ZaltoprofenCyclooxygenase (COX) inhibitor CAS# 74711-43-6 |
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| Cas No. | 74711-43-6 | SDF | Download SDF |
| PubChem ID | 5720 | Appearance | Powder |
| Formula | C17H14O3S | M.Wt | 298.36 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | CN100 | ||
| Solubility | DMSO : ≥ 100 mg/mL (335.17 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-(6-oxo-5H-benzo[b][1]benzothiepin-3-yl)propanoic acid | ||
| SMILES | CC(C1=CC2=C(C=C1)SC3=CC=CC=C3C(=O)C2)C(=O)O | ||
| Standard InChIKey | MUXFZBHBYYYLTH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8,10H,9H2,1H3,(H,19,20) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Zaltoprofen(CN100) is an inhibitor of COX for treatment of arthritis.
Target: COX
Zaltoprofen, a preferential COX-2 inhibitor, exhibited a potent inhibitory action on the nociceptive responses induced by a retrograde infusion of bradykinin into the right common carotid artery in rats. Zaltoprofen had a moderate inhibitory effect compared with those of the above-mentioned NSAIDs. the inhibitory effect of zaltoprofen on bradykinin-induced nociceptive responses is not explainable by the inhibition of cyclooxygenase (COX). Zaltoprofen did not bind to B(1) and B(2) receptors in a radio-ligand binding assay. In the cultured dorsal root ganglion cells of mature mice, zaltoprofen completely inhibited the bradykinin-induced increase of [Ca(2+)](i), which was inhibited by B(2) antagonist D-Arg-[Hyp(3), Thi(5,8), D-Phe(7)]-bradykinin, but not by B(1) antagonist. [1]. References: | |||||
Zaltoprofen Dilution Calculator
Zaltoprofen Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.3517 mL | 16.7583 mL | 33.5166 mL | 67.0331 mL | 83.7914 mL |
| 5 mM | 0.6703 mL | 3.3517 mL | 6.7033 mL | 13.4066 mL | 16.7583 mL |
| 10 mM | 0.3352 mL | 1.6758 mL | 3.3517 mL | 6.7033 mL | 8.3791 mL |
| 50 mM | 0.067 mL | 0.3352 mL | 0.6703 mL | 1.3407 mL | 1.6758 mL |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.6703 mL | 0.8379 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Zaltoprofen is a cyclooxygenase (COX) inhibitor that displays slight preferential inhibition for COX-2 (IC50s = 1.3 and 0.34 μM for COX-1 and COX-2, respectively).Independent of COX inhibition, zaltoprofen has also been reported to inhibit bradykinin-indu
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Oleic Acid Coated Gelatin Nanoparticles Impregnated Gel for Sustained Delivery of Zaltoprofen: Formulation and Textural Characterization.[Pubmed:26819927]
Adv Pharm Bull. 2015 Nov;5(4):537-48.
PURPOSE: In the present study, we have formulated Zaltoprofen loaded, surface decorated, biodegradable gelatin nanogel and evaluated its texture characterization. METHODS: The method used to prepare gelatin nanoparticles (GNP) was 'two step desolvation' and its surface decoration was performed with oleic acid (OA). The GNP was optimized by DOE software. Nanogels were evaluated for particle size entrapment efficiency, texture properties, SEM, in-vitro, ex-vivo drug release studies, in-vitro characterization, stability and in vivo evaluation of nanogel for anti-inflammatory activity was carried out by carrageenan induced rat paw edema method as an anti-inflammatory experimental model. RESULTS: The formulated GNP with particle size and entrapment efficiency of optimized batch was found to be 247.1 nm and 76.21% respectively. The SEM of GNP shows smooth and spherical shape. In-vitro and Ex-vivo drug release shows that there was 69.47% and 78.59% drug released within 48 hrs. It follows Ritger peppas model, which indicates sustained drug release. The good texture properties of nanogel were observed from texture analysis graphs.In vivo studies of our formulation give significant results compared to the marketed nanogel. Stability data revealed stability of nanogel formulation up to 3 months. CONCLUSION: The present approach can provide us promising results of the sustained analgesic activity and the stability of drug within the GNP.
Development of a drug-in-adhesive patch combining ion pair and chemical enhancer strategy for transdermal delivery of zaltoprofen: pharmacokinetic, pharmacodynamic and in vitro/in vivo correlation evaluation.[Pubmed:27257038]
Drug Deliv. 2016 Nov;23(9):3461-3470.
