reviews

No SERP comments found for ROLAPITANT

Probe ROLAPITANT is in the process of SERP review.

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