化合物AP 18 T21543

Product Introduction
Bioactivity


英文名: AP 18

描述: AP-18 是选择性的 TRPA1 抑制剂。AP-18 可以抑制 50 μM 肉桂醛诱导的 TRPA1 激活，在小鼠和人中的 IC50 分别为 4.5 μM 和 3.1 μM。AP-18 可以逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 可以浓度依赖的方式减弱 30 μM AITC 诱导的 Yo-Pro 摄取(IC50= 10.3 μM)。

体外活性: At concentrations up to 50 μM, AP-18 is unable to appreciably block activation of TRPV1, TRPV2, TRPV3, TRPV4, or TRPM8. AP-18 reversibly blocks mouse TRPA1 responses to iodoacetamide (an irreversible cysteine-alkylating agent) in CHO cells assayed by ratiometric Ca2+ imaging. AP-18 also blocks cold- and mustard-oil-induced activation of mouse TRPA1. AP-18 blocks cinnamaldehyde-induced TRPA1 currents in excised patches from Xenopus oocytes [1] [2] [3].

体内活性: AP18 (1 mM; injected in hindpaw of mice) significantly blocks cinnamaldehdye-induced but not capsaicin-induced nociceptive events, demonstrating efficacy and specificity [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (238.47 mM)


关键字: ganglia | TRP Channel | nerves | pain | Transient receptor potential channels | inhibit | nociceptive | root | hyperalgesia | Inhibitor | AP-18 | transduction | AP18 | dorsal | AP 18

相关产品: HC-030031 | JT010 | PF-05105679 | (E)-Cardamonin | MK-2295 | TRPM8 antagonist 3 | Olvanil | ABT 102 | TRPA1-IN-2 | Pinokalant

相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途