| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 2.36 μM (RXFP3), 7.82 μM (ERK1 phosphorylation), 13.86 μM (ERK2 phosphorylation) | ||||||||||||
| 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]. | ||||||||||||
| Name | RLX-33 | ||||||||||||
| CAS | 2784577-71-3 | ||||||||||||
| Formula | C24H19ClN4O4 | ||||||||||||
| Molar Mass | 462.89 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. https://pubmed.ncbi.nlm.nih.gov/35594150/ |