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Colchicine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Colchicine图片
CAS NO:64-86-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
200mg电议
500mg电议
1 g电议
5 g电议

产品名称
秋水仙碱
产品介绍
Colchicine 是微管蛋白 (tubulin) 抑制剂和微管 (microtubule) 干扰剂。 Colchicine 抑制微管聚合的IC50为 3 nM。Colchicine 还是α3甘氨酸受体 (GlyRs) 的竞争性拮抗剂。
生物活性

Colchicine is atubulininhibitor and amicrotubuledisrupting agent. Colchicine inhibits microtubule polymerization with anIC50of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of theα3 glycine receptors(GlyRs)[4].

IC50& Target

Microtubule/Tubulin[1]

体外研究
(In Vitro)

Exposure to 1μM Colchicine, a microtubule disrupting agent, triggered apoptosis in rat cerebellar granule cells (CGC). Colchicine treatment also causes alterations in Ca2+responses to chemical depolarization and a moderate, but progressive, increase in the resting intracellular Ca2+concentration[1]. Colchicine exerts its biological effects 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 of Colchicine binding to brain tubulin is explored in depth. The relationship between colchicinoid structure and tubulin binding activity provides insight into the structural features of Colchicine responsible for high affinity binding to tubulin and is reviewed for analogs in the Colchicine series. The thermodynamic and kinetic aspects of the association are described and evaluated in terms of the binding mechanism. Colchicine binding to tubulin results in unusual alterations in the low energy electronic spectra of Colchicine. The spectroscopic features of Colchicine bound to tubulin are discussed in terms of the nature of the Colchicine-tubulin complex. Attempts to locate the high affinity Colchicine binding site on tubulin are presented[2]. Colchicine treatment inhibits indomethacin-induced small intestinal injury by 86% (1 mg/kg) and 94% (3 mg/kg) as indicated by the lesion index 24 h after indomethacin administration. Colchicine inhibits the protein expression of cleaved caspase-1 and mature IL-1β, without affecting the mRNA expression of NLRP3 and IL-1β[3].

体内研究
(In Vivo)

Vehicle or Colchicine (1 mg/kg) is administered orally 30 min prior to indomethacin administration. The lesions stained with Evans blue in the small intestine are smaller in Colchicine-treated mice than those in vehicle-treated mice 24 h after indomethacin administration. In addition, histological examination shows that Colchicine-treated mice have less mucosal inflammation and ulceration and a decrease in the size and numbers of lesions compared with vehicle-treated mice. Colchicine treatment significantly reduces the lesion index 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-1β at doses of 1 mg/kg and 3 mg/kg (by 56% and 69%, respectively) without affecting those of pro-IL-1β. Colchicine treatment also significantly inhibits 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].

Clinical Trial
分子量

399.44

性状

Solid

Formula

C22H25NO6

CAS 号

64-86-8

中文名称

秋水仙素;秋水仙碱

结构分类
  • Others
来源
  • Plants
  • other families
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 48 mg/mL(120.17 mM)

H2O : ≥ 33.33 mg/mL(83.44 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5035 mL12.5175 mL25.0350 mL
5 mM0.5007 mL2.5035 mL5.0070 mL
10 mM0.2504 mL1.2518 mL2.5035 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 2.78 mg/mL (6.96 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。