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

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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查看 TRP Channel 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献


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

IC50 & Target


31.2 nM (IC50)


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].

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

(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





Room temperature in continental US; may vary elsewhere.


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

纯度 & 产品资料
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  • 稀释计算器

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

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.


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