A dual μ-opioid and nociceptin receptor partial agonist
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AT-121

Item No. 26150

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[1,2-dihydro-1'-[cis-4-(1-methylethyl)cyclohexyl]-3-oxospiro[isoquinoline-4(3H),4'-piperidin]-2-yl]ethyl]-sulfamide
CAS Number
2099681-31-7
Molecular Formula
C24H38N4O3S
Formula Weight
462.6
Purity
≥95%
Formulation
A 1 mg/ml solution in chloroform
Solubility(Learn about Variance in Solubility)
Chloroform: 10 mg/mlDMF: miscibleDMSO: miscibleEthanol: miscibleEthanol:PBS (pH 7.2) (1:20): 50µg/ml
SMILES
CC(C)[C@@H]1CC[C@H](N2CCC3(C(N(CCNS(N)(=O)=O)CC4=C3C=CC=C4)=O)CC2)CC1
InChi Code
InChI=1S/C24H38N4O3S/c1-18(2)19-7-9-21(10-8-19)27-14-11-24(12-15-27)22-6-4-3-5-20(22)17-28(23(24)29)16-13-26-32(25,30)31/h3-6,18-19,21,26H,7-17H2,1-2H3,(H2,25,30,31)/t19-,21+
InChi Key
LIZMNXKYQXVRSS-TYKWCNGQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 µg

    $69

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    500 µg

    $297

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    1 mg

    $493

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    Product Description

    AT-121 is a dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ding, H., Kiguchi, N., Yasuda, D., et al. A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates. Sci. Transl. Med. 10(456), eaar3483 (2018).