KOR agonist 6
KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects.
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- Formel: C35H40N4O4
- Molecular Weight:580.72
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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κ Opioid Receptor/KOR 0.25 pM (Ki) |
μ Opioid Receptor/MOR 14.1 nM (Ki) |
δ Opioid Receptor/DOR 120.7 nM (Ki) |
μ Opioid Receptor/MOR 44.78 nM (EC50) |
δ Opioid Receptor/DOR 15.26 nM (EC50) |
KOR agonist 6 (Compound 5i) exhibits ultra-high binding affinity to κ-opioid receptor (KOR (Ki = 0.00025 nM)) and exceptional subtype selectivity over μ-opioid receptor (MOR (Ki = 14.1 nM)) and δ-opioid receptor (DOR (Ki = 120.7nM))[1].
KOR agonist 6 shows agonistic activity at MOR (EC50 = 44.78 nM, Emax = 88.71%) and DOR (EC50 = 15.26 nM, Emax = 85.16%) in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation (EC50 = 200.3 nM, Emax = 99.51%)[1].
KOR agonist 6 stimulates KOR-mediated [35S]GTPγS binding with potent activity (EC50 = 0.024 nM, Emax = 106.9%) in KOR-expressing cell membranes, inhibits cAMP accumulation in KOR-expressing HEK293 cells with ultra-potent agonistic activity (EC50 = 0.43 pM, Emax = 63.63%) and induces β-arrestin recruitment in KOR-Tango plasmid-transfected HTLA cells with lower potency (EC50 = 0.143 nM, Emax = 42.89%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KOR agonist 6 (0.08-8.0 mg/kg, i.p., detected at 6 h post-administration) exerts dose-dependent antinociceptive activity in mice abdominal constriction test(ED50 = 1.5 mg/kg)[1].
KOR agonist 6 (0.8-8.0 mg/kg, i.p., conditioned for 6 days, tested on day 8 with 15 min free exploration) shows no significant conditioned place aversion in male CD1 mice[1].
KOR agonist 6 (0.8-8.0 mg/kg, i.p., monitored for 1 h at 6 h post-administration) does not cause significant reduction in spontaneous locomotor activity (total moving distance) in male Kunming mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Kunming mice (18-22 g) were used, with the nociceptive response (latency to licking back paws) assessed on a 55 °C heated smooth surface; mice with no response within 30 s before administration were excluded, and a 60 s cutoff time was set to prevent tissue damage[1]
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Dosage:0.4, 0.8, 1.2, 1.6, 8.0 mg/kg
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Administration:i.p., detected at 6 h post-administration
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Result:Showed dose-dependent antinociceptive efficacy in mice hot plate test (ED50 = 0.6 mg/kg).
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Animal Model:Male Kunming mice (18-22 g)[1]
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Dosage:0.08, 0.8, 3.2, 6.4, 8.0 mg/kg
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Administration:i.p., detected at 6 h post-administration followed by 0.6% acetic acid injection
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Result:Showed dose-dependent antinociceptive activity in mice abdominal constriction test(ED50 = 1.5 mg/kg).
Chemical Information
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Molecular Weight 580.72
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Formel C35H40N4O4
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SMILES
O=C(NC1=CC=C([C@H]2C[C@@]34CC[C@]2(OC)[C@H]5[C@]36C7=C(C(OC)=CC=C7CC4N(CC6)CC8CC8)O5)C=C1)C9=NN(C=C9)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
KOR agonist 6 Related Classifications
HY-175486 Related Classifications
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