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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-Remlifanserin
Remlifanserin

Chemical Structure : Remlifanserin

CAS No.: 2289704-13-6

Remlifanserin (ACP-204, ACP204)

货号: PC-25028Not For Human Use, Lab Use Only.

Remlifanserin (ACP-204, ACP204) is a potent, selective 5-HT2A serotonin receptor inverse agonist with Ki of 0.14 nM, acts as an antagonist/inverse agonist and has potencies of 0.3-0.5 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Remlifanserin (ACP-204, ACP204) is a potent, selective 5-HT2A serotonin receptor inverse agonist with Ki of 0.14 nM, acts as an antagonist/inverse agonist and has potencies of 0.3-0.5 nM.
ACP-204 did not have any appreciable functional activity (off-target effects) against 19 other monoamine targets at 5 uM.
ACP-204 reduced the potential to impact ion channels important in cardiovascular function compared with pimavanserin.
ACP-204 potently suppressed DOI-induced head twitches in mice and rats with minimum effective SC doses of 0.1 and 0.3 mg/kg, respectively.
ACP-204 achieved nearly complete suppression in mice and rats at SC doses of 0.3 and 1 mg/kg, respectively, and at an oral dose of 3 mg/kg in rats.
ACP-204 suppressed MK-801–induced locomotor activity in mice with a minimum effective dose of 0.1 mg/kg.

物理化学性质&存储条件

分子量 429.51
分子式 C24H29F2N3O2
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-(4-cyclopropoxybenzyl)-1-(2,4-difluorobenzyl)-1-(1-methylpiperidin-4-yl)urea

参考文献

1. Patent WO2019040107 A1.

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