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Colchicine

MCE China：Colchicine

Brand：MedChemExpress (MCE)

Cat. No.HY-16569

CAS：64-86-8

Purity：99.95%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research.

In Vitro：Colchicine (5 μM; pretreated 24 h) inhibits MIRI-induced apoptosis of H9C2 by regulating the PI3K/AKT/eNOS pathway[3].

In Vivo：Colchicine can be used to induce Alzheimer's disease models[6]. .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of Alzheimer’s disease (AD)[6] Background Colchicine is a tubulin inhibitor that binds irreversibly to tubulin dimers and inhibits microtubule assembly with disruption of their polymerization, leading to neurofibrillary degeneration and synaptic loss. This causes neurotrophic factor intracellular trafficking to be disrupted, as well as axonal excitotoxicity and oxidative damage. Specific Mmodeling Methods Rat: Wistar • male • adult, weighing 180-220 g (acclimate: 1 weeks)Administration: 7.5 μg in 5 μL/site • intracerebroventricular (icv) injection • single dose Note (1) For induction of AD, rats are anesthetized using intraperitoneal (i.p.) Thiopental sodium (45 mg/kg) and then positioned in stereotaxic apparatus.(2) The stereotaxic coordinates are 0.8 mm posterior to bregma, 1.8 mm lateral to sagittal suture and 3.6 mm beneath the cortical surface.(3) Using a 28-gauge micro-syringe (10 μL) 15 μg Colchicine dissolved in 10 μL ACSF is injected bilaterally into the lateral ventricle (7.5 μg in 5 μL/site). The injection rate is 2 μL/min, then the micro-syringe is remained in place for 2 min to avoid withdrawal of the injected fluid.(4) Artificial cerebrospinal fluid (ACSF constituents in milli mole: NaCl 147, MgCl2 1.6, KCl 2.9, CaCl2 1.7, and Dextrose 2.2) is freshly prepared. Modeling Indicators Molecular changes: Induced indicators: Aβ 1-40 and Aβ 1-42 peptides level, MDA concentration, TNF-α level in both hippocampus and prefrontal cortex Decrease indicators: SOD activity in both hippocampus and prefrontal cortex Correlated Product(s): β-Amyloid (1-42), human TFA (HY-P1363) Opposite Product(s): Sacubitril/Valsartan (HY-18204A)

IC50 & Target：Microtubule/Tubulin[1] Cellular Effect Cell Line Type Value Description References

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References：

[1]. Bonfoco E, et al. Colchicine induces apoptosis in cerebellar granule cells. Exp Cell Res. 1995 May;218(1):189-200.  [Content Brief]

[2]. Hastie SB. Interactions of colchicine with tubulin. Pharmacol Ther. 1991;51(3):377-401  [Content Brief]

[3]. Yuanjun Tang, et al. Network Pharmacology-Based Investigation and Experimental Exploration of the Antiapoptotic Mechanism of Colchicine on Myocardial Ischemia Reperfusion Injury. Front Pharmacol. 2021 Dec 16:12:804030.  [Content Brief]

[4]. Otani K, et al. Colchicine prevents NSAID-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Sci Rep. 2016 Sep 2;6:32587.  [Content Brief]

[5]. Carola Muñoz-Montesino, et al. Inhibition of the Glycine Receptor alpha 3 Function by Colchicine. Front Pharmacol. 2020 Jul 30;11:1143.  [Content Brief]

[6]. Sami H Hammadi, et al. Effect of sacubitril/valsartan on cognitive impairment in colchicine-induced Alzheimer's model in rats. Fundam Clin Pharmacol. 2023 Apr;37(2):275-286.  [Content Brief]