1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. AMG9678

AMG9678 

目录号: HY-104062
产品使用指南

AMG9678 是一种有效的、选择性的、具有口服活性的 TRPM8 拮抗剂,IC50 值为 31.2 nM。

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AMG9678 Chemical Structure

AMG9678 Chemical Structure

CAS No. : 1159997-27-9

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  • 参考文献

生物活性

AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM[1].

IC50 & Target

TRPM8

31.2 nM (IC50)

TRPA1

0.6 μM (IC50)

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
分子量

416.36

Formula

C20H18F6N2O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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HY-104062
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