ZaltoprofenCyclooxygenase (COX) inhibitor CAS# 74711-43-6 |
- Ebrotidine
Catalog No.:BCC1542
CAS No.:100981-43-9
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| 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. |
||
| 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. |
||
| 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. | |||||
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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
- 5-Hydroxyxanthotoxin
Catalog No.:BCC8107
CAS No.:7471-73-0
- Hydroxychloroquine Sulfate
Catalog No.:BCC5560
CAS No.:747-36-4
- Vibsanin C
Catalog No.:BCN4590
CAS No.:74690-89-4
- 1-Methoxycarbonyl-beta-carboline-N-oxide
Catalog No.:BCN8205
CAS No.:74690-74-7
- 4-hydroxy-1-methoxycarbonyl-beta-carboline
Catalog No.:BCN7909
CAS No.:74690-72-5
- 3-Methoxy-4,5-methylenedioxycinnamaldehyde
Catalog No.:BCN1364
CAS No.:74683-19-5
- Nuclear yellow
Catalog No.:BCC1810
CAS No.:74681-68-8
- 1,3,9-Trimethyluric acid
Catalog No.:BCN7393
CAS No.:7464-93-9
- Liquiritin Apioside
Catalog No.:BCC8334
CAS No.:74639-14-8
- 11-Hydroxydrim-7-en-6-one
Catalog No.:BCN7770
CAS No.:74635-87-3
- ent-3Beta-Angeloyloxykaur-16-en-19-oic acid
Catalog No.:BCN1365
CAS No.:74635-61-3
- Tylosin tartrate
Catalog No.:BCC4875
CAS No.:74610-55-2
- Secoxyloganin methyl ester
Catalog No.:BCN4299
CAS No.:74713-15-8
- Pterolactone A
Catalog No.:BCN6513
CAS No.:74730-10-2
- AUY922 (NVP-AUY922)
Catalog No.:BCC2123
CAS No.:747412-49-3
- VER-50589
Catalog No.:BCC5296
CAS No.:747413-08-7
- Ciglitazone
Catalog No.:BCC7014
CAS No.:74772-77-3
- Methylophiopogonone B
Catalog No.:BCN8182
CAS No.:74805-89-3
- Methylophiopogonone A
Catalog No.:BCN2841
CAS No.:74805-90-6
- Methylophiopogonanone B
Catalog No.:BCN5418
CAS No.:74805-91-7
- Methylophiopogonanone A
Catalog No.:BCN5417
CAS No.:74805-92-8
- Zalcitabine
Catalog No.:BCC5026
CAS No.:7481-89-2
- 3',5'-Anhydrothymidine
Catalog No.:BCC8596
CAS No.:7481-90-5
- GRP (porcine)
Catalog No.:BCC5809
CAS No.:74815-57-9
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.
