Retro-2
(Synonyms: RN 1-001) 目录号 : GC18485
Retro-2是一种强效埃博拉病毒（EBOV）感染抑制剂，EC50值为12.2μM。
Cas No.:1429192-00-6
Sample solution is provided at 25 µL, 10mM.
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Retro-2 is a potent ebolavirus (EBOV) infection inhibitor with an EC50 value of 12.2μM [1]. Retro-2 protects cells against ricin and Shiga toxin by blocking retrograde toxin transport at the early endosomes-TGN interface [2]. Retro-2 has been widely used to inhibit the replication of SARS-CoV-2 and to modify the Golgi structure[3].
In vitro, Retro-2 pretreatment at 20μM for 4 hours protected RAW264.7 cells from death caused by ricin toxin and restored protein synthesis function[4]. After 24 hours of treatment with 10μM Retro-2, the subcellular localization of Syntaxin 5 protein in HeLa cells was altered, and the abundance of Syntaxin 5 localized in the Golgi apparatus was decreased[5]. Treatment with 5μM Retro-2 for 4 hours induced autophagy in HeLa cells expressing GFP-LC3, accompanied by a significant increase in the number of large vesicles[6].
In vivo, Retro-2 (2.5μl; 20μM) was injected into the dentate gyrus of mice at a single dosage for 6 hours increased the generation activity of Aβ42 in the brain tissue of mice[7]. Retro-2 treatment via intraperitoneal injection at a single dose of 200mg/kg protected mice against intoxication by ricin and prolonged the survival of the mice[8].
References:
[1] Shtanko O, Sakurai Y, Reyes A N, et al. Retro-2 and its dihydroquinazolinone derivatives inhibit filovirus infection[J]. Antiviral research, 2018, 149: 154-163.
[2] Gupta N, Pons V, Noel R, et al. (S)-N-methyldihydroquinazolinones are the active enantiomers of Retro-2 derived compounds against toxins[J]. ACS medicinal chemistry letters, 2014, 5(1): 94-97.
[3] Yue X, Gim B, Zhu L, et al. Retro-2 alters Golgi structure[J]. Scientific Reports, 2022, 12(1): 14975.
[4] Jiao Z, Ke Y, Li S, et al. Pretreatment with retro‐2 protects cells from death caused by ricin toxin by retaining the capacity of protein synthesis[J]. Journal of Applied Toxicology, 2020, 40(10): 1440-1450.
[5] Morgens D W, Chan C, Kane A J, et al. Retro-2 protects cells from ricin toxicity by inhibiting ASNA1-mediated ER targeting and insertion of tail-anchored proteins[J]. Elife, 2019, 8: e48434.
[6] Nicolas V, Lievin-Le Moal V. Small trafficking inhibitor retro-2 disrupts the microtubule-dependent trafficking of autophagic vacuoles[J]. Frontiers in Cell and Developmental Biology, 2020, 8: 464.
[7] Kanatsu K, Hori Y, Ebinuma I, et al. Retrograde transport of γ‐secretase from endosomes to the trans‐Golgi network regulates Aβ42 production[J]. Journal of neurochemistry, 2018, 147(1): 110-123.
[8] Stechmann B, Bai S K, Gobbo E, et al. Inhibition of retrograde transport protects mice from lethal ricin challenge[J]. Cell, 2010, 141(2): 231-242.
Retro-2是一种强效埃博拉病毒（EBOV）感染抑制剂，EC50值为12.2μM[1]。Retro-2通过阻断早期内体与高尔基体反面网络界面之间的毒素逆行转运，保护细胞免受蓖麻毒素和志贺毒素的侵害[2]。Retro-2已被广泛用于抑制SARS-CoV-2的复制以及修饰高尔基体结构[3]。
在体外，使用20μM的Retro-2预处理4小时，保护了RAW264.7细胞免受蓖麻毒素引起的死亡，并恢复了蛋白质合成功能[4]。使用10μM的Retro-2处理24小时后，HeLa细胞中Syntaxin 5蛋白的亚细胞定位发生改变，定位于高尔基体的Syntaxin 5蛋白丰度降低[5]。使用5μM的Retro-2处理4小时，诱导了表达GFP-LC3的HeLa细胞发生自噬，并伴有大型囊泡数量的显著增加[6]。
在体内，向小鼠齿状回单次注射Retro-2（2.5μl；20μM）6小时，可增加小鼠脑组织中Aβ42的生成活性[7]。通过腹腔注射单次给予200mg/kg剂量的Retro-2，保护小鼠免受蓖麻毒素中毒，并延长了小鼠的存活时间[8]。
| Cell experiment [1]: | |
Cell lines | RAW264.7 cells |
Preparation Method | RAW264.7 cells were cultured in DMEM medium containing 10% fetal bovine serum, penicillin (100U/ml), and streptomycin (100μg/ml). The cells were cultured in a humidified environment at 37°C and 5% CO2. RAW264.7 cells were seeded at a density of 1.2×104 cells per well in a 96-well plate, and 100μl of the medium was added to each well. The cells were cultured for 24 hours. At 37°C, different concentrations of Retro-2 (10, 20, 30, and 40μM) were treated for 4h. In the presence of Retro-2 continuously, cells were treated with 200ng/ml ricin toxin. After the treatment, cell viability was detected. |
Reaction Conditions | 10, 20, 30, and 40μM; 4h |
Applications | Retro-2 treatment increased the viability of RAW264.7 cells challenged with ricin toxin in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female Balb/c mice |
Preparation Method | Six-week-old specific-pathogen-free (SPF) female Balb/c mice were housed under a 12-hour light/12-hour dark cycle and were allowed to freely access standard feed. One hour before intranasal administration of ricin, the mice were grouped. The control group was intraperitoneally injected with 500μl of sterile normal saline (0.9% NaCl), while the experimental group was intraperitoneally injected with a single dose of 200mg/kg Retro-2. The survival rates of the mice were then analyzed. |
Dosage form | 200mg/kg for once; i.p. |
Applications | Retro-2 treatment protected mice against intoxication by ricin and prolonged the survival of the mice. |
References: | |
| Cas No. | 1429192-00-6 | SDF | |
| 别名 | RN 1-001 | ||
| 化学名 | 2,3-dihydro-2-(5-methyl-2-thienyl)-3-phenyl-4(1H)-quinazolinone | ||
| Canonical SMILES | O=C1C2=CC=CC=C2NC(C3=CC=C(C)S3)N1C4=CC=CC=C4 | ||
| 分子式 | C19H16N2OS | 分子量 | 320.4 |
| 溶解度 | DMSO : ≥ 125 mg/mL (390.13 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1211 mL | 15.6055 mL | 31.211 mL |
| 5 mM | 624.2 μL | 3.1211 mL | 6.2422 mL |
| 10 mM | 312.1 μL | 1.5605 mL | 3.1211 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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