KOR agonist-9
KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus.
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- Formule: C36H45N3O4
- Masse moléculaire:583.76
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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κ Opioid Receptor/KOR 0.0016 nM (Ki) |
κ Opioid Receptor/KOR 1.41 nM (EC50) |
μ Opioid Receptor/MOR 0.20 nM (Ki) |
δ Opioid Receptor/DOR 15.15 nM (Ki) |
KOR agonist-9 (compound 10e) (17 h) shows significantly lower potency for β-arrestin recruitment in HTLA-KOR Tango cells (EC50 = 4912 nM) compared to cAMP inhibition, indicating G-protein biased signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KOR agonist-9 (5-10 mg/kg; i.p.; single dose; 4 hours pretreatment) induces dose-dependent antipruritic effects in the mouse histamine-induced pruritus model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, 18~22 g)[1]
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Dosage:2; 5; 10; 15; 20 mg/kg
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Administration:i.p.; single dose; 4 hours pretreatment
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Result:Produced dose-dependent antinociceptive effects.
Showed significant antinociception observed at the 15 mg/kg dose.
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Animal Model:ICR mice (male, 18~22 g)[1]
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Dosage:5; 10 mg/kg
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Administration:i.p.; single dose; 4 hours pretreatment
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Result:Elicited dose-dependent antipruritic activity.
Showed a significant reduction in scratching bouts observed at the 10 mg/kg dose.
Chemical Information
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Masse moléculaire 583.76
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Formule C36H45N3O4
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SMILES
COC1=C(O2)C([C@]([C@@H]2[C@]3(OC)[C@@H](N4CCN(C(CC5=CC=CC=C5)=O)CC4)C6)(CC7)[C@@]6(CC3)C(N7CC8CC8)C9)=C9C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KOR agonist-9 Related Classifications
HY-183773 Related Classifications
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