KOR modulator-1
KOR modulator-1 is a blood-brain barrier-permeable kappa opioid receptor (KOR) modulator. KOR modulator-1 induces antinociceptive effects without significant sedation or impairment of neuromuscular coordination. KOR modulator-1 can be used for the research of chronic pain.
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- Fòrmula: C26H27ClN4O2
- Peso molecular:462.97
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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κ Opioid Receptor/KOR |
KOR modulator-1 (15ao) (10 pM-10 μM) potently and selectively inhibits cAMP production via G-protein-dependent signaling in KOR-transfected HEK293T cells, with an IC50 of 5.1 nM[1].
KOR modulator-1 (10 pM-10 μM) induces β-arrestin 2 recruitment in HTLA cells expressing human KOR with an EC50 of 191 nM, and exhibits extreme G-protein-biased signaling with a bias factor of 1.55[1].
KOR modulator-1 (10 pM-10 μM) does not stimulate ERK1/2-MAPK signaling in KOR-transfected HEK293T cells[1].
KOR modulator-1 binds to the orthosteric pocket of active-state human KOR with key conserved interactions and a predicted MM-GBSA binding affinity of -59.70 kcal/mol[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KOR modulator-1 (5 mg/kg; s.c.; single dose) does not induce sedation in mice[1].
KOR modulator-1 (5-10 mg/kg; s.c.; single dose) does not impair neuromuscular coordination in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male)[1]
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Dosage:5 mg/kg
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Administration:s.c.; single dose
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Result:Induced a time-dependent increase in %MPE, with efficacy clearly separated from vehicle over early to mid-time points.
Produced a significant increase in the area under the %MPE-time curve (AUC) relative to vehicle, approaching the efficacy of the reference agonist U50488.
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Animal Model:C57BL/6 (male)[1]
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Dosage:5 mg/kg
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Administration:s.c.; single dose
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Result:Exhibited no significant suppression of locomotor activity compared to vehicle control, in contrast to the unbiased reference agonist U50488 and less biased compounds.
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Animal Model:C57BL/6 (male)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:s.c.; single dose
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Result:Showed no significant reduction in rotarod fall latency at either 5 mg/kg or 10 mg/kg, in contrast to the unbiased reference agonist U50488 which caused a significant impairment.
Chemical Information
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Peso molecular 462.97
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Fòrmula C26H27ClN4O2
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SMILES
CC(C)(C)NC(C(N1CC2=CC=CC=C2)C3=[N+](CC1=O)C=CC4=C3NC5=C4C=CC=C5)=O.[Cl-]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KOR modulator-1 Related Classifications
HY-187342 Related Classifications
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