Description
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 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 IC50 of 10.3 μM.
Product information
CAS Number: 55224-94-7
Molecular Weight: 209.67
Formula: C11H12ClNO
Chemical Name: (E)-N-[(3Z)-4-(4-chlorophenyl)-3-methylbut-3-en-2-ylidene]hydroxylamine
Smiles: C/C(=N\O)/C(/C)=C\C1C=CC(Cl)=CC=1
InChiKey: MHTJEUOFLVQMCL-XTYDYKDCSA-N
InChi: InChI=1S/C11H12ClNO/c1-8(9(2)13-14)7-10-3-5-11(12)6-4-10/h3-7,14H,1-2H3/b8-7-,13-9+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 Ca2+ 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.
In Vivo:
AP18 (1 mM; injected in hindpaw of mice) significantly blocks cinnamaldehdye-induced but not capsaicin-induced nociceptive events, demonstrating efficacy and specificity.
Products are for research use only. Not for human use.
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