LV-320,95.0%

产品编号:Bellancom-112711| CAS NO:2449093-46-1| 分子式:C29H26ClNO2S2| 分子量:520.11

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-112711
4500.00 杭州 北京(现货)
Bellancom-112711
7500.00 杭州 北京(现货)
Bellancom-112711
22500.00 杭州 北京(现货)

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LV-320

产品介绍 LV-320 是一种有效且非竞争性的 ATG4B抑制剂,其 IC50 值为 24.5 μM,Kd 值为 16 μM。 LV-320 抑制 ATG4B 的酶促活性,阻断细胞自噬,并且在体内稳定,无毒且有活性。
生物活性

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.

体外研究

LV-320 (0-120 µM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment results in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines.
LV-320 (120 µM; 48 hours; MDA-MB-231 cells) treatment results in an increase in LC3B-II, indicating that LV-320 blocks autophagic flux.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: SKBR3, MCF7, JIMT1, and MDA-MB-231 cells
Concentration: 0 µM, 25 µM, 50 µM, 75 µM, 100 µM, or 120 µM
Incubation Time:
Result: Resulted in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines.

Cell Autophagy Assay

Cell Line: MDA-MB-231 cells
Concentration: 120 µM
Incubation Time: 48 hours
Result: Blocked autophagic flux.
体内研究
(In Vivo)

LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GFP-LC3 mice (females, 9-14 weeks)
Dosage: 100 mg/kg or 200 mg/kg
Administration: Oral gavage; three times over two days (Pharmacokinetic study)
Result: Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased.
体内研究

LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GFP-LC3 mice (females, 9-14 weeks)
Dosage: 100 mg/kg or 200 mg/kg
Administration: Oral gavage; three times over two days (Pharmacokinetic study)
Result: Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased.
体内研究

LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: GFP-LC3 mice (females, 9-14 weeks)
Dosage: 100 mg/kg or 200 mg/kg
Administration: Oral gavage; three times over two days (Pharmacokinetic study)
Result: Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased.
性状Solid
溶解性数据
In Vitro: 

DMSO : 135 mg/mL (259.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9227 mL 9.6134 mL 19.2267 mL
5 mM 0.3845 mL 1.9227 mL 3.8453 mL
10 mM 0.1923 mL 0.9613 mL 1.9227 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: ≥ 2.25 mg/mL (4.33 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (4.33 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 22.5 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: ≥ 2.25 mg/mL (4.33 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (4.33 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 22.5 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 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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