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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-LY3154207
LY3154207

Chemical Structure : LY3154207

CAS No.: 1638667-79-4

LY3154207 (Mevidalen, LY-3154207)

货号: PC-73068Not For Human Use, Lab Use Only.

LY3154207 (Mevidalen, LY-3154207) is a potent, and subtype selective human dopamine D1 positive allosteric modulator (PAM) with EC50 of 3.0 nM.

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5 mg ¥3680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LY3154207 (Mevidalen, LY-3154207) is a potent, and subtype selective human dopamine D1 positive allosteric modulator (PAM) with EC50 of 3.0 nM.
LY3154207 displays exquisite selectivity over the human D5 receptor subtype (EC50>10 uM), and 14 other GPCRs, including D2, β1, β2, and 5HT6 receptors.
Mevidalen enhanced wakefulness (latency to fall asleep) in the hD1 mouse in a dose dependent [3-100 mg/kg, orally (PO)] fashion.
Mevidalen promoted wakefulness in mice after prior sleep deprivation and delayed sleep onset by 5.5- and 15.2-fold compared with vehicle-treated animals.
Mevidalen demonstrated a dose-dependent increase in latency to sleep onset in human clinical investigations.

物理化学性质&存储条件

分子量 450.4
分子式 C24H29Cl2NO3
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

2-(2,6-dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one

参考文献

1. Hao J, et al. J Med Chem. 2019 Oct 10;62(19):8711-8732.

2. McCarthy AP, et al. J Pharmacol Exp Ther. 2022 Mar;380(3):143-152.

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