SB-612111
Based on 2 publication(s) in Google Scholar
SB-612111 is a novel and potent 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.
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- CAS. Nr.: 371980-98-2
- Formel: C24H29Cl2NO
- Molecular Weight:418.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) SB-612111
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Biologische Aktivität
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NOP Receptor/ORL1 |
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | CC50 |
3.67 μM
Compound: SB-612111
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
0.77 μM
Compound: SB-612111
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats[1]
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Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg
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Administration:Intravenous injection; single dose
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Result:Had antihyperalgesic effects on carrageenan-induced rat paw.
Chemical Information
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CAS. Nr. 371980-98-2
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Molecular Weight 418.40
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Formel C24H29Cl2NO
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SMILES
O[C@H]1C[C@@H](CN2CCC(C3=C(Cl)C=CC=C3Cl)CC2)CCC4=C(C)C=CC=C41
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Neurotherapeutics
LY2940094, an NOPR antagonist, promotes oligodendrocyte generation and myelin recovery in an NOPR independent manner. [Abstract]2024 Sep;21(5):e00424. PMID: 39004556 -
Biochem Biophys Res Commun
SLL-023ACP, a KOR/MOR dual agonist, produces potent antinociception with fewer side effects. [Abstract]2026 Mar 26:806:153411. PMID: 41653647
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SB-612111 Related Classifications
HY-18618 Related Classifications
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