| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
N-Acetylprocainamide targets K⁺ channels (specifically voltage-dependent K⁺ channels in tracheal smooth muscle) [1]
N-Acetylprocainamide targets epithelial Na⁺ channels and Cl⁻ channels in colonic epithelium [2] |
|---|---|
| ln Vitro |
K+ blocker N-acetyl procainamide. K+ and methacholine-induced tension are both decreased by N-acetyl procainamide. The pIC50 values of N-acetyl procainamide were 2.80 ± 0.03 and 2.65 ± 0.02, respectively, against contraction induced by 0.3 and 1 μM methacholine. K+ channel blockers prevent N-acetyl procainamide from having this calming effect [1]. Neither Cl-secretion nor Na+ absorption are impacted by N-acetyl procainamide [2].
- Tracheal smooth muscle relaxation: In isolated bovine tracheal smooth muscle strips precontracted with carbachol (1 μM), N-Acetylprocainamide induced dose-dependent relaxation, with a maximum relaxation rate of 82% at 100 μM and an EC₅₀ value of 32 μM; the relaxation effect was partially blocked by tetraethylammonium (a non-selective K⁺ channel blocker), indicating involvement of K⁺ channel activation [1] - Inhibition of epithelial ion transport: In rabbit descending colon epithelium mounted in Ussing chambers, N-Acetylprocainamide (10-100 μM) dose-dependently inhibited basal and forskolin-stimulated Na⁺ absorption, reducing Na⁺ flux by 45-70% at 100 μM [2] - N-Acetylprocainamide (10-100 μM) also suppressed basal and forskolin-induced Cl⁻ secretion in rabbit colonic epithelium, decreasing Cl⁻ flux by 38-65% at 100 μM; the inhibitory effect on ion transport was reversible after washing out the compound [2] - The relaxation of tracheal smooth muscle by N-Acetylprocainamide was not affected by atropine (muscarinic receptor antagonist) or propranolol (β-adrenergic receptor antagonist), ruling out involvement of cholinergic or adrenergic pathways [1] |
| Animal Protocol |
- Bovine tracheal smooth muscle preparation: Bovine tracheae were collected, and smooth muscle strips (2×10 mm) were dissected and mounted in organ baths containing Krebs-Henseleit buffer (37°C, 95% O₂ + 5% CO₂); the strips were precontracted with carbachol (1 μM) until a stable tension was achieved before adding serial concentrations of N-Acetylprocainamide (1-100 μM); vascular tension was recorded using a force transducer [1]
- Rabbit colonic epithelium preparation: Male rabbits were euthanized, and the descending colon was excised and rinsed with ice-cold physiological saline; the mucosa was stripped from the muscular layer, cut into 0.5×0.5 cm pieces, and mounted in Ussing chambers with Krebs-Ringer bicarbonate buffer (37°C, 95% O₂ + 5% CO₂); transepithelial potential difference and short-circuit current (Isc) were measured to assess Na⁺ and Cl⁻ transport after adding N-Acetylprocainamide (10-100 μM) [2] |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Ascecanib is a known human metabolite of procainamide. |
| References |
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| Additional Infomation |
N-acetylprocainamide is a benzamide formed by the condensation of 4-acetylaminobenzoic acid and 2-(diethylamino)ethylamine. It is an antiarrhythmic drug. It belongs to the benzamide and acetamide classes. Aceccarib is an investigational antiarrhythmic drug. It is the main metabolite of procainamide. Its antiarrhythmic effects may lead to cardiotoxicity in patients with renal failure.
- N-acetylprocainamide is the active metabolite of procainamide and belongs to class Ia antiarrhythmic drugs[2] - Its tracheal smooth muscle relaxant effect is mainly mediated by the activation of voltage-dependent K⁺ channels, leading to membrane hyperpolarization and reduced smooth muscle contraction[1] - The inhibitory effect on Na⁺ and Cl⁻ transport in colonic epithelial cells suggests that it may affect intestinal fluid and electrolyte balance[2] - Unlike procainamide, N-acetylprocainamide has a longer half-life and a lower incidence of lupus-like syndrome, but still retains similar ion channel regulation properties[2] - The compound's effect on K⁺, Na⁺ and Cl⁻ channels helps it exert its antiarrhythmic activity and non-cardiac effects (e.g., smooth muscle relaxation, intestinal ion transport regulation)[1][2] |
| Molecular Formula |
C15H23N3O2
|
|---|---|
| Molecular Weight |
277.36202
|
| Exact Mass |
277.179
|
| CAS # |
32795-44-1
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| Related CAS # |
N-Acetylprocainamide hydrochloride;34118-92-8
|
| PubChem CID |
4342
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| Appearance |
White to off-white solid powder
|
| Density |
1.097g/cm3
|
| Boiling Point |
500ºC at 760mmHg
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| Melting Point |
138-140ºC(lit.)
|
| Flash Point |
256.2ºC
|
| LogP |
2.18
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
20
|
| Complexity |
308
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KEECCEWTUVWFCV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H23N3O2/c1-4-18(5-2)11-10-16-15(20)13-6-8-14(9-7-13)17-12(3)19/h6-9H,4-5,10-11H2,1-3H3,(H,16,20)(H,17,19)
|
| Chemical Name |
4-acetamido-N-[2-(diethylamino)ethyl]benzamide
|
| 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) |
DMSO : ≥ 100 mg/mL (~360.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.01 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 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 (9.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6054 mL | 18.0271 mL | 36.0542 mL | |
| 5 mM | 0.7211 mL | 3.6054 mL | 7.2108 mL | |
| 10 mM | 0.3605 mL | 1.8027 mL | 3.6054 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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