GLPBio

Colchicine

Catalog No.: GC13261Purity:>98.00%
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
Cas No.: 64-86-8
10mM (in 1mL DMSO)In Stock
$40.00
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250mgIn Stock
$36.00
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500mgIn Stock
$51.00
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Citations

4 publicationsPublications from researchers using this product

Description

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

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.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
64-86-8
Chemical Name
N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide
SMILES
CC(=O)NC1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC
Molecular Formula
C22H25NO6
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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