Size | Price | Stock | Qty |
---|---|---|---|
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Purity: ≥98%
ACA [also known as N-(p-amylcinnamoyl) Anthranilic Acid] is a broad-spectrum inhibitor of phospholipase A2 (PLA2) and a TRP channel blocker. It is structurally-related to non-steroidal anti-inflammatory drugs (NSAIDs) of the fenamate group and may also modulate various ion channels. In HEK293 cells transfected with human TRPM2, ACA (20 µM) completely blocked H2O2-induced Ca2+ signals and ADPR-induced whole-cell currents with IC50 value of 1.7 µM. The inhibitory effects of ACA on I(Cl(Ca)) are PLA(2)-independent and that the drug may serve as a useful tool in understanding the nature and function of cardiac anion channels.
ln Vitro |
N-(p-amylcinnamoyl) Anthranlilic Acid (ACA; 20 μM) totally inhibits H2O2-induced Ca2+ signals and ADPR-induced whole-cell currents in HEK293 cells transfected with human TRPM2 (IC50=1.7 μM) [1]. Additionally, N-(p-amylcinnamoyl) Anhranilic Acid (ACA; 20 μM) burns current through human TRPM8 and TRPC6[1], which are expressed in HEK293 cells. Several TRP channels are regulated by N-(p-amylcinnamoyl) Anthranlilic Acid (ACA) separately from PLA22 inhibition [1].
|
---|---|
References |
[1]. Kraft R, et al. Inhibition of TRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid. Br J Pharmacol. 2006 Jun;148(3):264-73.
[2]. Harteneck C, et al. N-(p-amylcinnamoyl)anthranilic acid (ACA): a phospholipase A(2) inhibitor and TRP channel blocker. Cardiovasc Drug Rev. 2007 Spring;25(1):61-75. [3]. Gwanyanya A, et al. Inhibition of the calcium-activated chloride current in cardiac ventricular myocytes by N-(p-amylcinnamoyl)anthranilic acid (ACA). Biochem Biophys Res Commun. 2010 Nov 19;402(3):531-6. |
Molecular Formula |
C21H23NO3
|
|
---|---|---|
Molecular Weight |
337.41
|
|
CAS # |
110683-10-8
|
|
Related CAS # |
|
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
|
SMILES |
CCCCCC1=CC=C(/C([H])=C([H])/C(O)=N/C2=CC=CC=C2C(O)=O)C=C1
|
|
Chemical Name |
|
|
Synonyms |
|
|
HS Tariff Code |
2934.99.9001
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 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: ≥ 2.08 mg/mL (6.16 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 20.8 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 | 2.9638 mL | 14.8188 mL | 29.6375 mL | |
5 mM | 0.5928 mL | 2.9638 mL | 5.9275 mL | |
10 mM | 0.2964 mL | 1.4819 mL | 2.9638 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.