1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. AP-18

AP-18 

目录号: HY-W014421
产品使用指南

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。

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AP-18 Chemical Structure

AP-18 Chemical Structure

CAS No. : 55224-94-7

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Description

AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM[1][2][3].

IC50 & Target[3]

TRPA1

~3 μM (IC50)

In Vitro

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].

In Vivo

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

Molecular Weight

209.67

Formula

C₁₁H₁₂ClNO

CAS No.

55224-94-7

SMILES

CC(/C(C)=C/C1=CC=C(Cl)C=C1)=N\O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

AP-18AP18AP 18TRP ChannelTransient receptor potential channelshyperalgesiapaintransductiondorsalrootganglianervesnociceptiveInhibitorinhibitorinhibit

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AP-18
目录号:
HY-W014421
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