AP-18

更新时间：2025-08-25 10:30:01

AP-18结构式	常用名	AP-18	英文名	AP-18
	CAS号	55224-94-7	分子量	209.672
	密度	1.1±0.1 g/cm3	沸点	348.4±34.0 °C at 760 mmHg
	分子式	C₁₁H₁₂ClNO	熔点	N/A
	MSDS	中文版美版	闪点	164.5±25.7 °C
	符号	GHS07	信号词	Warning

AP-18用途

AP-18 是一种选择性 TRPA1 抑制剂,AP-18 阻断 50 μM 肉桂醛对 TRPA1 的激活,在人和小鼠中的 IC50 分别为 3.1 μM 和 4.5 μM。AP-18 逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 以浓度依赖的方式减弱了 30 μM AITC 诱导的 Yo-Pro 摄取,IC50 为 10.3 μM。

英文名	4-(4-Chlorophenyl)-3-methyl-3-buten-2-oneoxime
英文别名	更多

描述	AP-18 是一种选择性 TRPA1 抑制剂,AP-18 阻断 50 μM 肉桂醛对 TRPA1 的激活,在人和小鼠中的 IC50 分别为 3.1 μM 和 4.5 μM。AP-18 逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 以浓度依赖的方式减弱了 30 μM AITC 诱导的 Yo-Pro 摄取,IC50 为 10.3 μM。
相关类别	信号通路 >> 跨膜转运 >> TRP频道研究领域 >> 神经疾病
靶点实验	TRPA1:~3 μM (IC50)
体外研究	浓度达50μM时,AP-18不能明显阻断TRPV1、TRPV2、TRPV3、TRPV4或TRPM8的激活。AP-18可逆地阻断小鼠TRPA1对碘乙酰胺(一种不可逆的半胱氨酸烷基化剂)的反应。AP-18还阻断冷和芥末油诱导的小鼠TRPA1活化。AP-18阻断了肉桂醛诱导的爪蟾卵母细胞的TRPA1电流[1]。
体内研究	AP18(1 mM；小鼠后肢注射)显著阻断肉桂醛染料诱导的伤害性事件,而不是辣椒素诱导的伤害性事件,证明了其有效性和特异性[1]。
参考文献	[1]. Petrus M, et al. A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition. Mol Pain. 2007;3:40. Published 2007 Dec 17. [2]. Chen J, et al. Pore dilation occurs in TRPA1 but not in TRPM8 channels. Mol Pain. 2009;5:3. Published 2009 Jan 21. [3]. Taylor-Clark TE, et al. Nitrooleic acid, an endogenous product of nitrative stress, activates nociceptive sensory nerves via the direct activation of TRPA1. Mol Pharmacol. 2009;75(4):820-829.

密度	1.1±0.1 g/cm3
沸点	348.4±34.0 °C at 760 mmHg
分子式	C₁₁H₁₂ClNO
分子量	209.672
闪点	164.5±25.7 °C
精确质量	209.060745
PSA	32.59000
LogP	3.72
InChIKey	MHTJEUOFLVQMCL-NJHPPEEMSA-N
SMILES	CC(=Cc1ccc(Cl)cc1)C(C)=NO
蒸汽压	0.0±0.8 mmHg at 25°C
折射率	1.529
储存条件	-20°C，密闭，干燥

符号	GHS07
信号词	Warning
危害声明	H302
个人防护装备	dust mask type N95 (US);Eyeshields;Faceshields;Gloves
危害码 (欧洲)	Xn
风险声明 (欧洲)	22
危险品运输编码	NONH for all modes of transport

TRPA1 has a key role in the somatic pro-nociceptive actions of hydrogen sulfide.

PLoS ONE 7(10) , e46917, (2012)

Hydrogen sulfide (H(2)S), which is produced endogenously from L-cysteine, is an irritant with pro-nociceptive actions. We have used measurements of intracellular calcium concentration, electrophysiolo...

TRPV1 and TRPA1 mediate peripheral nitric oxide-induced nociception in mice.

PLoS ONE 4 , e7596, (2009)

Nitric oxide (NO) can induce acute pain in humans and plays an important role in pain sensitization caused by inflammation and injury in animal models. There is evidence that NO acts both in the centr...

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To investigate the involvement of transient receptor potential ankyrin 1 (TRPA1) in inflammatory hyperalgesia mediated by tumor necrosis factor α(TNFα) and joint inflammation.Mechanical hyperalgesia w...

(2E,3E)-4-(4-Chlorophenyl)-N-hydroxy-3-methyl-3-buten-2-imine

(2E,3E)-4-(4-Chlorophenyl)-N-hydroxy-3-methylbut-3-en-2-imine

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4-(4-chlorophenyl)-3-methylbut-3-en-2-one oxime

AP-18