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Colchicine Data Sheet

Product Name: Colchicine
CAS No.: 64-86-8
Cat. No.: HY-16569
MWt: 399.44
Formula: C22H25NO6
Purity : >98%
Solubility: H<sub>2</sub>O : ≥ 33.33 mg/mL;DMSO : ≥ 48 mg/mL
Mechanisms: Target: Cancer
Biological Activity:
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[1][2][3][4][5]. IC50 & Target:Microtubule/Tubulin[1] 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 (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)[4].
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
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)

Caution: Not fully tested. For research purposes only

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