| Bioactivity | 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]. |
| Invitro | 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]. |
| Name | AP-18 |
| CAS | 55224-94-7 |
| Formula | C11H12ClNO |
| Molar Mass | 209.67 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [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. |