AP 18 |
Katalog-Nr.GC18020
One-Click Copy Product Info
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AP 18, ein potenter und selektiver TRPA1-Inhibitor, blockiert die Aktivierung von TRPA1 durch 50 μM Zimtaldehyd mit einem IC50-Wert von 3,1 μM bzw. 4,5 μM für menschliches bzw. Maus-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 selective channel blocker which can reversibly inhibit TRPA1 of human and mouse with IC50 of 3.1 µM and 4.5 µM, respectively.
TRPV1 belongs to the transient receptor potential family of cation channels and is activated by low pH, heat, and capsaicin. Originally known as a noxious cold-activated ion channel, TRPA1 is expressed in the same sensory neurons as TRPV1 and is activated directly by a variety of chemicals via covalent modification, and indirectly through G-protein coupled receptors.
In odontoblasts, AP18 is effective to inhibit the increase in intracellular Ca2+ concentration induced by allyl isothiocyanate and cinnamaldehyde (the TRPA1 agonists) 1.
In vivo, AP-18 blocks the transient receptor potential ankyrin 1 receptors and can reduce chronic pain associated with arthritis. This product is also capable to induce cinnamaldehyde-induced nociception and to block cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation 2. In addition, AP18 treatment reversed CFA-induced mechanical hyperalgesia in mice 2. Thus, TRPA1 is essential for sensitization of nociception.
References:
1. Egbuniwe O, Grover S, Duggal AK, et al. TRPA1 and TRPV4 activation in human odontoblasts stimulates ATP release. Journal of dental research. 2014;93(9):911-917.
2. Petrus M, Peier AM, Bandell M, et al. A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition. Molecular pain. 2007;3:40.
| 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 |
| Löslichkeit | 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- 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.)