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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $350 | In Stock | |
5 mg | $828 | In Stock | |
10 mg | $1,130 | In Stock | |
25 mg | $1,590 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,500 | In Stock | |
500 mg | $4,900 | In Stock |
Description | 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. |
Targets&IC50 | μ opioid receptor:16.49 nM(Ki ), [35S]-GTPγS:19.6 nM(EC50), [35S]-GTPγS:34.7 nM(EC50), Nociception:3.67 nM(Ki ) |
In vivo | AT-121 (0.003-0.03 mg/kg; s.c.; rhesus monkeys) decreases capsaicin-induced thermal allodynia dose-dependently without increasing scratching activity or inducing hyperalgesia, a marker of tolerance development, in doses of 0.01 or 0.03 mg/kg in rhesus monkeys. [1] |
Molecular Weight | 462.65 |
Formula | C24H38N4O3S |
Cas No. | 2099681-31-7 |
Smiles | O=C1C2(C=3C(CN1CCNS(N)(=O)=O)=CC=CC3)CCN(CC2)[C@@H]4CC[C@H]([C@H](C)C)CC4 |
Relative Density. | 1.25 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | 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 | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Chloroform/DMSO
DMSO
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