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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Amfenac Sodium monohydrate (AHR 5850; AHR5850; AHR5850), the sodium salt of amfenac which is an NSAID, is a non-steroidal analgesic anti-inflammatory agent with antipyretic and analgesic activities. It acts as an inhibitor of COX-1 and COX-2 enzymes with IC50s of 15.3 and 20.4 nM, respectively. Amfenac is transformed in vivo to the active metabolite nepafenac which is also a non-steroidal anti-inflammatory drug (NSAID).
| Targets |
COX-2; non-steroidal anti-inflammatory drug/NSAIDs
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| ln Vitro |
The rate of cell proliferation is higher in transfected COX-2-expressing cells than non-transfected ones. All cell lines exhibit a considerable reduction in proliferation rate upon the addition of Amfenac Sodium Hydrate. The addition of melanoma conditioned media inhibits the generation of nitric oxide by macrophages; this inhibition is somewhat alleviated by the addition of amfenac sodium hydroxide[1]. The findings indicate that Amfenac Sodium Hydrate prevents B-glucuronidase from being released: in the presence of 10 -8 and 10-7 M FMLP, respectively, 5×10-4 M Amfenac Sodium Hydrate prevents the release of the enzyme by 35.3 and 16.3%, respectively. After 16 minutes of incubation with 10-8 M FMLP, the aggregation of polymorphonuclear leukocytes (PMNs) is inhibited by 28.3% upon the addition of 10-4 M Amfenac Sodium Hydrate[2].
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| ln Vivo |
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| Cell Assay |
Human uveal melanoma cell lines were transfected to constitutively express COX-2 and the proliferative rate of these cells using two different methods, with and without the addition of Amfenac, was measured. Nitric oxide production by macrophages was measured after exposure to melanoma-conditioned medium from both groups of cells as well as with and without Amfenac, the active metabolite of Nepafenac.
Results: Cells transfected to express COX-2 had a higher proliferation rate than those that did not. The addition of Amfenac significantly decreased the proliferation rate of all cell lines. Nitric oxide production by macrophages was inhibited by the addition of melanoma conditioned medium, the addition of Amfenac partially overcame this inhibition. Conclusion: Amfenac affected both COX-2 transfected and non-transfected uveal melanoma cells in terms of their proliferation rates as well as their suppressive effects on macrophage cytotoxic activity[1]. |
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| Animal Protocol |
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| Toxicity/Toxicokinetics |
rat LD50 oral 311 mg/kg BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY); BEHAVIORAL: ATAXIA; GASTROINTESTINAL: OTHER CHANGES Agents and Actions, A Swiss Journal of Pharmacology., 7(133), 1977 [PMID:871089]
rat LD50 subcutaneous 240 mg/kg Iyakuhin Kenkyu. Study of Medical Supplies., 16(1461), 1985 rat LD50 intravenous 277 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); GASTROINTESTINAL: HYPERMOTILITY, DIARRHEA Journal of Toxicological Sciences., 9(87), 1984 [PMID:6471132] rat LD50 intramuscular 277 mg/kg Iyakuhin Kenkyu. Study of Medical Supplies., 16(1461), 1985 mouse LD50 oral 615 mg/kg BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY); GASTROINTESTINAL: ULCERATION OR BLEEDING FROM STOMACH; BLOOD: OTHER CHANGES Agents and Actions, A Swiss Journal of Pharmacology., 7(133), 1977 [PMID:871089] |
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| References |
[1]. Marshall JC, et al. The effects of a cyclooxygenase-2 (COX-2) expression and inhibition on human uveal melanoma cell proliferation and macrophage nitric oxide production. J Carcinog. 2007 Nov 27;6:17.
[2]. Matsumoto T, et al. Effect of a non-steroidal anti-inflammatory drug (amfenac sodium) on polymorphonuclear leukocytes. Pharmacol Res Commun. 1982 Jun;14(6):523-32 |
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| Additional Infomation |
Amfenac sodium hydrate is a hydrate that is the monohydrate of the sodium salt of amfenac. It has a role as an antipyretic, a cyclooxygenase 2 inhibitor, a cyclooxygenase 1 inhibitor, a non-narcotic analgesic and a non-steroidal anti-inflammatory drug. It contains a sodium (2-amino-3-benzoylphenyl)acetate.
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| Molecular Formula |
C15H12NO3.H2O.NA
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| Molecular Weight |
295.27
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| Exact Mass |
295.082
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| Elemental Analysis |
C, 61.02; H, 4.78; N, 4.74; Na, 7.79; O, 21.67
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| CAS # |
61618-27-7
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| Related CAS # |
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| PubChem CID |
23663941
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| Appearance |
Typically exists as Light yellow to yellow solid at room temperature
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| Boiling Point |
520ºC at 760 mmHg
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| Melting Point |
242-244ºC
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| Flash Point |
268.3ºC
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| LogP |
1.309
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
342
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Na+].O=C(C1C([H])=C([H])C([H])=C([H])C=1[H])C1=C([H])C([H])=C([H])C(C([H])([H])C(=O)[O-])=C1N([H])[H].O([H])[H]
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| InChi Key |
QZNJPJDUBTYMRS-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H13NO3.Na.H2O/c16-14-11(9-13(17)18)7-4-8-12(14)15(19)10-5-2-1-3-6-10;;/h1-8H,9,16H2,(H,17,18);;1H2/q;+1;/p-1
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| Chemical Name |
Benzeneacetic acid, 2-amino-3-benzoyl-, sodium salt, monohydrate
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| Synonyms |
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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, avoid exposure to moisture. |
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| 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) |
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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 | 3.3867 mL | 16.9337 mL | 33.8673 mL | |
| 5 mM | 0.6773 mL | 3.3867 mL | 6.7735 mL | |
| 10 mM | 0.3387 mL | 1.6934 mL | 3.3867 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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