SP187 (MON-DNJ)
(Synonyms: MON-?DNJ; UV4) 目录号 : GC32247
SP187 (MON-DNJ) 是一种靶向宿主的亚氨基糖，在体外和体内具有抗丝状病毒感染的活性。
Cas No.:615253-61-7
Sample solution is provided at 25 µL, 10mM.
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SP187 is a host-targeted iminosugar with activity against filovirus infections in vitro and in vivo. SP187 is active against influenza and dengue in vivo.
The antiviral activity of iminosugar SP187 (UV-4) in vitro against EBOV and MARV is assessed using a yield-plaque assay format and the IC50 is determined. Antiviral activity for SP187 is observed with IC50 of 29.97 and 47.72 μM for EBOV and MARV, respectively[1].
The efficacy of SP187 (UV-4), the active free base component of UV-4B, and UV-5, the most potent iminosugar tested in vitro, is first assessed using a mouse model of EBOV infection. In this study, C57Bl/6 mice are administered 10 or 100 mg/kg of SP187 or UV-5 via oral gavage or IP injection. Dosing started ~1h before infection with ~1000 pfu of mouse-adapted EBOV and is repeated BID for 10 days at approximately 12 hour intervals for UV-5 or TID at approximately 8 hour intervals for SP187. The selected doses and schedule are based on tolerability studies in na?ve mice. No efficacy is observed in the iminosugar treated mice as compared to the vehicle control[1].
[1]. Warfield KL, et al. Assessment of the potential for host-targeted iminosugars UV-4 and UV-5 activity against filovirus infections in vitro and in vivo. Antiviral Res. 2017 Feb;138:22-31.
Cell experiment: | To test the activity of the iminosugars UV-1, UV-2, UV-3, SP187 (UV-4) and UV-5 against EBOV (Zaire-Kikwit) or MARV (Ci67), a yield-plaque assay is conducted in Vero cells. Multiple concentrations of compounds are incubated on 24-well plates of Vero cells for 1h at 8 concentrations (2 fold dilutions starting at 62.5 μM). After ~1h, pretreatment medium is aspirated and virus inoculums added (MOI of 0.1 with EBOV or MARV). After an additional hour of infection, virus inoculum is removed (no washing) and 1 mL of compound medium is added at the final concentration. After incubation for 72 hours, supernatants are harvested and competent viral particles released from the cells are enumerated by plaque assay in duplicate. Percent inhibition is determined by comparing DMSO-treated cells (average value) infected with virus to those treated with compound at the various concentrations. The IC50 are calculated using GraphPad Prism based on the % inhibition at each concentration[1]. |
Animal experiment: | Mice[1] Mouseadapted EBOV and MARV-Ravn are used to infect female C57Bl/6 or BALB/c mice with target challenge dose of 1000 pfu via intraperitoneal injection. SP187 (free base) and UV-5 are prepared in acidified water for oral gavage (PO) or in phosphate buffered saline (PBS) for intraperitoneal infection (IP) and subcutaneous (SQ) delivery. SP187 (UV-4) or UV-5 are administered via PO, IP or SQ for 7-10 days starting 30-60 minutes before virus challenge at 5, 10, 20, or 100 mg/kg or vehicle only (water for PO or PBS for IP delivery). Compounds are administered either twice (BID) or three times (TID) daily at 12 or 8 hour intervals, respectively. Weights, morbidity and mortality are monitored for up to 21 days. Animals which displaye severe illness are euthanized based on predefined scoring systems. |
References: [1]. Warfield KL, et al. Assessment of the potential for host-targeted iminosugars UV-4 and UV-5 activity against filovirus infections in vitro and in vivo. Antiviral Res. 2017 Feb;138:22-31. | |
| Cas No. | 615253-61-7 | SDF | |
| 别名 | MON-?DNJ; UV4 | ||
| Canonical SMILES | OC[C@H]1N(C[C@H](O)[C@@H](O)[C@@H]1O)CCCCCCCCCOC | ||
| 分子式 | C16H33NO5 | 分子量 | 319.44 |
| 溶解度 | DMSO : 100 mg/mL (313.05 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| 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 | 3.1305 mL | 15.6524 mL | 31.3048 mL |
| 5 mM | 0.6261 mL | 3.1305 mL | 6.261 mL |
| 10 mM | 0.313 mL | 1.5652 mL | 3.1305 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet