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AT-121

AT-121
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.
Catalog No. T37610Cas No. 2099681-31-7
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Purity:97.95%
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AT-121

Purity: 97.95%
Catalog No. T37610Cas No. 2099681-31-7

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.
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Pack SizePriceAvailabilityQuantity
1 mg$350In Stock
5 mg$828In Stock
10 mg$1,130In Stock
25 mg$1,590In Stock
50 mg$1,980In Stock
100 mg$2,500In Stock
500 mg$4,900In Stock
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight462.65
FormulaC24H38N4O3S
Cas No.2099681-31-7
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.1615 mL10.8073 mL21.6146 mL108.0731 mL
5 mM0.4323 mL2.1615 mL4.3229 mL21.6146 mL
10 mM0.2161 mL1.0807 mL2.1615 mL10.8073 mL
DMSO
1mg5mg10mg50mg
20 mM0.1081 mL0.5404 mL1.0807 mL5.4037 mL
50 mM0.0432 mL0.2161 mL0.4323 mL2.1615 mL
100 mM0.0216 mL0.1081 mL0.2161 mL1.0807 mL

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