AMG9678
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.
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- CAS. Nr.: 1159997-27-9
- Formel: C20H18F6N2O
- Molecular Weight:416.36
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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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TRPM8 31.2 nM (IC50) |
TRPA1 0.6 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
27 nM
Compound: 29
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Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin challenge by luminometry
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin challenge by luminometry
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[PMID: 24597733] |
AMG9678 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 7.6 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age) [1]
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Dosage:10, 30 and 100 mg/kg
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Administration:Oral administration, once or once daily for 4 consecutive days
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Result:Produced a significant and somewhat dose-dependent decrease in Tb at 10, 30 and 100 mg/kg. The magnitude of TRPM8 blockade-induced decrease in body temperature is reduced after repeated dosing.
Effect of AMG9678 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCT
Compound Dose mg/kg (route) Max Tb decrease (°C) P value * Time post dosing (min) Plasma concentration AMG9678 10 (p.o.) 0.72 p < 0.001 60 0.04 ± 0.006 AMG9678 30 (p.o.) 0.70 p < 0.01 60 0.34 ± 0.1 AMG9678 100 (p.o.) 0.83 p < 0.05 60 0.36 ± 0.12
Chemical Information
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CAS. Nr. 1159997-27-9
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Molecular Weight 416.36
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Formel C20H18F6N2O
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SMILES
O=C(N1CCC2=C(C=CC=C2)[C@H]1C3=CC=C(C(F)(F)F)C=C3)N[C@@H](C)C(F)(F)F
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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)
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