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AP 18

Catalog No. T21543   CAS 55224-94-7

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).

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AP 18 Chemical Structure
AP 18, CAS 55224-94-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 113.00
25 mg In stock $ 239.00
50 mg In stock $ 378.00
100 mg In stock $ 592.00
500 mg In stock $ 1,270.00
1 mL * 10 mM (in DMSO) In stock $ 72.00
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Purity: 99.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
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, evidencing 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

Solubility Information

DMSO: 50 mg/mL (238.47 mM)

TargetMolReferences and Literature

1. Matt Petrus, et al. A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition. Mol Pain. 2007;3:40. Published 2007 Dec 17. 2. Jun Chen, et al. Pore dilation occurs in TRPA1 but not in TRPM8 channels. Mol Pain. 2009;5:3. Published 2009 Jan 21. 3. Thomas E Taylor-Clark, 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Membrane Protein-targeted Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

Related Products

Related compounds with same targets
Diphenyleneiodonium chloride WS-12 TRPM4-IN-1 D-3263 hydrochloride (Z)-Capsaicin M8-B Hydrochloride TRPM8 antagonist 2 PF-04745637

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Keywords

AP 18 55224-94-7 Membrane transporter/Ion channel TRP/TRPV Channel ganglia TRP Channel nerves pain Transient receptor potential channels inhibit nociceptive root hyperalgesia Inhibitor AP-18 transduction AP18 dorsal inhibitor

 

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