| Identification | Back Directory | [Name]
Sulfamide, N-[2-[1,2-dihydro-1'-[cis-4-(1-methylethyl)cyclohexyl]-3-oxospiro[isoquinoline-4(3H),4'-piperidin]-2-yl]ethyl]- | [CAS]
2099681-31-7 | [Synonyms]
AT 121,AT121
Sulfamide, N-[2-[1,2-dihydro-1'-[cis-4-(1-methylethyl)cyclohexyl]-3-oxospiro[isoquinoline-4(3H),4'-piperidin]-2-yl]ethyl]- | [Molecular Formula]
C24 H38 N4 O3 S | [MDL Number]
MFCD34469231 | [MOL File]
2099681-31-7.mol | [Molecular Weight]
462.65 |
| Chemical Properties | Back Directory | [Boiling point ]
650.6±65.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Chloroform: 10 mg/ml; DMF: miscible; DMSO: miscible; Ethanol: miscible; Ethanol:PBS (pH 7.2) (1:20): 50μg/ml | [form ]
Liquid | [pka]
10.81±0.60(Predicted) | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [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. | [Uses]
AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects[1]. | [in vivo]
AT-121 (0.003-0.03 mg/kg; s.c.) produces potent antinociceptive effect[1]. | Animal Model: | Adult male and female rhesus monkeys[1] | | Dosage: | 0.003-0.03 mg/kg | | Administration: | Subcutaneous | | Result: | Produced antinociceptive effects against an acute noxious stimulus, 50 °C water, in a dose-dependent.
|
| [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). |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
|