| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
Alclofenac, a drug of the non-steroidal anti-inflammatory drug (NSAIDs) class, has been used to treat patients with chronic rheumatic diseases but was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash. Alclofenac has a pronounced effect upon the acute-phase protein response and the extent to which L-tryptophan is bound to plasma protein.
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Alclofenac absorption in the gastrointestinal tract is irregular. Peak plasma concentrations are reached within 1–4 hours after oral or rectal administration. Alclofenac is primarily excreted in the urine as glucuronide and the unchanged active substance. The volume of distribution is 0.1 L/kg. At an oral dose of 500 mg: renal clearance (mean) 35 ml/min; total clearance (mean) 37–69 ml/min. Metabolism/Metabolites The main metabolites are alclofenac and its glucuronide. Biological Half-Life The plasma half-life is 1.5 to 5.5 hours. |
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| Toxicity/Toxicokinetics |
The binding rate of protein to plasma proteins is 90-99%.
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| References |
J Chromatogr. 1993 Nov 24;621(2):209-14.
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| Additional Infomation |
Alclofenac is an aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid. It was a nonsteroidal anti-inflammatory drug (NSAID) withdrawn from the UK market in 1979 due to concerns about its association with vasculitis and rashes. It is a nonsteroidal anti-inflammatory drug, a non-narcotic analgesic, and also a drug allergen. It is an aromatic ether, a monocarboxylic acid, and belongs to the monochlorobenzene class of compounds. The drug was withdrawn from the UK market in 1979. Drug Indications Alclofenac is indicated for rheumatic diseases, particularly for the treatment of rheumatoid arthritis and ankylosing spondylitis, and can be used as an analgesic for painful arthritis. Mechanism of Action Alclofenac is a prostaglandin H2 synthase inhibitor. It inhibits the activity of cyclooxygenase by reversibly blocking its activity. Therefore, it can prevent the production of inflammatory mediators (and pain) such as prostacyclin and prostaglandins. Alclofenac's ability to inhibit prostaglandin biosynthesis is likely an important factor in the action of this type of drug. In addition, the fact that these drugs displace endogenous anti-inflammatory substances from plasma protein binding sites is also considered an equally important factor in their mechanism of action.
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| Molecular Formula |
C11H11O3CL
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|---|---|
| Molecular Weight |
226.65624
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| Exact Mass |
226.04
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| CAS # |
22131-79-9
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| Related CAS # |
22131-79-9 (Alclofenac); 59960-34-8 (Alclofenac lysinate); 24049-18-1 (Alclofenac sodium)
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| PubChem CID |
30951
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| Appearance |
White to off-white solid
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| Density |
1.252g/cm3
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| Boiling Point |
368.3ºC at 760mmHg
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| Flash Point |
176.6ºC
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| Vapour Pressure |
4.49E-06mmHg at 25°C
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| Index of Refraction |
1.553
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| LogP |
2.531
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
15
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| Complexity |
230
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C=CCOC1=C(C=C(C=C1)CC(=O)O)Cl
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| InChi Key |
ARHWPKZXBHOEEE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H11ClO3/c1-2-5-15-10-4-3-8(6-9(10)12)7-11(13)14/h2-4,6H,1,5,7H2,(H,13,14)
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| Chemical Name |
(4-(Allyloxy)-3-chlorophenyl)acetic acid
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| Synonyms |
W 7320; W-7320; W7320; MY 101; MY-101; MY101; BRN 2116510; BRN-2116510; BRN2116510.
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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 |
| 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: ~16.7 mg/mL (~73.6 mM; with ultrasonication and warming by heating to 60°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (16.7 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 1.67 mg/mL (7.37 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 DMSO stock solution (16.7 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 1.67 mg/mL (7.37 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 DMSO stock solution (16.7 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4119 mL | 22.0595 mL | 44.1189 mL | |
| 5 mM | 0.8824 mL | 4.4119 mL | 8.8238 mL | |
| 10 mM | 0.4412 mL | 2.2059 mL | 4.4119 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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