LV-320 - CAS:2449093-46-1

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LV-320

目录号 : KM3485 CAS No. : 2449093-46-1 纯度 : ≥95%

Data Sheet 产品使用指南

LV-320 是一种有效且非竞争性的 ATG4B 抑制剂，其 IC₅₀ 值为 24.5 μM，K_d 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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC₅₀ of 24.5 µM and a K_d 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.

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

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.

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.

分子式

C₂₉NO₂S₂ClH₂₆

分子量

520.11

CAS号

2449093-46-1

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

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。
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。