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Colchicine

Catalog No.GC13261 Copy One-Click Copy Product Info

Colchicine, an orally active alkaloid, disrupts cytoskeletal function by inhibiting the polymerization of β-tubulin into microtubules, with an IC50 of 3 nM.

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Colchicine Chemical Structure

Cas No.: 64-86-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$40.00
In stock
250mg
$36.00
In stock
500mg
$51.00
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Sample solution is provided at 25 µL, 10mM.



Product has been cited by 4 publications

Description of Colchicine

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.

Protocol of Colchicine

Cell experiment [1]:

Cell lines

MDMs (Human monocyte-derived macrophages) differentiated from human THP-1 cells 

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. 

Reaction Conditions

10 nM; 1h 

Applications

Colchicine prevented foam cell formation induced by oxidized LDL (ox-LDL) in macrophages differentiated from human THP-1 cells. 
Animal experiment [2]:

Animal models

C57BL / 6J Apoe−/− mice 

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. 

Dosage form

0.102 mg/kg; 12weeks; i.g 

Applications

Colchicine reduces lipidic atherosclerotic plaques in mouse aorta. 

References:
[1]. 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.

Chemical Properties of Colchicine

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Colchicine

Prepare stock solution
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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In vivo Formulation Calculator (Clear solution) of Colchicine

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Related Video of Colchicine

    Colchicine-GlpBio

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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