RLX-33 |
RLX-33 : Allosteric antagonist of RXFP3
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| RXFP3 |
|
Allosteric
up to 10 uM
Selectivity
In Cell Selectivity Assessment
Potency Assay Off-Target:
Within target family:
RLX-33 had no detectable agonist activity (or antagonist activity at RXFP1 at ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Outside target family:
RLX-33 was assessed in radioligand binding assays against a panel of 45 GPCRs ...
Potency Cellular
In Vitro
RXFP3
Mode of Action: Allosteric
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.2c00508
In Vivo Validations
Rat
Dose: 10 mg/Kg
Route of delivery:
Intraperitoneal
Plasma half life:
1.9 (Plasma), 4.9 (Brain) h
Systemic clearance:
43.8 mL/min/Kg
Cmax:
1401 (Plasma), 1552 (Brain) ng/mL
Tmax:
0.5 (plasma), 2.0 (Brain) h
Area Under the Curve::
5352 (Plasma), 12519 (Brain) ng/mL*h
Target engagement assay:
brain/plasma ratio: 2.3
DOI Reference: 10.1021/acs.jmedchem.2c00508
Chemical Information
| Molecular Formula | C24H19ClN4O4 |
| SMILEs | O=C(Nc1ccc(-c2nc(-c3ccc(Cl)cc3)no2)cc1)C1CC(=O)N(Cc2ccco2)C1 |
| InChI | InChI=1S/C24H19ClN4O4/c25-18-7-3-15(4-8-18)22-27-24(33-28-22)16-5-9-19(10-6-16)26-23(31)17-12-21(30)29(13-17)14-20-2-1-11-32-20/h1-11,17H,12-14H2,(H,26,31) |
| Molecular weight | 462.11 Da |
| AlogP | 0.0 |
| HBond acceptors | 8 |
| HBond donors | 1 |
| Atoms | 52 |
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