AT-121

A dual μ-opioid and nociceptin receptor partial agonist

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库存: 现货

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100ug

￥1012.00

810.00

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500ug

￥4525.00

3620.00

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1mg

￥7550.00

6040.00

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货号: ajci69972
CAS: 2099681-31-7
别名:
分子式: C24H38N4O3S
分子量: 462.6
纯度: >98%
溶解度: Chloroform: 10 mg/ml,DMF: miscible,DMSO: miscible,Ethanol: miscible,Ethanol:PBS (pH 7.2) (1:20): 50μ g/ml
储存: Store at -20°C
库存: 现货

Background

AT-121 is a dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing μ-opioid or nociceptin receptors (EC50s = 19.6 and 34.7 nM, respectively). AT-121 (0.003-0.03 mg/kg) decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner. It lacks reinforcing effects, a marker of abuse potential, and reduces oxycodone, but not food pellet, reinforcement in a drug self-administration assay in rhesus monkeys when administered at doses ranging from 0.3 to 10 μg/kg per injection. AT-121 (0.01 or 0.03 mg/kg) does not induce hyperalgesia, a marker of tolerance development, in rhesus monkeys.