The aim of the study was to develop a drug-in-adhesive patch system for transdermal delivery of Zaltoprofen (ZAL). The formulation was designed in combination with the ion pair and chemical enhancer strategy. Seven organic amines were chosen as counter ions, and the prepared ion pairs were characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The in vivo pharmacokinetic performance of ZAL was studied on rabbits following transdermal and intravenous administration. A deconvolution method was applied to determine the correlation between the in vitro permeation and the in vivo absorption. Acetic acid-induced writhing response was conducted on mice to evaluate the analgesic effect. In vitro permeation results showed that both ion pairs and chemical enhancers were effective in modulating ZAL skin permeation from patches. The enhancement ratio was negatively correlated to the polar surface area (PSA) of counter ions, and was positively correlated to the octanol-water partition coefficient (log Ko/w) of chemical enhancers, respectively. The optimized formulation contained 10% (w/w) ZAL-triethylamine and 10% (w/w) isopropyl myristate, with DURO-TAK(R) 87-4098 as the pressure sensitive adhesive matrix. Furthermore, the in vitro permeation data were well correlated with the in vivo absorption data. The analgesic effect of the optimized patch was comparable to the commercial indometacin plasters. In conclusion, it was feasible for transdermal delivery of ZAL by the synergistic action of ion pair and chemical enhancer, and the in vitro permeation data were indicative of the in vivo performance for the developed patches.
Preparation, optimization, and evaluation of Zaltoprofen-loaded microemulsion and microemulsion-based gel for transdermal delivery.[Pubmed:26785055]
J Liposome Res. 2016 Dec;26(4):297-306.
CONTEXT: Zaltoprofen, a non-steroidal anti-inflammatory drug, has potent inhibitory action against nociceptive responses. However, gastrointestinal ulcer accompanied with anemia due to the bleeding are most cited side effects associated with it. Due to this, administration of Zaltoprofen is not suitable for individuals with gastric ulcer. Thus, there is unmet need to develop an alternative delivery system that will be easy to administer and can avoid ulcerogenic side effects associated with it. OBJECTIVE: Present study was aimed to prepare and evaluate microemulsion (ME) and microemulsion-based gel formulation of Zaltoprofen for transdermal delivery. MATERIALS AND METHODS: Pseudo-ternary phase diagrams were utilized to prepare ME formulations. Effect of surfactant and co-surfactant mass ratio on the ME formation and permeation of ME were evaluated and formulation was optimized. Permeation studies were performed using excised pigskin was studied. Efficacy of optimized formulations was evaluated in rat model of inflammation and pain. RESULTS: Composition of optimized formulation was 1% (w/w) Zaltoprofen, 20% (w/w) Capryol 90, 50% (w/w) Smix (2:1, Cremophor RH 40 and Transcutol P). Optimized formulation showed globule size of 22.11 nm, polydispersity index of 0.251 and zeta potential of -11.4 mV. ME gel was found safe in skin irritation study. Significant analgesic activity and anti-inflammatory activity of ME gel was observed in hot plate test and rat paw edema test, respectively. CONCLUSION: In conclusion, results of present study suggest that ME could be a promising formulation for transdermal administration of Zaltoprofen.
Co-grinding Effect on Crystalline Zaltoprofen with beta-cyclodextrin/Cucurbit[7]uril in Tablet Formulation.[Pubmed:28368030]
Sci Rep. 2017 Apr 3;7:45984.
This work aimed to investigate the co-grinding effects of beta-cyclodextrin (beta-CD) and cucurbit[7]uril (CB[7]) on crystalline Zaltoprofen (ZPF) in tablet formulation. Crystalline ZPF was prepared through anti-solvent recrystallization and fully analyzed through single-crystal X-ray diffraction. Co-ground dispersions and mono-ground ZPF were prepared using a ball grinding process. Results revealed that mono-ground ZPF slightly affected the solid state, solubility, and dissolution of crystalline ZPF. Co-ground dispersions exhibited completely amorphous states and elicited a significant reinforcing effect on drug solubility. UV-vis spectroscopy, XRPD, FT-IR, DSC, ssNMR, and molecular docking demonstrated the interactions in the amorphous product. Hardness tests on blank tablets with different beta-CD and CB[7] contents suggested the addition of beta-CD or CB[7] could enhance the compressibility of the powder mixture. Disintegration tests showed that CB[7] could efficiently shorten the disintegrating time. Dissolution tests indicated that beta-CD and CB[7] could accelerate the drug dissolution rate via different mechanisms. Specifically, CB[7] could accelerate the dissolution rate by improving disintegration and beta-CD showed a distinct advantage in solubility enhancement. Based on the comparative study on beta-CD and CB[7] for tablet formulation combined with co-grinding, we found that CB[7] could be considered a promising drug delivery, which acted as a disintegrant.
