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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-Aticaprant
Aticaprant

Chemical Structure : Aticaprant

CAS No.: 1174130-61-0

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Aticaprant (CERC-501, JSPA 0658, LY2456302)

货号: PC-62110Not For Human Use, Lab Use Only.

LY 2456302 (CERC-501, JSPA 0658, Aticaprant) is a potent, selective, short-acting antagonist of κ-opioid receptor (KOR) with Ki of 0.81 nM.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 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

LY 2456302 (CERC-501, JSPA 0658, Aticaprant) is a potent, selective, short-acting antagonist of κ-opioid receptor (KOR) with Ki of 0.81 nM.
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) displays >30-fold selectivity over MOR and DOR.
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) selectively and potently occupies central kappa opioid receptors in vivo (ED50=0.33 mg/kg).
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) produces antidepressant-like effects in the mouse forced swim test and enhanced the effects of imipramine and citalopram.
LY 2456302 (CERC-501, JSPA 0658, Aticaprant) shows orally-bioavailablilty and excellent pharmacokinetic properties.

物理化学性质&存储条件

分子量 418.512
分子式 C26H27FN2O2
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

4-(4-(((2S)-2-(3,5-dimethylphenyl)-1-pyrrolidinyl)methyl)phenoxy)-3-fluoro-benzamide

参考文献

1. Rorick-Kehn LM, et al. Neuropharmacology. 2014 Feb;77:131-44.

2. Jackson KJ, et al. Neuropharmacology. 2015 Oct;97:270-4.

3. Naganawa M, et al. J Pharmacol Exp Ther. 2016 Feb;356(2):260-6.

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