Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 80,500 |
5 mg | 在庫あり | ¥ 190,000 |
10 mg | 在庫あり | ¥ 259,500 |
25 mg | 在庫あり | ¥ 365,000 |
50 mg | 在庫あり | ¥ 454,500 |
100 mg | 在庫あり | ¥ 574,000 |
500 mg | 在庫あり | ¥ 1,124,500 |
説明 | AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects. |
ターゲット&IC50 | Nociception:3.67 nM(Ki ), μ opioid receptor:16.49 nM(Ki ), [35S]-GTPγS:19.6 nM(EC50), [35S]-GTPγS:34.7 nM(EC50) |
In vivo |
AT-121 (0.003-0.03 mg/kg; s.c.; rhesus monkeys) decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner.[1] AT-121 (0.01 or 0.03 mg/kg) does not induce hyperalgesia, a marker of tolerance development, in rhesus monkeys.[1] |
分子量 | 462.65 |
分子式 | C24H38N4O3S |
CAS No. | 2099681-31-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (118.88 mM)
Chloroform: 9.0 mg/mL (19.4 mM)
DMF: Miscible
Ethanol: Miscible
Ethanol:PBS (pH 7.2) (1:20): 50 μg/mL
You can also refer to dose conversion for different animals. 詳細
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AT-121 2099681-31-7 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor AT121 AT 121 Inhibitor inhibitor inhibit