Colchicine-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEColchicineCat. No.: HY-16569CAS No.: 64-86-8分式: CHNO分量: 399.44作靶点: Microtubule/Tubulin; Autophagy作通路: Cell Cycle/DNA Damage; Cytoskeleton; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验

2、DMSO : 48 mg/mL (120.17 mM)H2O : 33.33 mg/mL (83.44 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5035 mL 12.5175 mL 25.0350 mL5 mM 0.5007 mL 2.5035 mL 5.0070 mL10 mM 0.2504 mL 1.2518 mL 2.5035 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实

3、验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.21 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.21 m

4、M); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.21 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Colchicine微管蛋抑制剂和微管扰剂。 Colchicine抑制微管聚合的IC50为3 nM。IC50 & Target Microtubule/Tubulin 1体外研究 Exposure to 1M Colchicine, a microtub

5、ule disrupting agent, triggered apoptosis in rat cerebellar granulecells (CGC). Colchicine treatment also causes alterations in Ca2+ responses to chemical depolarization anda moderate, but progressive, increase in the resting intracellular Ca2+ concentration 1. Colchicine exerts itsbiological effect

6、s through binding to the soluble tubulin heterodimer, the major component of the microtubule.The Colchicine binding abilities of tubulins from a variety of sources are summarized, and the mechanism ofColchicine binding to brain tubulin is explored in depth. The relationship between colchicinoid stru

7、cture andtubulin binding activity provides insight into the structural features of Colchicine responsible for high affinitybinding to tubulin and is reviewed for analogs in the Colchicine series. The thermodynamic and kineticaspects of the association are described and evaluated in terms of the bind

8、ing mechanism. Colchicinebinding to tubulin results in unusual alterations in the low energy electronic spectra of Colchicine. Thespectroscopic features of Colchicine bound to tubulin are discussed in terms of the nature of the Colchicine-tubulin complex. Attempts to locate the high affinity Colchic

9、ine binding site on tubulin are presented 2.Colchicine treatment inhibits indomethacin-induced small intestinal injury by 86% (1 mg/kg) and 94% (3mg/kg) as indicated by the lesion index 24 h after indomethacin administration. Colchicine inhibits the proteinexpression of cleaved caspase-1 and mature

10、IL-1, without affecting the mRNA expression of NLRP3 and IL-1 3.体内研究 Vehicle or Colchicine (1 mg/kg) is administered orally 30 min prior to indomethacin administration. Thelesions stained with Evans blue in the small intestine are smaller in Colchicine-treated mice than those invehicle-treated mice

11、24 h after indomethacin administration. In addition, histological examination shows thatColchicine-treated mice have less mucosal inflammation and ulceration and a decrease in the size andnumbers of lesions compared with vehicle-treated mice. Colchicine treatment significantly reduces the lesioninde

12、x at doses of 1 mg/kg and 3 mg/kg (by 86% and 94%, respectively) compared with vehicle treatment.Colchicine treatment significantly inhibits the protein levels of mature IL-1 at doses of 1 mg/kg and 3 mg/kg(by 56% and 69%, respectively) without affecting those of pro-IL-1. Colchicine treatment also

13、significantlyinhibits the protein levels of cleaved caspase-1 at doses of 1 mg/kg and 3 mg/kg (by 26% and 39%,respectively) without affecting those of pro-caspase-1 3.PROTOCOLAnimal Mice 3Administration 3 Specific-pathogen-free 8-week-old male mice are used. Wild-type C57BL/6 mice and NLRP3/ mice on

14、 aC57BL/6 background are used. To examine the effects of Colchicine on NSAID-induced small intestinal2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEinjury, vehicle or Colchicine (1 or 3 mg/kg) is administered orally 30 min prior to indomethacin administration.Mice received intraperitoneal injectio

15、ns of sterilized phosphate buffered saline or mouse recombinant IL-1(0.1 g/kg) 3 h after indomethacin treatment. Vehicle or Colchicine (1 or 3 mg/kg) is also administered toNLRP3/ mice before indomethacin administration. The lesion index is evaluated 24 h after indomethacinadministration, and examin

16、ed mRNA and protein expression of inflammasome components 6 h afterindomethacin administration.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Biochim Biophys Acta. 2018 May;1862(5):1134-1147. Front Microbiol. 2019 May 9;10:939.See more cust

17、omer validations on HYPERLINK / www.MedChemEREFERENCES1. 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):377-4013. Otani K, et al. Colchicine prevents NSAID-induced small intestinal injury by inhibiting activa