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首页-小分子抑制剂&激动剂-GPCR-Melatonin Receptor-ASP5633
ASP5633

Chemical Structure : ASP5633

CAS No.: 1536477-48-1

ASP5633 (ASP-5633)

货号: PC-26382Not For Human Use, Lab Use Only.

ASP5633 is potent, highly selective peripherally restricted melatonin MT1/MT2 receptor agonist with EC50 of 12.3, 18.6, 36.2 and 36.4 nM for human MT1, human MT2, rat MT1 and rat MT2 by Ca2+ flux assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ASP5633 is potent, highly selective peripherally restricted melatonin MT1/MT2 receptor agonist with EC50 of 12.3, 18.6, 36.2 and 36.4 nM for human MT1, human MT2, rat MT1 and rat MT2 by Ca2+ flux assays.
ASP5633 shows agonistic effects in human and rat MT1 and MT2 receptors without significant species differences in the assay using a Gqi chimeric protein to convert Gi signaling into intracellular Ca2+ responses.
ASP5633 shows no activity against a total of 56 receptors, ion channels, transporters and enzymes.
ASP5633 induced contraction of isolated rat urethral strips in a concentration-dependent manner (EC50=72 nM) in rat urethral strips, shows agonistic activity in MT1 receptor-mediated Gq signaling pathway.
ASP5633 (0.03–0.3 mg/kg) dose-dependently increased UPP with statistical significance at doses of 0.1 mg/kg in anesthetized rats.
ASP5633 increased urethral pressure in the bladder filling phase without affecting bladder pressure in either phase, or urethral pressure in the voiding phase.

物理化学性质&存储条件

分子量 307.33
分子式 C15H18FN3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(2-acetamidoethyl)-6-fluoro-5-methoxy-N-methyl-1H-indole-2-carboxamide

参考文献

1. Matsui S, et al. Eur J Pharmacol. 2026 Mar 11;1019:178782.

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