RLX-33

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RLX-33 是一种有效且具有选择性和血脑屏障透过性的松弛素家族肽 3 (RXFP3) 拮抗剂，也阻断松弛素 3 (relaxin 3) 诱导的 ERK1/2 磷酸化，对 RXFP3、以及 ERK1 和 ERK2 磷酸化的 IC50 分别为 2.36 μM、7.82 μM 和 13.86 μM。RLX-33 能阻断 RXFP3 选择性激动剂 R3/I5 诱导的大鼠食物摄取增加。RLX-33 可用于代谢综合征的研究。

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.

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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).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.

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Others

Other Targets

RXFP receptor | ERK

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2784577-71-3

462.89

C24H19ClN4O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (270.04 mM; 超声助溶 )

N(C(=O)C1CN(CC2=CC=CO2)C(=O)C1)C3=CC=C(C4=NC(=NO4)C5=CC=C(Cl)C=C5)C=C3

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(-20℃)

With Ice Pack

≥ 2 years