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BIIE0246 | Antagonist of NPY2R
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
NPY2R
  • IC50:3.3 nM
Antagonist
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
Selectivity vs family members was assessed on rat homologs using radioligand binding assay in HEK ...

Potency
Cellular
In Vitro

NPY2R

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/sj.bjp.0703162

In Vivo Validations

Mouse, Rat, Rabbit
Dose: 3 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: <3h

DOI Reference: 10.1038/sj.bjp.0703162

Negative Control Compounds

BIIE0212

Chemical Information

Molecular Formula C49H57N11O6
SMILEs N=C(N)NCCC[C@H](NC(=O)CC1(CC(=O)N2CCN(C3c4ccccc4NC(=O)c4ccccc43)CC2)CCCC1)C(=O)NCCn1c(=O)n(-c2ccccc2)n(-c2ccccc2)c1=O
InChI InChI=1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45(64)52-26-27-58-47(65)59(34-14-3-1-4-15-34)60(48(58)66)35-16-5-2-6-17-35)54-41(61)32-49(23-11-12-24-49)33-42(62)56-28-30-57(31-29-56)43-36-18-7-8-19-37(36)44(63)55-39-21-10-9-20-38(39)43/h1-10,14-21,40,43H,11-13,22-33H2,(H,52,64)(H,54,61)(H,55,63)(H4,50,51,53)/t40-,43?/m0/s1
Molecular weight 895.45 Da
AlogP 3.49427
HBond acceptors 17
HBond donors 7
Atoms 123

Vendors

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Expert Reviews

by SERP
(on 7 Jul 2021 )
Cellular Use Rating
In Model Organisms
For in vivo CNS studies inject intrathecally or directly in region of interest.
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
Consult opnME (Boehringer Ingelheim) for further in depth ADME and selectivity data. Due to the poor reported solubility, permeability, moderate metabolic stability (and PPB), BIIE0246 is not recommended...
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