产品
编 号：F741810
分子式：C24H19ClN4O4
分子量：462.89
分子式：C24H19ClN4O4
分子量：462.89
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2784577-71-3
产品详情
生物活性：
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.
体内研究：
RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats.RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma.Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg).plasma brain
Cmax (ng/mL)14011552
tmax (h)0.52.0
t1/2 (h)1.94.9
AUCinf (ng/mL·h)535212519
CL_F (mL/min/kg)43.8
Animal Model:Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake
Dosage:10 mg/kg
Administration:IP, single dosage
Result:Attenuated the R3/I5-induced increase in food intake.
Animal Model:Male Wistar rats
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.
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.
体内研究：
RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats.RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma.Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg).plasma brain
Cmax (ng/mL)14011552
tmax (h)0.52.0
t1/2 (h)1.94.9
AUCinf (ng/mL·h)535212519
CL_F (mL/min/kg)43.8
Animal Model:Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake
Dosage:10 mg/kg
Administration:IP, single dosage
Result:Attenuated the R3/I5-induced increase in food intake.
Animal Model:Male Wistar rats
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.
产品资料
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