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AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $43 | In Stock | |
10 mg | $67 | In Stock | |
25 mg | $143 | In Stock | |
50 mg | $226 | In Stock | |
100 mg | $355 | In Stock | |
500 mg | $762 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
Description | AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM). |
In vitro | At concentrations up to 50 μM, AP-18 does not significantly inhibit the activation of TRPV1, TRPV2, TRPV3, TRPV4, or TRPM8. However, it effectively and reversibly inhibits the activation of mouse TRPA1 by iodoacetamide (an irreversible cysteine-alkylating agent) in CHO cells, as determined through ratiometric Ca2+ imaging. Additionally, AP-18 prevents cold- and mustard-oil-triggered activation of mouse TRPA1 and inhibits TRPA1 currents induced by cinnamaldehyde in Xenopus oocyte excised patches, demonstrating its specificity and effectiveness in modulating TRPA1 activity [1] [2] [3]. |
In vivo | AP18 (1 mM; injected in the hindpaw of mice) effectively inhibits nociceptive events triggered by cinnamaldehyde, but not those induced by capsaicin, demonstrating its specificity and efficacy [1]. |
Molecular Weight | 209.67 |
Formula | C11H12ClNO |
Cas No. | 55224-94-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (238.47 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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