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

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (SB-612111 hydrochloride) usually boasts enhanced water solubility and stability.

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

SB-612111 Chemical Structure

SB-612111 Chemical Structure

CAS No. : 371980-98-2

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Description

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[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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

418.40

Formula

C24H29Cl2NO
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SB-612111 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-612111371980-98-2SB612111SB 612111Opioid ReceptorantinociceptivethermalhyperalgesiapainCHOHEK293AntihyperalgesicInhibitorinhibitorinhibit

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