| Size | Price | Stock | Qty |
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| 500mg |
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| Other Sizes |
| Targets |
Propacetamol hydrochloride is a prodrug that is hydrolyzed to paracetamol (acetaminophen) by plasma esterases. Paracetamol then acts as a centrally acting analgesic and antipyretic. Its mechanism of action is not fully understood but is thought to involve inhibition of cyclooxygenase (COX) enzymes, particularly COX-2, in the central nervous system. Paracetamol also modulates the endocannabinoid system and activates TRPV1 channels, contributing to its analgesic effects.
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| ln Vitro |
In vitro, propacetamol hydrochloride is rapidly hydrolyzed to paracetamol in plasma and other biological fluids. Its activity is assessed by measuring the conversion to paracetamol using HPLC or LC-MS/MS. Paracetamol's analgesic activity is characterized by its ability to inhibit prostaglandin synthesis in the central nervous system. Specific IC50 values for COX inhibition are not detailed in the provided search results.
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| ln Vivo |
In vivo, propacetamol hydrochloride is administered intravenously or intramuscularly for the management of pain and fever. It is particularly useful in postoperative settings, in patients who cannot take oral medications, and in acute pain management. The compound is hydrolyzed to paracetamol, which then provides the therapeutic effects. Propacetamol is used as an alternative to oral paracetamol when parenteral administration is required.
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| Enzyme Assay |
The in vitro activity of propacetamol hydrochloride is assessed using hydrolysis assays. Plasma or esterase-containing solutions are incubated with propacetamol hydrochloride, and the formation of paracetamol is measured by HPLC or LC-MS/MS. The rate of hydrolysis is determined. For paracetamol activity, COX inhibition assays are performed using recombinant COX enzymes or cell-based systems, and prostaglandin production is measured.
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| Cell Assay |
For cellular assays, hepatocytes or other cell lines expressing esterases are used to study the hydrolysis of propacetamol to paracetamol. Cells are cultured in appropriate media and treated with various concentrations of propacetamol hydrochloride. Paracetamol levels in the culture medium are measured by HPLC. Cell viability is assessed using standard assays to ensure that observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo, propacetamol hydrochloride is administered intravenously or intramuscularly to patients or animal models. In animal models, the compound is administered at doses equivalent to paracetamol doses (typically 10-50 mg/kg). Analgesic effects are assessed using the tail-flick test, hot plate test, or formalin test. Antipyretic effects are assessed in models of fever (e.g., LPS-induced fever). Plasma levels of paracetamol are measured by HPLC or LC-MS/MS.
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| ADME/Pharmacokinetics |
Propacetamol hydrochloride has a molecular weight of 300.78 g/mol and a molecular formula of C14H20N2O3·HCl. It is a water-soluble prodrug of paracetamol that is stable in solid form but rapidly hydrolyzed in solution. The compound should be stored under appropriate conditions to maintain stability. Specific pharmacokinetic parameters such as half-life and bioavailability are similar to those of paracetamol after hydrolysis.
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| Toxicity/Toxicokinetics |
Propacetamol hydrochloride is generally well-tolerated. As a prodrug of paracetamol, its side effect profile is similar to that of paracetamol. Common side effects are rare but may include injection site reactions, allergic reactions, and, at high doses, hepatotoxicity. The compound should be used with caution in patients with liver disease and should not exceed the recommended maximum daily dose of paracetamol.
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| Additional Infomation |
Propacetamol hydrochloride is a clinically approved medication used for the management of pain and fever when oral administration of paracetamol is not possible. It is available in some countries as an injectable formulation. Propacetamol provides the analgesic and antipyretic benefits of paracetamol in a parenteral form. It is particularly useful in postoperative settings, emergency departments, and in patients with swallowing difficulties. Propacetamol is available as a generic medication in some regions.
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| Molecular Formula |
C14H21CLN2O3
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|---|---|
| Molecular Weight |
300.7811
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| Exact Mass |
300.124
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| CAS # |
66532-86-3
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| Related CAS # |
Propacetamol;66532-85-2
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| PubChem CID |
108082
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
434.5ºC at 760 mmHg
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| Melting Point |
224-227ºC
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| Flash Point |
216.6ºC
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| LogP |
2.767
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
20
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| Complexity |
295
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)C(C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O
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| InChi Key |
WGTYJNGARJPYKG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H20N2O3.ClH/c1-4-16(5-2)10-14(18)19-13-8-6-12(7-9-13)15-11(3)17;/h6-9H,4-5,10H2,1-3H3,(H,15,17);1H
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| Chemical Name |
(4-acetamidophenyl) 2-(diethylamino)acetate;hydrochloride
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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. |
| 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) |
H2O : ~250 mg/mL (~831.17 mM)
DMSO : ~25 mg/mL (~83.12 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3247 mL | 16.6234 mL | 33.2469 mL | |
| 5 mM | 0.6649 mL | 3.3247 mL | 6.6494 mL | |
| 10 mM | 0.3325 mL | 1.6623 mL | 3.3247 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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