Clonixin
Based on 1 Customer Validation
Clonixin (SCH-10304) is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.
For research use only. We do not sell to patients.
- Purity : 98.88%
- CAS No.: 17737-65-4
- Formula: C13H11ClN2O2
- Molecular Weight:262.69
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bone marrow cell | EC50 |
>20 μM
Compound: Clonixin
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Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
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[PMID: 27994748] |
| THP-1 | EC50 |
>20 μM
Compound: Clonixin
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Induction of human THP1 cell differentiation after 4 days by flow cytometry
Induction of human THP1 cell differentiation after 4 days by flow cytometry
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[PMID: 27994748] |
| U-937 | EC50 |
>20 μM
Compound: Clonixin
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Induction of human U937 cell differentiation after 4 days by flow cytometry
Induction of human U937 cell differentiation after 4 days by flow cytometry
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[PMID: 27994748] |
In Vivo
Clonixin (40-120 mg/kg; i.p.; single dose) produces dose-dependent analgesia in the rat formalin nociception model[3].
Clonixin (i.p.) has an intraperitoneal LD50 of 308.0 mg/kg in Wistar rats[3].
Clonixin (i.p.) has an intraperitoneal LD50 of 266.4 mg/kg in Swiss AsW mice[3].
Clonixin (Low-intermediate-high exposure doses; i.v.; single dose) produces dose-dependent hypotension and bradycardia in rats, with reversibility limited to low doses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (male, 4-6 weeks old, 200-250 g, bleomycin-induced pulmonary fibrosis)[1]
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Dosage:142 mg/kg
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Administration:p.o.; daily; 7 days (days 1-7 post-bleomycin or days 8-14 post-bleomycin)
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Result:Attenuated bleomycin-induced body weight loss.
Significantly reduced lung coefficient.
Significantly reduced airway resistance.
Markedly reduced total leukocyte count in bronchoalveolar lavage fluid (BALF).
Significantly reduced lymphocyte count in BALF.
Significantly reduced monocyte count in BALF.
Reduced lung tissue malondialdehyde (MDA) levels, and restored reduced glutathione (GSH), superoxide dismutase (SOD), and catalase levels.
Significantly reduced lung hydroxyproline content.
Significantly reduced Ashcroft fibrosis score.
Reduced immunohistochemical expression of fibrotic markers α-SMA, FAP, and TNF-α in lung tissue, particularly in the days 8-14 dosing group.
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Animal Model:Wistar (adult male and female; formalin-induced nociception model)[3]
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Dosage:40 mg/kg; 80 mg/kg; 120 mg/kg
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Administration:i.p.; single dose
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Result:Had no effect on formalin-induced nociceptive response at 40 mg/kg.
Produced significant, dose-dependent reductions in pain intensity ratings at 80 mg/kg and 120 mg/kg.
Showed non-linear temporal course of analgesia at 120 mg/kg, with pain ratings returning to control levels by end of 30-minute observation period.
Significantly reduced formalin-induced pain intensity when combined with nifedipine 5 mg/kg at 80 mg/kg.
Was approximately 10 times less potent than nifedipine and morphine in this assay.
Chemical Information
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CAS No. 17737-65-4
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Appearance Solid
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Molecular Weight 262.69
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Formula C13H11ClN2O2
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Color White to off-white
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SMILES
O=C(C1=CC=CN=C1NC2=CC=CC(Cl)=C2C)O
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Synonyms
SCH-10304
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (380.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Multiplex immunofluorescence IHC
Multiplex immunofluorescence IHC detects multiple protein biomarkers in one tissue section by sequential antibody staining, HRP-mediated tyramide fluorophore deposition, heat-mediated antibody stripping, nuclear counterstaining, multispectral imaging, spectral unmixing, and digital cell phenotyping; TSA deposits fluorophore near the antigen so the fluorescence signal remains after primary and secondary antibodies are removed, enabling repeated staining cycles, including with antibodies from the same host species. Classic FFPE tumor immune-profiling applications use panels such as CD3, CD8, CD68/CD163, FOXP3, PD-1, PD-L1, pancytokeratin, Ki67, and DAPI to identify tumor cells, immune-cell subsets, checkpoint-marker expression, co-expression phenotypes, cell density, and spatial relationships in the tumor microenvironment.
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Multiplex immunohistochemistry
Multiplex immunohistochemistry (mIHC), also known as tyramide dignal amplification (TSA), is an enzymatic detection method that uses horseradish peroxidase (HRP) to perform high-density in-situ labeling of target proteins or nucleic acids.
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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
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1].
Gawli C, et al. Repurposing clonixin and flunixin as anti-fibrotic candidates: Computational and preclinical evaluation in bleomycin-induced pulmonary fibrosis in rats. Res Vet Sci. 2025 Dec;197:105923.
[Content Brief]
[2].
Ferreira H, et al. Interaction of clonixin with EPC liposomes used as membrane models. J Pharm Sci. 2005 Jun;94(6):1277-87.
[Content Brief]
[3].
Bustamante D, et al. Analgesic action of clonixin, nifedipine and morphine using the formalin test. Gen Pharmacol. 1989;20(3):319-22.
[Content Brief]
[4].
Morales MA, et al. Vasorelaxant effect of the analgesic clonixin on rat aorta. Gen Pharmacol. 1995 Mar;26(2):425-30.
[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 | 3.8068 mL | 19.0338 mL | 38.0677 mL | 95.1692 mL |
| 5 mM | 0.7614 mL | 3.8068 mL | 7.6135 mL | 19.0338 mL | |
| 10 mM | 0.3807 mL | 1.9034 mL | 3.8068 mL | 9.5169 mL | |
| 15 mM | 0.2538 mL | 1.2689 mL | 2.5378 mL | 6.3446 mL | |
| 20 mM | 0.1903 mL | 0.9517 mL | 1.9034 mL | 4.7585 mL | |
| 25 mM | 0.1523 mL | 0.7614 mL | 1.5227 mL | 3.8068 mL | |
| 30 mM | 0.1269 mL | 0.6345 mL | 1.2689 mL | 3.1723 mL | |
| 40 mM | 0.0952 mL | 0.4758 mL | 0.9517 mL | 2.3792 mL | |
| 50 mM | 0.0761 mL | 0.3807 mL | 0.7614 mL | 1.9034 mL | |
| 60 mM | 0.0634 mL | 0.3172 mL | 0.6345 mL | 1.5862 mL | |
| 80 mM | 0.0476 mL | 0.2379 mL | 0.4758 mL | 1.1896 mL | |
| 100 mM | 0.0381 mL | 0.1903 mL | 0.3807 mL | 0.9517 mL |
Clonixin Related Classifications
HY-121235 Related Classifications
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Keywords
- Clonixin
- 17737-65-4
- SCH-10304
- SCH10304
- SCH 10304
- COX
- Calcium Channel
- TGF-β Receptor
- rat formalin nociception model
- EPC LUVs
- Swiss AsW mice
- voltage-operated type-L calcium channel
- EPC liposome bilayer
- Wistar rats
- male Sprague Dawley rats
- bleomycin-induced pulmonary fibrosis
- TGF-β
- idiopathic pulmonary fibrosis
- Inhibitor
- inhibitor
- inhibit