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SB-612111

  Cat. No.:  DC22415   Featured
Chemical Structure
371980-98-2
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More than 5000 active chemicals with high quality for research!
Field of application
SB-612111 is a potent, selective nociceptin/orphanin FQ receptor (NOP receptor) antagonist with Ki of 0.33 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 371980-98-2
Chemical Name: 7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride
Synonyms: 7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride;(5S,7S)-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-1-methyl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ol,hydrochloride;SB612111;(5S,7S)-7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol
SMILES: Cl.ClC1=CC=CC(Cl)=C1C1CCN(CC2CCC3=C(C=CC=C3C(O)C2)C)CC1
Formula: C24H30Cl3NO
M.Wt: 454.860104084015
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
Target: Ki: 0.33 nM (hORL-1) Ki: 57.6 nM (μ-receptor); 160.5 nM (κ-receptor); 2109 nM (δ-receptor)[1]
In Vivo: SB-612111 (intravenous injection; 0.6-10 nmol/mouse) antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg[1]. SB-612111 (intravenous injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected[1]. Animal Model: Male rats[1] Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg Administration: Intravenous injection; single dose Result: Had antihyperalgesic effects on carrageenan-induced rat paw.
References: [1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).J Pharmacol Exp Ther. 2004 Feb;308(2):454-61.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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