AP-18

Name: AP-18
Brand: MedChemExpress
SKU: HY-W014421
Rating: 4.5 (1 reviews)

Cat. No.: HY-W014421 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

AP-18 Chemical Structure

CAS No. : 55224-94-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 730	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[3]

TRPA1

~3 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	3.1 μM Compound: AP18	Antagonist activity at human TRPA1 expressed in CHO cells assessed as inhibition of CA-induced increase in calcium influx by Fluo-4 dye based FLIPR analysis in presence of 50 uM CA Antagonist activity at human TRPA1 expressed in CHO cells assessed as inhibition of CA-induced increase in calcium influx by Fluo-4 dye based FLIPR analysis in presence of 50 uM CA	[PMID: 30878828]
HEK293	IC₅₀	2.8 μM Compound: 5, AP18 5	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as [45]Ca2+ influx by microbeta plate count Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as [45]Ca2+ influx by microbeta plate count	[PMID: 19945872]
HEK293	IC₅₀	4 μM Compound: AP18	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy	[PMID: 30878828]
IMR-90	IC₅₀	2.2 μM Compound: AP18	Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis	[PMID: 22325155]

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^[1].

MedChemExpress (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

209.67

Formula

C₁₁H₁₂ClNO

CAS No.

55224-94-7

Appearance

Solid

Color

White to off-white

SMILES

CC(/C(C)=C/C1=CC=C(Cl)C=C1)=N\O

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

In Vitro:

DMSO : ≥ 100 mg/mL (476.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (11.92 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (11.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (271 KB) SDS (392 KB)

COA (245 KB) HNMR (190 KB) RP-HPLC (290 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[2]. Chen J, et al. Pore dilation occurs in TRPA1 but not in TRPM8 channels. Mol Pain. 2009;5:3. Published 2009 Jan 21. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.7694 mL	23.8470 mL	47.6940 mL	119.2350 mL
	5 mM	0.9539 mL	4.7694 mL	9.5388 mL	23.8470 mL
	10 mM	0.4769 mL	2.3847 mL	4.7694 mL	11.9235 mL
	15 mM	0.3180 mL	1.5898 mL	3.1796 mL	7.9490 mL
	20 mM	0.2385 mL	1.1923 mL	2.3847 mL	5.9617 mL
	25 mM	0.1908 mL	0.9539 mL	1.9078 mL	4.7694 mL
	30 mM	0.1590 mL	0.7949 mL	1.5898 mL	3.9745 mL
	40 mM	0.1192 mL	0.5962 mL	1.1923 mL	2.9809 mL
	50 mM	0.0954 mL	0.4769 mL	0.9539 mL	2.3847 mL
	60 mM	0.0795 mL	0.3974 mL	0.7949 mL	1.9872 mL
	80 mM	0.0596 mL	0.2981 mL	0.5962 mL	1.4904 mL
	100 mM	0.0477 mL	0.2385 mL	0.4769 mL	1.1923 mL

AP-18 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AP-1855224-94-7AP18AP 18TRP ChannelTransient receptor potential channelshyperalgesiapaintransductiondorsalrootganglianervesnociceptiveInhibitorinhibitorinhibit

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AP-18

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Complete Stock Solution Preparation Table

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