AT-121

TargetMol
Product Code: TAR-T37610
Supplier: TargetMol
CodeSizePrice
TAR-T37610-1mg1mg£352.00
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TAR-T37610-5mg5mg£736.00
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TAR-T37610-10mg10mg£978.00
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TAR-T37610-25mg25mg£1,348.00
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TAR-T37610-50mg50mg£1,661.00
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TAR-T37610-100mg100mg£2,079.00
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TAR-T37610-500mg500mg£4,006.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

1 / 1

Further Information

Bioactivity:
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.
CAS:
2099681-31-7
Formula:
C24H38N4O3S
Molecular Weight:
462.6
Pathway:
GPCR/G Protein|Endocrinology/Hormones|Neuroscience
Purity:
0.98
SMILES:
CC(C)[C@@H]1CC[C@H](N2CCC3(C(N(CCNS(N)(=O)=O)CC4=C3C=CC=C4)=O)CC2)CC1
Target:
Opioid Receptor

References

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