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Cat. No.: HY-18617

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rel-SB-612111 hydrochloride

rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with K_i values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

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CAS No.: 371980-94-8
Formule: C₂₄H₃₀Cl₃NO
Masse moléculaire:454.86

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

Data Sheet (270 KB)

rel-SB-612111 hydrochloride Chemical Structure

CAS No.: 371980-94-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Pureté et documentation
Références
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Description

IC₅₀ & Target

NOP Receptor/ORL1

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In Vivo

rel-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].
rel-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].

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.

Chemical Information

CAS No. 371980-94-8
Masse moléculaire 454.86
Formule C₂₄H₃₀Cl₃NO
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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- IC₅₀ & Target
- In Vivo
Chemical Information
Pureté et documentation
Références

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rel-SB-612111 hydrochloride

Voir tous les produits spécifiques à Isoform Opioid Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

rel-SB-612111 hydrochloride Related Classifications

HY-18617 Related Classifications