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

Chemical Structure : Mesdopetam hemitartrate

CAS No.: 2562346-14-7

Mesdopetam hemitartrate (IRL790, IRL-790)

货号: PC-47115Not For Human Use, Lab Use Only.

Mesdopetam (IRL790) is a novel dopamine transmission modulator and dopamine D3 receptor antagonist with Ki/IC50 of 0.09/0.41 uM.

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

生物&药学活性

Mesdopetam hemitartrate (IRL790) is a novel dopamine transmission modulator and dopamine D3 receptor antagonist with Ki/IC50 of 0.09/0.41 uM.
IRL790 also shows sub-micromolar affinities at DA D2 and σ1 receptors, and micromolar affinities at 5-HT1a, 5-HT2a, and 5-HT7 receptors, does not show any agonist-like properties at D2, D3, 5-HT2, or 5-HT7 receptors.
IRL790 displays balancing effects on aberrant motor phenotypes, reducing l-DOPA-induced dyskinesias in the rodent 6-hydroxydopamine lesion model and reducing psychostimulant-induced locomotor hyperactivity elicited by pretreatment with either d-amphetamine or dizocilpine, without negatively impacting normal motor performance.
IRL790 is active in models of perturbed dopaminergic and glutamatergic signaling, including rodent 6-hydroxydopamine l-DOPA-induced dyskinesias and psychostimulant-induced hyperactivity, in a dose range that does not impair normal behavior.

物理化学性质&存储条件

分子量 700.77
分子式 C12H18FNO3S.1/2C4H6O6
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

1-Propanamine, N-[2-[3-fluoro-5-(methylsulfonyl)phenoxy]ethyl]-, (2R,3R)-2,3-dihydroxybutanedioate (2:1)

参考文献

1. Waters S, et al. J Pharmacol Exp Ther. 2020 Jul;374(1):113-125.

2. Becanovic K, et al. J Pharmacol Exp Ther. 2020 Jul;374(1):126-133.

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