产品说明书

Aticaprant

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Chemical Structure| 1174130-61-0 同义名 : CERC-501;Ly2456302;JNJ-67953964
CAS号 : 1174130-61-0
货号 : A354780
分子式 : C26H27FN2O2
纯度 : 99%+
分子量 : 418.5
MDL号 : MFCD22572355
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(250.89 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Aticaprant, also known as CERC-501, binds to the human kappa opioid receptor with high affinity, having a Ki value of 0.807 nM. Its affinity is 30 times greater for the human mu opioid receptor and 190 times greater for the human delta opioid receptor. Aticaprant shows no significant affinity for several non-opioid cell surface G-protein coupled receptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors, or ion channel/transport protein binding targets or the central benzodiazepine binding site[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.19mL

23.89mL

4.78mL

2.39mL

参考文献

[1]Rorick-Kehn LM, et al. LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44.

[2]Jackson KJ, et al. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302on nicotine withdrawal in mice. Neuropharmacology. 2015 Oct;97:270-4.