标签归档：溶酶体

Vacuolin-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Vacuolin-1  纯度: 98.82%

Vacuolin-1 是一种有效的细胞渗透溶酶体胞吐 (lysosomal exocytosis) 抑制剂。Vacuolin-1 阻断了溶酶体 Ca2+ 依赖性的胞吐作用，在不影响再封闭过程的情况下阻止溶酶体内容物的释放。Vacuolin-1 是一种有效的选择性 PIKfyve 抑制剂，通过损害溶酶体成熟来抑制晚期自噬 (autophagy)。

Vacuolin-1

Vacuolin-1 Chemical Structure

CAS No. : 351986-85-1

规格 价格 是否有货 数量
5 mg ￥2650 In-stock
10 mg ￥4500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Vacuolin-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation[1][2].
体外研究
(In Vitro)

Vacuolin-1 (1 μM; Pretreatment 1 hour) blocks ionomycin-induced exocytosis of lysosomes but not of enlargeosomes. It results in vacuolation of lysosomes (A) and complete inhibition of the surface expression of Lamp-1[1].
Vacuolin-1 (1 μM; 20-180 min) disrupts the segregation of inner and limiting membranes characteristic of endosomes and lysosomes. Ultrastructural analysis also shows that vacuolin-1 favours fusion of inner and limiting membranes[1].
Vacuolin-1 (5 or 10 μM; 2 hours) blocks the Ca2+-dependent release of β-hexosaminidase from lysosomes. In HeLa cells, ionomycin results in the expected release of 18-20% of lysosomal β-hexosaminidase. But when cells pretreated with vacuolin-1, releases no more β-hexosaminidase compared with cells that are not exposed to ionomycin (4%)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

577.42

Formula

C26H24IN7O
CAS 号

351986-85-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 10 mg/mL (17.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7318 mL 8.6592 mL 17.3184 mL
5 mM 0.3464 mL 1.7318 mL 3.4637 mL
10 mM 0.1732 mL 0.8659 mL 1.7318 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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (1.73 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (1.73 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Jan Cerny, et al.The small chemical vacuolin-1 inhibits Ca(2+)-dependent lysosomal exocytosis but not cell resealing. EMBO Rep. 2004 Sep;5(9):883-8.

    [2]. Osamu Sano, et al. Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett. 2016 Jun;590(11):1576-85.

    [3]. Yingying Lu, et al. Vacuolin-1 potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A. Autophagy

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1-Dodecylimidazole(Synonyms: N-Dodecylimidazole)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

1-Dodecylimidazole (Synonyms: N-Dodecylimidazole) 纯度: 99.25%

1-Dodecylimidazole (N-Dodecylimidazole) 是一种溶酶体活性洗涤剂和细胞毒性剂。1-Dodecylimidazole 通过其在溶酶体中的酸依赖性积累、溶酶体膜的破坏和半胱氨酸蛋白酶释放到细胞质中而导致细胞死亡。1-Dodecylimidazole 具有降胆固醇和广谱抗真菌活性。

1-Dodecylimidazole(Synonyms: N-Dodecylimidazole)

1-Dodecylimidazole Chemical Structure

CAS No. : 4303-67-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
100 mg ￥350 In-stock
250 mg ￥600 In-stock
500 mg ￥850 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

1-Dodecylimidazole 相关产品

•相关化合物库:

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  • Anti-Infection Compound Library
  • Anti-Cancer Compound Library
  • Antifungal Compound Library

生物活性

1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity[1][2][3].

体外研究
(In Vitro)

N-dodecylimidazole, an acid activated detergent with a pKa of 6.3, has been shown to be cytotoxic to cells in culture. N-dodecylimidazole displayed extracellular pH (pHe)-dependent cytotoxicity against EMT-6 and MGH U1 cells. cell killing was dose dependent and was 100-fold greater at pHe 6.0 than pHe 7.0[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The hypocholesterolaemic activity of 1-dodecylimidazole results in part from the inhibition of cholesterol biosynthesis at the level of 2,3-oxidosqualene sterol cyclase[2].
1-dodecylimidazole (150 mg/kg body wt; by stomach tube; daily for 10 days) has lower serum cholesterol concentrations than control rats[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats[2]
Dosage: 150 mg/kg body wt
Administration: By stomach tube; daily for 10 days
Result: Had significantly lower serum cholesterol concentrations than untreated animals.

分子量

236.40

Formula

C15H28N2
CAS 号

4303-67-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (423.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.2301 mL 21.1506 mL 42.3012 mL
5 mM 0.8460 mL 4.2301 mL 8.4602 mL
10 mM 0.4230 mL 2.1151 mL 4.2301 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.58 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.58 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wilson PD, et al. A relationship between multidrug resistance and growth-state dependent cytotoxicity of the lysosomotropic detergent N-dodecylimidazole. Biochem Biophys Res Commun. 1991;176(3):1377-1382.

    [2]. Atkin SD, et al. The isolation of 2,3-oxidosqualene from the liver of rats treated with 1-dodecylimidazole, a novel hypocholesterolaemic agent. Biochem J. 1972;130(1):153-157.

    [3]. Firestone RA, et al. Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents. J Med Chem. 1987;30(8):1519-1521.

    [4]. Boyer MJ, et al. pH dependent cytotoxicity of N-dodecylimidazole: a compound that acquires detergent properties under acidic conditions. Br J Cancer. 1993;67(1):81-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务