AP 18 |
Catalog No.GC18020
One-Click Copy Product Info
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AP 18 is a potent and selective TRPA1 inhibitor, blocking activation of TRPA1 by 50μM Cinnamaldehyde with an IC50 value of 4.5μM for mouse TRPA1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 55224-94-7
Sample solution is provided at 25 µL, 10mM.
AP 18 is a potent and selective TRPA1 inhibitor, blocking activation of TRPA1 by 50μM Cinnamaldehyde with an IC50 value of 4.5μM for mouse TRPA1[1]. AP 18 attenuates 30μM allyl isothiocyanate (AITC)-induced divalent cation Yo-Pro uptake in HEK-293F cells expressing rat TRPA1, with an IC50 value of 10.3μM[2]. AP 18 targets TRPA-1 to inhibit Ca2+ influx mediated by oxidative stress, prevent the Ca2+-dependent anti-apoptotic pathway, downregulate the expression of N-cadherin and vimentin, and upregulate the expression of E-cadherin[3]. AP 18 has been used to inhibit cholinergic twitch responses evoked by electrical field stimulation of cholinergic nerves as well as contractions in response to acetylcholine and histamine in the guinea pig small intestine[4].
In vitro, AP 18 treatment (100µM) for 48 hours reduced the viability of LU-NB-3 cells and altered the morphology, promoting the cells to transform into flat adherent structures with dendritic protrusions[5]. Incubation of AP 18 (10µM) and Resveratrol (50µM) for 24h decreased the hypoxia-mediated upregulation of apoptotic (caspase -3, -8, and -9) and oxidative (ROS and lipid peroxidation) concentrations, and mitigated mitochondrial dysfunction in SH-SY5Y cells[6]. The 12-day treatment with 1µM AP 18 weakened the inhibitory effect of 1µM trans-Pellitorine on lipid accumulation in 3T3-L1 cells and restored the expression levels of the PPARγ gene and protein[7].
In vivo, AP 18 treatment via intraperitoneal administration at a dose of 3mg/kg 30min before intraplantar lipopolysaccharide (LPS) injection completely prevented development of the LPS-induced hyperalgesia in C57Bl/6 mice[8]. In CD1 mice, intra-articular injection of AP 18 (25nmol/10µl) at 22 hours after Freund's complete adjuvant (CFA) injection alleviated CFA-induced mechanical hyperalgesia[9].
References:[1] Petrus M, Peier A M, Bandell M, et al. A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition[J]. Molecular pain, 2007, 3: 1744-8069-3-40.
[2] Chen J, Kim D, Bianchi B R, et al. Pore dilation occurs in TRPA1 but not in TRPM8 channels[J]. Molecular pain, 2009, 5: 1744-8069-5-3.
[3] Wang Y, Yin S, Mei L, et al. A dual receptors-targeting and size-switchable “cluster bomb” co-loading chemotherapeutic and transient receptor potential ankyrin 1 (TRPA-1) inhibitor for treatment of triple negative breast cancer[J]. Journal of Controlled Release, 2020, 321: 71-83.
[4] Bartho L, Sándor Z, Kelemen D, et al. Smooth muscle-depressant activity of AP-18, a putative TRPA1 antagonist in the guinea pig intestine[J]. Pharmacology, 2014, 94(3-4): 131-134.
[5] Seger A, Adamič D, Olmos E M, et al. Evaluation of TRPA1 as a Therapeutic Target in MYCN‐Amplified Neuroblastoma[J]. Pediatric Blood & Cancer, 2025, 72(9): e31875.
[6] Ertilav K. Resveratrol Reduces Hypoxia-Caused Increases of Apoptosis and Oxidative Neurotoxicity via TRPA1 Cation Channel Suppression in Glioblastoma Cells[J]. Online Turkish Journal of Health Sciences, 2025, 10(4): 382-389.
[7] Lieder B, Zaunschirm M, Holik A K, et al. The alkamide trans-pellitorine targets PPARγ via TRPV1 and TRPA1 to reduce lipid accumulation in developing 3T3-L1 adipocytes[J]. Frontiers in pharmacology, 2017, 8: 316.
[8] Andersson D A, Gentry C, Bevan S. TRPA1 has a key role in the somatic pro-nociceptive actions of hydrogen sulfide[J]. PLoS ONE, 2012, 7(10): e46917.
[9] Fernandes E S, Russell F A, Spina D, et al. A distinct role for transient receptor potential ankyrin 1, in addition to transient receptor potential vanilloid 1, in tumor necrosis factor α–induced inflammatory hyperalgesia and Freund's complete adjuvant–induced monarthritis[J]. Arthritis & Rheumatism, 2011, 63(3): 819-829.
| Cell experiment [1]: | |
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Cell lines |
LU-NB-3 cells |
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Preparation Method |
LU-NB-3 cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin, 2% B27 without vitamin A, epidermal growth factor (20ng/ml), and fibroblast growth factor (40ng/ml) at 37°C in an incubator with 5% CO2. In 96-well plates, LU-NB-3 cells were plated in triplicate and subjected to 24h treatments with different concentrations of AP 18 (0, 1, 5, 10, and 100µM). After 48h, and cell viability was tested. |
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Reaction Conditions |
0, 1, 5, 10, and 100µM; 48h |
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Applications |
AP 18 treatment markedly promoted cell death of LU-NB-3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
C57Bl/6J mice |
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Preparation Method |
C57Bl/6J mice (8 weeks old) were housed in SPF conditions with an automatic 12h/12h light-dark cycle at a constant temperature (20-25°C). LPS (10µg in 25µl saline) was injected subcutaneously into the plantar surface of one of the hind paws using a 50µl syringe fitted with a 26-gauge×3/8 inch intradermal needle. AP 18 was made up in 1% DMSO/0.5% Tween 80/saline. Pretreatment with AP 18 (3mg/kg; i.p.; 30min before LPS). The nociceptive effect of local LPS was measured. |
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Dosage form |
3mg/kg; once; i.p. |
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Applications |
AP 18 treatment prevented the development of the LPS-induced hyperalgesia in C57Bl/6 mice. |
| References: [1] Seger A, Adamič D, Olmos E M, et al. Evaluation of TRPA1 as a Therapeutic Target in MYCN‐Amplified Neuroblastoma[J]. Pediatric Blood & Cancer, 2025, 72(9): e31875. [2] Andersson D A, Gentry C, Bevan S. TRPA1 has a key role in the somatic pro-nociceptive actions of hydrogen sulfide[J]. PLoS ONE, 2012, 7(10): e46917. | |
| Cas No. | 55224-94-7 | SDF | |
| Chemical Name | (2E,3Z)-4-(4-chlorophenyl)-3-methylbut-3-en-2-one oxime | ||
| Canonical SMILES | ClC1=CC=C(C=C1)/C=C(C)\C(C)=N\O | ||
| Formula | C11H12ClNO | M.Wt | 209.67 |
| Solubility | 20 mg/ml in enathol; 30 mg/ml in DMSO | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.7694 mL | 23.847 mL | 47.694 mL |
| 5 mM | 953.9 μL | 4.7694 mL | 9.5388 mL |
| 10 mM | 476.9 μL | 2.3847 mL | 4.7694 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)