Retro-2

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。

Retro-2  纯度: ≥98.0%

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)。

Retro-2

Retro-2 Chemical Structure

CAS No. : 1201652-50-7

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50 mg ¥9500 In-stock
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Retro-2 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Autophagy Compound Library
  • Antiparasitic Compound library

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[1][2][3].

IC50 & Target

EC50: 12.2 µM (Ebolavirus)[3]

体外研究
(In Vitro)

Retro-2 (1 μM; 1-4 hours) induces autophagy in GFP-LC3-expressing HeLa cells and promoted the dramatic cytoplasmic accumulation of large autophagosomes[2].
Retro-2 (1 μM; 0.5-4 hours) treatment hows an increase over time of the abundance of LC3-II protein in cells[2].
Retro-2 impairs the trafficking between autophagosomes and lysosomes. Retro-2 abolishes autolysosomes formation[2].
Retro-2 (20 μM; pretreatment for 30 min) inhibits HeLa cell intoxication by ricin, Shiga-like toxins 1 (Stx1) and 2 (Stx2)[1].
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[3].

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.

Cell Autophagy Assay[2]

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[2]

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
(In Vivo)

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[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.

Animal Model: Female Balb/c mice (Pathogen-free 6-week-old) injected with ricin (2 μg/kg)[1]
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.

分子量

320.41

Formula

C19H16N2OS

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。

    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: 2.08 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。

    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: ≥ 2.08 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。

*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]. Bahne Stechmann, et al. Inhibition of retrograde transport protects mice from lethal ricin challenge. Cell. 2010 Apr 16;141(2):231-42.

    [2]. Valérie Nicolas, et al. Small Trafficking Inhibitor Retro-2 Disrupts the Microtubule-Dependent Trafficking of Autophagic Vacuoles. Front Cell Dev Biol. 2020 Jun 18;8:464.

    [3]. Olena Shtanko, et al. Retro-2 and its dihydroquinazolinone derivatives inhibit filovirus infection. Antiviral Res. 2018 Jan;149:154-163.

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