2784577-71-3
2784577-71-3 structure
- Name: RLX-33
- Chemical Name: RLX-33
- CAS Number: 2784577-71-3
- Molecular Formula: C24H19ClN4O4
- Molecular Weight: 462.89
- Catalog: Signaling Pathways MAPK/ERK Pathway ERK
- Create Date: 2022-09-04 15:24:14
- Modify Date: 2023-02-23 10:53:14
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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].
| Name | RLX-33 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 2.36 μM (RXFP3), 7.82 μM (ERK1 phosphorylation), 13.86 μM (ERK2 phosphorylation)[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 |
| Molecular Formula | C24H19ClN4O4 |
|---|---|
| Molecular Weight | 462.89 |