| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
AP-18 targets the transient receptor potential ankyrin 1 (TRPA1) ion channel. It acts as a reversible antagonist. TRPA1 is involved in sensing noxious stimuli and mediating pain and inflammation. By blocking TRPA1, AP-18 can reduce chronic pain associated with arthritis and other conditions.
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| ln Vitro |
Even at 50 μM, AP-18 did not substantially prevent TRPV1, TRPV2, TRPV3, TRPV4, or TRPM8 from activating. Ratiometric Ca2+ imaging in CHO cells demonstrates that AP-18 reversibly suppresses mouse TRPA1 responses to iodoacetamide, an irreversible cysteine alkylating agent. Additionally, AP-18 prevents mice from having their TRPA1 activated by cold oil and mustard oil. In ablated plaques of Xenopus oocytes, AP-18 inhibits TRPA1 currents generated by cinnamon aldehyde [1].
In vitro, AP-18 is a potent and selective TRPA1 inhibitor. It blocks activation of TRPA1 by 50 µM cinnamaldehyde with an IC50 of 3.1 µM. It has minimal effect on TRPV1-4 or TRPM8. These activities confirm its profile as a selective TRPA1 channel blocker. |
| ln Vivo |
AP18 (1 mM; injected into mice hind feet) effectively suppresses nociceptive events elicited by cinnamaldehyde dye but not capsaicin, exhibiting effectiveness and selectivity [1].
In vivo, AP-18 reduces cinnamaldehyde-induced nociception. It blocks cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation. It is widely used in preclinical research to study TRPA1-mediated pathways in neuropathic pain, asthma, and inflammatory diseases. |
| Enzyme Assay |
The in vitro ion channel assay for AP-18 measures its ability to block TRPA1 channel activity. These assays typically use patch-clamp techniques or calcium imaging on cells expressing TRPA1. The compound's potency (IC50) is determined by measuring the reduction in channel activity. Its selectivity is assessed by testing against other TRP channels.
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| Cell Assay |
In vitro cellular assays for AP-18 assess its effects on TRPA1-mediated signaling. Cells expressing TRPA1 are stimulated with agonists like cinnamaldehyde, and the compound's ability to inhibit calcium influx or other downstream signals is measured. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for AP-18 have been conducted in models of pain and inflammation to evaluate its efficacy. AP-18 reduces cinnamaldehyde-induced nociception and blocks TRPA1-mediated responses. These studies demonstrate the compound's in vivo efficacy.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for AP-18 are not extensively detailed in the available literature. As a small molecule, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as half-life and bioavailability are not provided. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for AP-18 are not extensively detailed in the available literature. As a TRPA1 channel blocker, its toxicity profile is likely related to its mechanism of action. However, its use in preclinical research suggests a manageable safety profile. It is intended for research purposes only.
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| References |
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| Additional Infomation |
AP-18 is a potent and selective TRPA1 channel blocker. It reversibly inhibits TRPA1 with IC50s of 3.1 and 4.5 µM for human and mouse, respectively. It is used to study TRPA1’s role in pain and inflammation. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C11H12CLNO
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| Molecular Weight |
209.67200
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| Exact Mass |
209.06
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| CAS # |
55224-94-7
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| PubChem CID |
9584673
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
348.4±34.0 °C at 760 mmHg
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| Flash Point |
164.5±25.7 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.529
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| LogP |
3.72
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
240
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C/C(=C\C1=CC=C(C=C1)Cl)/C(=N/O)/C
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| InChi Key |
MHTJEUOFLVQMCL-NJHPPEEMSA-N
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| InChi Code |
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+
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| Chemical Name |
(NE)-N-[(E)-4-(4-chlorophenyl)-3-methylbut-3-en-2-ylidene]hydroxylamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~476.94 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (11.92 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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