AMG8788

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AMG8788

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1159996-43-6

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

AMG8788 是一种有效的、选择性的、具有口服活性的TRPM8拮抗剂，IC₅₀值为 63.2 nM。

生物活性

AMG8788 is a potent, selective, orally active antagonist ofTRPM8with anIC₅₀of 63.2 nM^[1].

IC₅₀& Target

TRPM8

63.2 nM (IC₅₀)

TRPA1

1 μM (IC₅₀)

体外研究
(In Vitro)

AMG8788 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T_1/2) in rats is 6.7 h^[1].

体内研究
(In Vivo)

AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (T_b) 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 T_bfrom 40 min to 70 min post dosing.
Effect of AMG8788 on T_bin rats. P value is for comparing compound administered rat T_bwith vehicle administered rat T_b. 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 T_bdecrease (℃)	Pvalue *	Time post dosing (min)	Plasma concentration
AMG8788	30 (p.o.)	0.53	p< 0.05	40	1.5 ± 0.6

分子量

414.40

Formula

C₂₃H₁₈F₄N₂O

CAS 号

1159996-43-6

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.