K185
K185 is a selective MT2 melatonin receptor antagonist. K185 has a pKi of 9.30 for human MT2. K185 can be used for research on febrile seizures.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 244160-11-0
- Formel: C24H28N2O2
- Molecular Weight:376.49
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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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
MT2 |
In Vitro
K185 (60 min) is a competitive Melatonin (HY-B0075) antagonist in Xenopus laevis melanophores with a pKB of 7.06 and no agonist activity[1].
K185 acts as an MT2-selective antagonist in NIH3T3 cells, antagonizing the inhibitory effect of Melatonin on Forskolin (HY-15371)-stimulated cAMP, and exhibits no agonist activity at concentrations up to 10 µM[1].
K185 (10 μM; 30 min) blocks MT2 receptor-mediated inhibition of mechanical sensitivity by Melatonin in guinea pig low-threshold muscle-mucosal bladder afferent fibers, while administration alone does not affect mechanical sensitivity[2].
K185 inhibits Saccharin (HY-Y0272)-induced melanosome aggregation in Labeo rohita scales, with an inhibition rate of 66.51% at 4.87 × 10-6 M saccharin, suggesting the involvement of MT2 receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 22-30 days); Wistar albino (male)[4]
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Dosage:2 mg/kg
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Administration:s.c.; single dose; 15 min before febrile-seizure induction
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Result:Rectal temperature with Melatonin was pre 35.15 °C and post 42.41 °C.
With Melatonin plus Luzindole, rectal temperature was pre 35.39 °C and post 42.19 °C.
With Melatonin plus Prazosin, rectal temperature was pre 34.99 °C and post 42.65 °C.
With Melatonin plus Luzindole plus Prazosin, rectal temperature was pre 35.15 °C and post 42.38 °C.
Seizure duration increased compared with Melatonin alone.
Racine seizure severity increased compared with Melatonin alone.
Seizure latency increased only with Melatonin plus Luzindole and with Melatonin plus Prazosin compared with the other groups; other combinations did not show this latency increase.
Chemical Information
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CAS. Nr. 244160-11-0
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Molecular Weight 376.49
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Formel C24H28N2O2
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SMILES
O=C(CCC)NCCC1=C(C2=CC=CC=C2CCC3)N3C4=C1C=C(C=C4)OC
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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)
K185 Related Classifications
HY-187978 Related Classifications
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