RLX-33

• CAT Number: I043322
• CAS Number: 2784577-71-3
• Molecular Formula: C24H19ClN4O4
• Molecular Weight: 462.89
• Purity: ≥95%
• Synonyms: N-[4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]phenyl]-1-(furan-2-ylmethyl)-5-oxopyrrolidine-3-carboxamide
• 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)
• InChIKey: LTOAWFRZXVPHAJ-UHFFFAOYSA-N
• SMILES: C1C(CN(C1=O)CC2=CC=CO2)C(=O)NC3=CC=C(C=C3)C4=NC(=NO4)C5=CC=C(C=C5)Cl

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].
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

Reference

[1]. https://pubmed.ncbi.nlm.nih.gov/35594150/
 [Content Brief]