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。
| 生物活性 | RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrantrelaxin family peptide 3 (RXFP3)antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, withIC50values of 2.36 μM for RXFP3, 7.82 and 13.86 μM forERK1andERK2phosphorylation, 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]. |
| IC50& Target | IC50: 2.36 μM (RXFP3), 7.82 μM (ERK1 phosphorylation), 13.86 μM (ERK2 phosphorylation)[1] |
体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(270.04 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1603 mL | 10.8017 mL | 21.6034 mL | | 5 mM | 0.4321 mL | 2.1603 mL | 4.3207 mL | | 10 mM | 0.2160 mL | 1.0802 mL | 2.1603 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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