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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.88%
- CAS. Nr.: 17737-65-4
- Formel: C13H11ClN2O2
- Molecular Weight:262.69
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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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] |
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. Nr. 17737-65-4
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Appearance Solid
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Molecular Weight 262.69
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
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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)
Verweise
[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 |
|---|---|---|---|---|---|
| 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
- 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