Retro-2 - CAS:1201652-50-7

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Retro-2

目录号 : KM10167 CAS No. : 1201652-50-7 纯度 : ≥98%

Data Sheet 产品使用指南

Retro-2 是一种内体蛋白质-高尔基体逆行运输的选择性抑制剂。Retro-2 是一种埃博拉病毒 (EBOV) 感染抑制剂，在 HeLa 细胞中的EC₅₀ 为 12.2 µM。Retro-2 还可诱导细胞自噬 (autophagy)。

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生物活性

Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC₅₀ of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy.

体外研究

Retro-2 (1 μM; 1-4 hours) induces autophagy in GFP-LC3-expressing HeLa cells and promoted the dramatic cytoplasmic accumulation of large autophagosomes.
Retro-2 (1 μM; 0.5-4 hours) treatment hows an increase over time of the abundance of LC3-II protein in cells.
Retro-2 impairs the trafficking between autophagosomes and lysosomes. Retro-2 abolishes autolysosomes formation.
Retro-2 (20 μM; pretreatment for 30 min) inhibits HeLa cell intoxication by ricin, Shiga-like toxins 1 (Stx1) and 2 (Stx2).
Retro-2 blocked invasion of cells by the intracellular parasite Leishmania, as well as replication of non-enveloped viruses, including polyoma-, papilloma-, and adeno-associated viruses.

Cell Autophagy Assay

Cell Line:	HeLa cells
Concentration:	1 μM
Incubation Time:	1 hour, 2 hours, 4 hours
Result:	Resulted in a large significant increase in the number of small and large vesicles.

Western Blot Analysis

Cell Line:	HeLa cells
Concentration:	1 μM
Incubation Time:	0.5 hour, 2 hours, 4 hours
Result:	Showed an increase over time of the abundance of LC3-II protein in cells.

体内研究

Retro-2 (2-200 mg/kg; i.p; daily; for 21 days) treatment clearly protects from lethal nasal exposure to ricin in mice. 200 mg/kg of Retro-2 fully protects mice against ricin challenge.

Animal Model:	Female Balb/c mice (Pathogen-free 6-week-old) injected with ricin (2 μg/kg)
Dosage:	2 mg/kg, 10 mg/kg, 20 mg/kg, 200 mg/kg
Administration:	Intraperitoneal injection; daily; for 21 days
Result:	Protected mice against ricin challenge.

分子式

C₁₉H₁₆N₂Os

分子量

320.41

CAS号

1201652-50-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 250 mg/mL (780.25 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1210 mL	15.6050 mL	31.2100 mL
5 mM	0.6242 mL	3.1210 mL	6.2420 mL
10 mM	0.3121 mL	1.5605 mL	3.1210 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 (protect from light)。-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: 2.08 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.49 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 20.8 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% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.49 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 20.8 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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.49 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。