Colchicine |
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Catalog No.GC13261
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Colchicine, an orally active alkaloid, disrupts cytoskeletal function by inhibiting the polymerization of β-tubulin into microtubules, with an IC50 of 3 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 64-86-8
Sample solution is provided at 25 µL, 10mM.
Colchicine, an orally active alkaloid, disrupts cytoskeletal function by inhibiting the polymerization of β-tubulin into microtubules, with an IC50 of 3 nM. Additionally, colchicine acts as a competitive antagonist of the α3 glycine receptor (GlyR) [1]. Colchicine exhibits a broad spectrum of anti-inflammatory, immunosuppressive, and potent anti-fibrotic effects, making it effective in controlling gout and reducing the risk of cardiovascular events [2-3].
Colchicine(10 nM; 1h) prevented foam cell formation induced by ox-LDL in macrophages differentiated from human THP-1 cells[4]. Colchicine (1 nM; 24h) treatment diminished GSK-3β phosphorylation and β-catenin translocation to the nucleus in cultured human aortic SMCs exposed to PDGF-BB stimulation[5].
Colchicine (0.102 mg/kg; 12 weeks; i.g) demonstrates anti-atherosclerotic and plaque-stabilizing effects at low doses by inhibiting foam cell formation and reducing cholesterol crystal-induced inflammation[4]. Colchicine (0.1 mg/kg/d; i.p.; 2 weeks) can restrict abdominal aortic aneurysm (AAA) formation by preventing the infiltration of immune cells into the aortic wall[6]. Colchicine inhibits the activation of the NLRP3 inflammasome, thereby preventing small intestine damage induced by non-steroidal anti-inflammatory drugs (NSAIDs)[7].
References:
[1]. Muñoz-Montesino C, Burgos CF, et,al. Inhibition of the Glycine Receptor alpha 3 Function by Colchicine. Front Pharmacol. 2020 Jul 30;11:1143. doi: 10.3389/fphar.2020.01143. PMID: 32903667; PMCID: PMC7438739.
[2]. McKenzie BJ, Wechalekar MD, et,al. Colchicine for acute gout. Cochrane Database Syst Rev. 2021 Aug 26;8(8):CD006190. doi: 10.1002/14651858.CD006190.pub3. PMID: 34438469; PMCID: PMC8407279.
[3]. Zhang FS, He QZ, et,al.Therapeutic potential of colchicine in cardiovascular medicine: a pharmacological review. Acta Pharmacol Sin. 2022 Sep;43(9):2173-2190. doi: 10.1038/s41401-021-00835-w. Epub 2022 Jan 19. PMID: 35046517; PMCID: PMC8767044.
[4]. Schwarz N, Fernando S, et,al. Colchicine exerts anti-atherosclerotic and -plaque-stabilizing effects targeting foam cell formation. FASEB J. 2023 Apr;37(4):e22846. doi: 10.1096/fj.202201469R. PMID: 36856983.
[5]. Chen M, Yang D, et,al. Colchicine Blocks Abdominal Aortic Aneurysm Development by Maintaining Vascular Smooth Muscle Cell Homeostasis. Int J Biol Sci. 2024 Mar 17;20(6):2092-2110. doi: 10.7150/ijbs.93544. PMID: 38617538; PMCID: PMC11008260.
[6]. Zhao Y, Shen QR, et,al. Colchicine protects against the development of experimental abdominal aortic aneurysm. Clin Sci (Lond). 2023 Oct 11;137(19):1533-1545. doi: 10.1042/CS20230499. PMID: 37748024; PMCID: PMC10550771.
[7]. Otani K, Watanabe T, et,al. Colchicine prevents NSAID-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Sci Rep. 2016 Sep 2;6:32587. doi: 10.1038/srep32587. PMID: 27585971; PMCID: PMC5009328.
| Cell experiment [1]: | |
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Cell lines |
MDMs (Human monocyte-derived macrophages) differentiated from human THP-1 cells |
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Preparation Method |
For studying human ORO foam cell formation, MDMs were initially treated for 1 hour with colchicine (10 nM), vinblastine (10 nM), or paclitaxel (100 nM), and subsequently exposed to ox-LDL as described previously. |
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Reaction Conditions |
10 nM; 1h |
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Applications |
Colchicine prevented foam cell formation induced by oxidized LDL (ox-LDL) in macrophages differentiated from human THP-1 cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL / 6J Apoe−/− mice |
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Preparation Method |
Mice were fed an atherogenic high-cholesterol diet (HCD) containing 0.15% cholesterol and 21% fat for 16 weeks, starting at 8 weeks of age. In the fourth week, they were randomly assigned to receive either phosphate-buffered saline (PBS) or colchicine at 0.102 mg/kg via daily oral gavage for 12 weeks. |
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Dosage form |
0.102 mg/kg; 12weeks; i.g |
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Applications |
Colchicine reduces lipidic atherosclerotic plaques in mouse aorta. |
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References: |
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| Cas No. | 64-86-8 | SDF | |
| Chemical Name | N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide | ||
| Canonical SMILES | CC(=O)NC1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC | ||
| Formula | C22H25NO6 | M.Wt | 399.44 |
| Solubility | ≥ 19.972 mg/mL in DMSO, ≥ 50.8 mg/mL in EtOH with gentle warming, ≥ 45.5 mg/mL in Water with gentle warming | Storage | Store at 4°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5035 mL | 12.5175 mL | 25.035 mL |
| 5 mM | 500.7 μL | 2.5035 mL | 5.007 mL |
| 10 mM | 250.4 μL | 1.2518 mL | 2.5035 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)