1159997-27-9
1159997-27-9 structure
- Name: AMG9678
- Chemical Name: AMG9678
- CAS Number: 1159997-27-9
- Molecular Formula: C20H18F6N2O
- Molecular Weight: 416.36
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2022-06-17 12:59:16
- Modify Date: 2024-01-09 16:17:34
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AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM[1].
| Name | AMG9678 |
|---|
| Description | AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM[1]. |
|---|---|
| Related Catalog | |
| Target |
TRPM8:31.2 nM (IC50) TRPA1:0.6 μM (IC50) |
| In Vitro | 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]. |
| In Vivo | AMG9678 (0-100 mg/kg; p.o.; once) produces a significant and somewhat dose-dependent decrease in body temperature (Tb) in rats[1]. AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing in rats[1]. Animal Model: Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age) [1] Dosage: 10, 30 and 100 mg/kg Administration: Oral administration, once or once daily for 4 consecutive days 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 |
| References |
| Molecular Formula | C20H18F6N2O |
|---|---|
| Molecular Weight | 416.36 |