| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Fentiazac acts as a COX inhibitor, targeting cyclooxygenase enzymes involved in the production of prostaglandins. By inhibiting COX, fentiazac reduces the synthesis of pro-inflammatory prostaglandins, leading to its anti-inflammatory, analgesic, and antipyretic effects. The compound's platelet anti-aggregation activity is also related to its inhibition of prostaglandin synthesis.
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| ln Vitro |
Fentiazac demonstrates anti-inflammatory, analgesic, and antipyretic activity in vitro. Its activity can be assessed using various in vitro assays, including COX inhibition assays and assays measuring prostaglandin production. The compound's platelet anti-aggregation activity can be evaluated using platelet aggregation assays.
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| ln Vivo |
Rats, monkeys, and dogs were able to tolerate repeated oral administration of fentizac without substantial alterations in blood chemistry, heart function, or bone marrow function [1]. Fentizac tolerance in dogs, rats, and monkeys [1]. Rats 0–50 mg/kg/day 90 days, Red monkeys 40 mg/kg/day 90 days, African green monkeys 0–8 mg/kg/day 79–93 days, and Tengus 16.6 mg/kg/day 180 days are the species-tolerated dose dosing days.
Fentiazac is used in vivo as an anti-inflammatory and analgesic agent. It has been used for the treatment of chronic arthritis, osteoarthritis, periarthritis of the shoulder, low back pain, and respiratory tract inflammation. It has also been used for inflammation and pain following trauma, surgery, and tooth extraction. The compound's efficacy has been demonstrated in clinical studies. |
| Enzyme Assay |
Non-cellular enzyme assays for fentiazac involve assessing its inhibition of COX-1 and COX-2 enzymes using purified enzyme preparations. The enzyme activity is measured by monitoring the conversion of arachidonic acid to prostaglandins using a spectrophotometric or radiometric assay. IC50 values for COX-1 and COX-2 inhibition are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for fentiazac involve treating inflammatory cells (e.g., macrophages) with the compound and measuring prostaglandin E2 (PGE2) production. Cells are stimulated with lipopolysaccharide (LPS) to induce COX-2 expression, and PGE2 levels in the culture medium are quantified by ELISA. The inhibition of PGE2 production by fentiazac is measured, and the IC50 is determined. Platelet anti-aggregation activity is assessed using platelet-rich plasma and aggregating agents.
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| Animal Protocol |
In vivo animal experiments with fentiazac involve administering the compound to rodent models of inflammation and pain. In the carrageenan-induced paw edema model, rats are treated with fentiazac, and paw swelling is measured. In pain models such as the acetic acid writhing test or the hot plate test, the compound's analgesic effects are assessed. Pharmacokinetic studies have been conducted in humans.
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| ADME/Pharmacokinetics |
Fentiazac has a molecular weight of 329.80-329.81 and a molecular formula of C17H12ClNO2S. It is a solid at room temperature and is typically stored at room temperature. Purity is typically ≥98%. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Fentiazac is generally well-tolerated at therapeutic doses. Like other NSAIDs, it can cause gastrointestinal side effects including dyspepsia, nausea, and gastric ulceration. It may also affect renal function and platelet aggregation. The compound should be used with caution in patients with a history of peptic ulcer disease or renal impairment.
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| References |
[1]. Emilio Marmo, et al. Experimental and clinical pharmacology of fentiazac, a new, non-steroidal anti-inflammatory agent. Current Medical Research and Opinion.Volume 6, 1979 - Issue sup2.
[2]. Gabor Katona, et al. Efficacy and tolerability of fentiazac in rheumatoid arthritis: Double-blind study versus indomethacin. Current Medical Research and Opinion. Volume 6, 1979 - Issue sup2. [3]. Famaey JP, Gaci O, Ginsberg F. Fentiazac in the treatment of osteoarthritis and tendinitis. Curr Med Res Opin. 1983;8(9):675-81. |
| Additional Infomation |
2-[4-(4-chlorophenyl)-2-phenyl-5-thiazolyl]acetic acid is a member of the thiazole class of compounds.
Fentiazac (BR-700; CAS 18046-21-4) is a non-steroidal anti-inflammatory agent with analgesic, antipyretic, and platelet anti-aggregation activity. It has been used for the treatment of chronic arthritis, osteoarthritis, periarthritis of the shoulder, low back pain, and respiratory tract inflammation. The compound has also been used for inflammation and pain following trauma, surgery, and tooth extraction. Fentiazac is available from various commercial suppliers for research applications. |
| Molecular Formula |
C17H12NO2SCL
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|---|---|
| Molecular Weight |
329.80068
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| Exact Mass |
329.028
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| CAS # |
18046-21-4
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| Related CAS # |
85721-24-0 (calcium);96593-16-7 (sodium);18046-21-4 (free acid);
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| PubChem CID |
28871
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| Appearance |
White to off-white solid powder
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| Density |
1.362g/cm3
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| Boiling Point |
556.2ºC at 760mmHg
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| Melting Point |
162ºC
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| Flash Point |
290.2ºC
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| Vapour Pressure |
3.3E-13mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
4.757
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
381
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(C2=C(CC(O)=O)SC(C3C=CC=CC=3)=N2)=CC=1
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| InChi Key |
JIEKMACRVQTPRC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12ClNO2S/c18-13-8-6-11(7-9-13)16-14(10-15(20)21)22-17(19-16)12-4-2-1-3-5-12/h1-9H,10H2,(H,20,21)
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| Chemical Name |
2-[4-(4-chlorophenyl)-2-phenyl-1,3-thiazol-5-yl]acetic acid
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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 : ~100 mg/mL (~303.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.58 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 (7.58 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 (7.58 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 | 3.0321 mL | 15.1607 mL | 30.3214 mL | |
| 5 mM | 0.6064 mL | 3.0321 mL | 6.0643 mL | |
| 10 mM | 0.3032 mL | 1.5161 mL | 3.0321 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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