1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. SB-612111 hydrochloride

SB-612111 hydrochloride 

Cat. No.: HY-18617
Handling Instructions

SB-612111 hydrochloride 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 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

For research use only. We do not sell to patients.

SB-612111 hydrochloride Chemical Structure

SB-612111 hydrochloride Chemical Structure

CAS No. : 371980-94-8

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Description

SB-612111 hydrochloride 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 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].

IC50 & 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 hydrochloride (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 hydrochloride (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.
Molecular Weight

454.86

Formula

C₂₄H₃₀Cl₃NO

CAS No.

371980-94-8

SMILES

O[[email protected]@H]1C[[email protected]](CN2CCC(C3=C(Cl)C=CC=C3Cl)CC2)CCC4=C(C)C=CC=C41.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SB-612111SB612111SB 612111Opioid ReceptorantinociceptivethermalhyperalgesiapainCHOHEK293AntihyperalgesicInhibitorinhibitorinhibit

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SB-612111 hydrochloride
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HY-18617
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