Fenclozic acid
Based on 1 Customer Validation
Fenclozic acid (ICI-54450) is an orally active anti-inflammatory, analgesic, and antipyretic agent. Fenclozic acid exhibits anti-inflammatory activity in Edadjuvant-induced arthritis and Carrageenin-induced oedema in rats. Fenclozic acid can be used for the research of arthritis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.52%
- CAS No.: 17969-20-9
- Formule: C11H8ClNO2S
- Masse moléculaire:253.70
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
>1000 μM
Compound: Fenclozic acid
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Fenclozic acid
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
In Vitro
Fenclozic acid (0.5-5 mM) is not significantly metabolized by isolated rat duodenal mucosal whole cells or homogenates, with <5% converted to a decarboxylated derivative[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Fenclozic acid (2.5-50 mg/kg; p.o.; daily; 14 days) exhibits anti-inflammatory activity in developing and establish edadjuvant-induced arthritis in rats[2].
Fenclozic acid (10, 30, and 90 mg/kg; p.o.; single dose) exhibits anti-inflammatory activity in Carrageenin-induced oedema in rats[2].
Fenclozic acid (25-100 mg/kg; p.o.; single dose) exhibits antipyretic activity in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mature MRC-hooded rats (200-350g)[1]
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Dosage:100 mg/kg
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Administration:p.o.; two doses 15 hours apart; or daily for 6 days
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Result:Increased tryptophan pyrrolase activity from a control level of 4.4 units/g liver to 13.7 units/g liver (two-dose regime).
Increased tryptophan pyrrolase activity from a control level of 4.4 units/g liver to 14.0 units/g liver (six-day daily regime).
Achieved an approximate three-fold increase in enzyme activity regardless of dose schedule.
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Animal Model:Male Alderley Park strain I (200 g) with arthritis induced by Adjuvant[2]
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Dosage:2.5; 5; 10; 20; 25; 45; 50 mg/kg
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Administration:p.o.; daily; 14 days (starting 1 day before adjuvant injection)
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Result:Produced 41% inhibition of injected foot thickness increase on day 3 and 53% inhibition on day 14 at 20 mg/kg.
Associated with improved body weight gain compared to untreated controls.
Produced a dose-dependent decrease in foot thickness of both injected and non-injected hind feet over 14 days of treatment.
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Animal Model:Male Alderley Park strain I (200 g) with oedema induced by Carrageenin[2]
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Dosage:10; 30; 90 mg/kg
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Administration:p.o.; single dose; 3 hours before Carrageenin injection
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Result:Produced a dose-dependent reduction in carrageenin-induced foot swelling.
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Animal Model:Male Alderley Park strain I (200 g) intravenously injected with Pertussis vaccine B.P.
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Dosage:25; 50; 100 mg/kg
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Administration:p.o.; single dose; immediately before Pertussis vaccine injection
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Result:Completely prevented the pyrogen-induced increase in body temperature at 100 mg/kg.
Partially suppressed the temperature rise at 50 mg/kg and 25 mg/kg doses.
Chemical Information
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CAS No. 17969-20-9
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Appearance Solid
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Masse moléculaire 253.70
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Formule C11H8ClNO2S
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Color White to light yellow
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SMILES
O=C(O)CC1=CSC(C2=CC=C(Cl)C=C2)=N1
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Synonyms
ICI-54450; Acidum fenclozicum; Mialex
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (394.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
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- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Curtis CG, et al. The fate of fenclozic acid in the gut and its effect on some aspects of gut metabolism. Xenobiotica. 1983;13(8):483-496. [Content Brief]
[2]. Newbould BB, et al. The pharmacology of fenclozic acid (2-(4-chlorophenyl)-thiazol-4-ylacetic acid; I.C.I. 54,450; 'Myalex'); a new compound with anti-inflammatory, analgesic and antipyretic activityl. Br J Pharmacol. 1969;35(3):487-497. [Content Brief]
[3]. Martin S, et al. Identification of the reactive metabolites of fenclozic acid in bile duct cannulated rats. Anal Chem. 2014;86(22):11281-11289. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.9417 mL | 19.7083 mL | 39.4166 mL | 98.5416 mL |
| 5 mM | 0.7883 mL | 3.9417 mL | 7.8833 mL | 19.7083 mL | |
| 10 mM | 0.3942 mL | 1.9708 mL | 3.9417 mL | 9.8542 mL | |
| 15 mM | 0.2628 mL | 1.3139 mL | 2.6278 mL | 6.5694 mL | |
| 20 mM | 0.1971 mL | 0.9854 mL | 1.9708 mL | 4.9271 mL | |
| 25 mM | 0.1577 mL | 0.7883 mL | 1.5767 mL | 3.9417 mL | |
| 30 mM | 0.1314 mL | 0.6569 mL | 1.3139 mL | 3.2847 mL | |
| 40 mM | 0.0985 mL | 0.4927 mL | 0.9854 mL | 2.4635 mL | |
| 50 mM | 0.0788 mL | 0.3942 mL | 0.7883 mL | 1.9708 mL | |
| 60 mM | 0.0657 mL | 0.3285 mL | 0.6569 mL | 1.6424 mL | |
| 80 mM | 0.0493 mL | 0.2464 mL | 0.4927 mL | 1.2318 mL | |
| 100 mM | 0.0394 mL | 0.1971 mL | 0.3942 mL | 0.9854 mL |
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