1159996-43-6
1159996-43-6 structure
- Name: AMG8788
- Chemical Name: AMG8788
- CAS Number: 1159996-43-6
- Molecular Formula: C23H18F4N2O
- Molecular Weight: 414.40
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2022-06-25 12:41:16
- Modify Date: 2024-01-14 20:27:16
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AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM[1].
| Name | AMG8788 |
|---|
| Description | AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM[1]. |
|---|---|
| Related Catalog | |
| Target |
TRPM8:63.2 nM (IC50) TRPA1:1 μM (IC50) |
| In Vitro | AMG8788 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 6.7 h[1]. |
| In Vivo | AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (Tb) in rats[1]. Animal Model: Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age) [1] Dosage: 30 mg/kg Administration: Oral administration, once Result: Produced a significant decrease of Tb from 40 min to 70 min post dosing. Effect of AMG8788 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 AMG8788 30 (p.o.) 0.53 p < 0.05 40 1.5 ± 0.6 |
| References |
| Molecular Formula | C23H18F4N2O |
|---|---|
| Molecular Weight | 414.40 |