| Identification | Back Directory | [Name]
3-Pyrrolidinecarboxamide, N-[4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]phenyl]-1-(2-furanylmethyl)-5-oxo- | [CAS]
2784577-71-3 | [Synonyms]
3-Pyrrolidinecarboxamide, N-[4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]phenyl]-1-(2-furanylmethyl)-5-oxo-
N-{4-[3-(4-Chlorophenyl)-1,2,4-oxadiazol-5-yl]phenyl}-1-[(furan-2-yl)methyl]-5-oxopyrrolidine-3-carboxamide | [Molecular Formula]
C24H19ClN4O4 | [MOL File]
2784577-71-3.mol | [Molecular Weight]
462.89 |
| Hazard Information | Back Directory | [Uses]
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome[1]. | [in vivo]
RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats[1].
RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma[1].
Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg)[1].
| plasma | brain | | Cmax (ng/mL) | 1401 | 1552 | | tmax (h) | 0.5 | 2.0 | | t1/2 (h) | 1.9 | 4.9 | | AUCinf (ng/mL·h) | 5352 | 12519 | | CL_F (mL/min/kg) | 43.8 | |
| Animal Model: | Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake[1] | | Dosage: | 10 mg/kg | | Administration: | IP, single dosage | | Result: | Attenuated the R3/I5-induced increase in food intake. |
| Animal Model: | Male Wistar rats[1] | | Dosage: | 10 mg/kg | | Administration: | IP, single dosage (Pharmacokinetic Analysis) | | Result: | Exhibited a good brain penetration and highly protein-bound, with protein binding of 99.8% in rat plasma. |
| [References]
[1] https://pubmed.ncbi.nlm.nih.gov/35594150/ DOI:10.1021/acs.jmedchem.2c00508 |
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