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SB-612111 | SB-612111 : NOP antagonist of OPRL1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
OPRL1
  • Ki:0.33 ± 0.03 nM
  • EC50:0.05 nM
Antagonist
300 nM, can be used up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - ORL-1 57.6 ± 8.0 nM

Potency Assay Off-Target:
Competitive radioligand binding assays using membranes prepared from clonal cell lines
Selectivity Assessment Description:
SB-612111 is highly selective versus μ-(174-fold), δ-(6391-fold), and κ (486-fold)-opioid recepto ...

Potency
Cellular
In Vitro

OPRL1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1124/jpet.103.055848

In Vivo Validations

Male Swiss albino and CD1/C57BL6/J-129 NOP+/+ and NOP–/– mice
Dose: 1-10 mg/Kg
Route of delivery: Intravenous, Oral

DOI Reference: 10.1124/jpet.103.055848

Chemical Information

Molecular Formula C24H29Cl2NO
SMILEs Cc1cccc2c1CC[C@H](CN1CCC(c3c(Cl)cccc3Cl)CC1)C[C@@H]2O
InChI InChI=1S/C24H29Cl2NO/c1-16-4-2-5-20-19(16)9-8-17(14-23(20)28)15-27-12-10-18(11-13-27)24-21(25)6-3-7-22(24)26/h2-7,17-18,23,28H,8-15H2,1H3/t17-,23-/m0/s1
Molecular weight 417.16 Da
AlogP 6.167320000000006
HBond acceptors 2
HBond donors 1
Atoms 57

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 25 Jul 2021 )
Cellular Use Rating
In Model Organisms
Note: SB-612111 appears to be slowly reversible. From Spagnolo 2007 “Apart from antagonist potency, the reversibility test conducted in the mouse vas deferens experiments demonstrated another important...
by SERP
(on 4 Aug 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 5 Aug 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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