Colchicine [64-86-8]
Referencia HY-16569-1ml
embalaje : 10mM/1mL
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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.
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Colchicine Estructura química
No. CAS : 64-86-8
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- Colchicine plays an antipyroptosis role by inhibiting intracellular oxidative stress. HUVECs are treated for 10 or 24 h with different doses of Colchicine (0-10 nM) in the presence of cholesterol crystal (0.5 mg/mL). Intracellular ROS level is detected using a DCFH-DA probe. JC-1 Staining Kit is used for the detection of mitochondrial membrane potential.
- Colchicine alleviates NLRP3 inflammasome activation relevant in pyroptosis. HUVECs are treated for 24 h with different doses of Colchicine (0-10 nM) in the presence of cholesterol crystal (0.5 mg/mL. Western blotting Is dedicated to examine the protein expression levels of NLRP3, ASC-1, procaspase-1, caspase-1, IL-18, and IL-1β. Colchicine treatment significantly blocks NLRP3 signal activity. Colchicine significantly inhibits CC-induced mRNA and protein expression of IL-18 and IL-1β, particularl
- CS1 and Colchicine (Col) induce the phosphorylation of H1 (T18) and H3 (S29) as detected by western blotting.
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| 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. | Microtubule/Tubulin | ||||||||||||||||
| In Vitro | Colchicine (5 μM; pretreated 24 h) inhibits MIRI-induced apoptosis of H9C2 by regulating the PI3K/AKT/eNOS pathway. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis Analysis
Western Blot Analysis
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| In Vivo | Colchicine (1, 3 mg/kg; orally 30 min prior) causes less mucosal inflammation and ulceration and a decrease in the size and numbers of lesions compared with vehicle-treated mice with Indomethacin (HY-14397). Induction of Alzheimer’s disease (AD) 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 Rats: 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 同类产品: β-Amyloid (1-42), human TFA (HY-P1363) 拮抗产品:Sacubitril/Valsartan (HY-18204A) MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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| White to light yellow | |||||||||||||||||
| CC(N[C@H](C1=C2)CCC3=CC(OC)=C(OC)C(OC)=C3C1=CC=C(OC)C2=O)=O | |||||||||||||||||
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Room temperature in continental US; may vary elsewhere. | |||||||||||||||||
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| In Vitro: DMSO : ≥ 48 mg/mL (120.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : ≥ 33.33 mg/mL (83.44 mM) *"≥" means soluble, but saturation unknown. Preparing Stock Solutions
View the 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. * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo: For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator Please enter the basic information of animal experiments: Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Calculation results: Working solution concentration: mg/mL This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details. The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE). | |||||||||||||||||
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[1]. Bonfoco E, et al. Colchicine induces apoptosis in cerebellar granule cells. Exp Cell Res. 1995 May;218(1):189-200.
[2]. Hastie SB. Interactions of colchicine with tubulin. Pharmacol Ther. 1991;51(3):377-401
[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.
[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.
[5]. Carola Muñoz-Montesino, et al. Inhibition of the Glycine Receptor alpha 3 Function by Colchicine. Front Pharmacol. 2020 Jul 30;11:1143.
[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.
* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.5035 mL | 12.5175 mL | 25.0350 mL | 62.5876 mL |
| 5 mM | 0.5007 mL | 2.5035 mL | 5.0070 mL | 12.5175 mL | |
| 10 mM | 0.2504 mL | 1.2518 mL | 2.5035 mL | 6.2588 mL | |
| 15 mM | 0.1669 mL | 0.8345 mL | 1.6690 mL | 4.1725 mL | |
| 20 mM | 0.1252 mL | 0.6259 mL | 1.2518 mL | 3.1294 mL | |
| 25 mM | 0.1001 mL | 0.5007 mL | 1.0014 mL | 2.5035 mL | |
| 30 mM | 0.0835 mL | 0.4173 mL | 0.8345 mL | 2.0863 mL | |
| 40 mM | 0.0626 mL | 0.3129 mL | 0.6259 mL | 1.5647 mL | |
| 50 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL | 1.2518 mL | |
| 60 mM | 0.0417 mL | 0.2086 mL | 0.4173 mL | 1.0431 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3129 mL | 0.7823 mL | |
| DMSO | 100 mM | 0.0250 mL | 0.1252 mL | 0.2504 mL | 0.6259 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
- Induced Disease Models Products
- Nervous System Disease Models
- Alzheimer's Disease Models
- Cell Cycle/DNA Damage Cytoskeleton Immunology/Inflammation Autophagy Apoptosis
- Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis
- Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Colchicine64-86-8Microtubule/TubulinNOD-like Receptor (NLR)AutophagyApoptosisOrallyalkaloidtubulinmicrotubuleα3 glycine receptorsGlyRsnon-steroidal anti-inflammatory drugNSAIDintestinal injuryimmunosuppressiveanti-fibrosisgouty arthritisAlzheimer’s diseaseADInhibitorinhibitorinhibit
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- Nombre del producto:
- Colchicine
- Cat. No.:
- HY-16569
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