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)。
| 生物活性 | Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is anebolavirus (EBOV)infectioninhibitor with anEC50of 12.2 μM in HeLa cells. Retro-2 induces cellautophagy[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 parasiteLeishmania, as well as replication of non-enveloped viruses, including polyoma-, papilloma-, and adeno-associated viruses[3].
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. |
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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].
| 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. |
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| 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 | 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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。 *以上所有助溶剂都可在本网站选购。
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