[CAS NO. 55224-94-7] AP-18
PRODUCTS SPECIFICATIONS [55224-94-7]
DESCRIPTION [55224-94-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 209.67 |
| Molecular Formula | C11H12ClNO |
| SMILES | CC(/C(C)=C/C1=CC=C(Cl)C=C1)=N\O |
Summary
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC 50 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 IC 50 of 10.3 μM [1] [2] [3] .
IC50 & Target
|
TRPA1 ~3 μM (IC 50 ) |
In Vitro
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 Ca 2+ 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
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)
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 476.94 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.7694 mL | 23.8470 mL | 47.6940 mL |
| 5 mM | 0.9539 mL | 4.7694 mL | 9.5388 mL |
| 10 mM | 0.4769 mL | 2.3847 mL | 4.7694 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (11.92 mM); Clear solution
References
- [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.