| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
| Targets |
The primary targets of Alminoprofen are the cyclooxygenase (COX) enzymes, COX-1 and COX-2, which are key enzymes in the prostaglandin biosynthesis pathway. By inhibiting COX enzymes, Alminoprofen reduces the production of pro-inflammatory prostaglandins, thereby exerting its analgesic and anti-inflammatory effects. The compound belongs to the phenylpropionic acid class of NSAIDs, which are characterized by their ability to inhibit COX enzymes and reduce inflammation.
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|---|---|
| ln Vitro |
Alminoprofen inhibits both sPLA2 and COX-2, resulting in dual anti-inflammatory actions. PGE2 levels in the CRL-1517 cell line are dose-relatedly inhibited by alminoprofen (0 to 50 μM) [1].
Alminoprofen demonstrates in vitro anti-inflammatory and analgesic activity through the inhibition of COX-1 and COX-2 enzymes. However, detailed IC50 values for COX inhibition are not extensively reported in the available literature. The compound's activity is assessed in standard NSAID assays measuring the inhibition of prostaglandin production. Its in vitro efficacy confirms its mechanism of action as a COX inhibitor. |
| ln Vivo |
Aminolofen (100-300 mg/kg; oral) provides anti-inflammatory action [1].
Alminoprofen significantly suppresses passive anaphylactic bronchoconstrictions at 30 mg/kg given intraduodenally. The compound is used for the short-term management of dental, traumatic, and postpartum pain. These in vivo findings confirm the compound's analgesic and anti-inflammatory efficacy. However, detailed in vivo efficacy data are not extensively reported in the available literature. |
| Enzyme Assay |
In vitro enzyme assays for Alminoprofen typically involve measuring its inhibition of COX-1 and COX-2 activity. Recombinant human COX-1 or COX-2 enzymes are incubated with arachidonic acid substrate in the presence of varying concentrations of Alminoprofen. The production of prostaglandins is measured, and the IC50 for inhibition is calculated. These assays are used to characterize the compound's anti-inflammatory activity.
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| Cell Assay |
Cellular assays for Alminoprofen are typically performed using inflammatory cell models, such as macrophages or other immune cells. Cells are stimulated with LPS or other inflammatory agents in the presence or absence of Alminoprofen, and the production of pro-inflammatory cytokines or prostaglandins is measured. The compound's ability to reduce inflammatory mediator production is assessed.
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| Animal Protocol |
Animal/Disease Models: Wistar rat group (paw edema) [1]
Doses: 100 mg/kg Route of Administration: Oral Experimental Results:Statistically significant dose-dependent antagonistic effect throughout the 2-hour observation period. In vivo animal studies with Alminoprofen have been performed to evaluate its anti-inflammatory and analgesic efficacy. In these studies, Alminoprofen is administered orally or intraduodenally, and its effects on inflammation and pain are assessed. At a dose of 30 mg/kg given intraduodenally, Alminoprofen significantly suppresses passive anaphylactic bronchoconstrictions. However, specific protocols are not extensively detailed in the available literature. |
| ADME/Pharmacokinetics |
Alminoprofen has a molecular weight that is not specified in the available literature. It has a molecular formula of C13H17NO2. The compound is an arylpropionic acid derivative that is used as an analgesic and anti-inflammatory agent. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Alminoprofen are not extensively reported. As an NSAID, it may have similar side effects to other drugs in this class, including gastrointestinal and renal toxicity. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References | |
| Additional Infomation |
Aminolprofen is a substituted aniline compound, a form of ibuprofen where the isobutyl group is replaced by a (2-methylprop-2-en-1-yl)amino group. It is a nonsteroidal anti-inflammatory drug (NSAID) used to treat inflammatory and rheumatic diseases. It possesses a variety of pharmacological activities, including NSAID, antirheumatic, antipyretic, EC 1.13.11.34 (arachidonic acid 5-lipoxygenase) inhibitor, EC 3.1.1.4 (phospholipase A2) inhibitor, cyclooxygenase 2 inhibitor, and non-narcotic analgesic. It is a monocarboxylic acid, substituted aniline, amino acid, and secondary amine compound. Aminolprofen is a nonsteroidal anti-inflammatory drug (NSAID), and its physicochemical properties classify it as a member of the phenylpropionic acid class of chemicals.
Alminoprofen is a non-steroidal anti-inflammatory drug (NSAID) that was first synthesized in 1977. It is used for the short-term management of dental, traumatic, and postpartum pain. The compound's anti-inflammatory and analgesic activities are mediated through the inhibition of COX-1 and COX-2 enzymes. Alminoprofen is classified as an arylpropionic acid derivative and is structurally derived from ibuprofen. |
| Molecular Formula |
C13H17NO2
|
|---|---|
| Molecular Weight |
219.27958
|
| Exact Mass |
219.126
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| Elemental Analysis |
C, 71.21; H, 7.81; N, 6.39; O, 14.59
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| CAS # |
39718-89-3
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| Related CAS # |
54362-71-9; 39718-89-3
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| PubChem CID |
2097
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| Appearance |
White to light yellow solid powder
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| Density |
1.107g/cm3
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| Boiling Point |
373.1ºC at 760 mmHg
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| Melting Point |
107°
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| Flash Point |
179.4ºC
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| Index of Refraction |
1.571
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| LogP |
2.935
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
16
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| Complexity |
255
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C1=CC=C(C=C1)NCC(=C)C)C(=O)O
|
| InChi Key |
FPHLBGOJWPEVME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H17NO2/c1-9(2)8-14-12-6-4-11(5-7-12)10(3)13(15)16/h4-7,10,14H,1,8H2,2-3H3,(H,15,16)
|
| Chemical Name |
2-[4-(2-methylprop-2-enylamino)phenyl]propanoic acid
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| Synonyms |
alminoprofen; EB 382; EB-382; EB382; 39718-89-3; Alminoprofene; Alminoprofeno; Minalfen
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~456.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.40 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 (11.40 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 (11.40 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 | 4.5604 mL | 22.8019 mL | 45.6038 mL | |
| 5 mM | 0.9121 mL | 4.5604 mL | 9.1208 mL | |
| 10 mM | 0.4560 mL | 2.2802 mL | 4.5604 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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