1. Anti-infection
  2. Dengue virus Flavivirus
  3. SP187

SP187  (Synonyms: MON-​DNJ; UV4)

目录号: HY-U00160 纯度: ≥98.0%
COA 产品使用指南

SP187 是一种靶向作用于宿主的针对丝状病毒感染的亚胺糖。SP187 在体内抗流感和登革热。

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SP187 Chemical Structure

SP187 Chemical Structure

CAS No. : 615253-61-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥6600
In-stock
1 mg ¥3000
In-stock
5 mg ¥6000
In-stock
10 mg ¥9300
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

IC50: 29.97 μM (EBOV), 47.72 μM (MARV)[1]

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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 naïve mice. No efficacy is observed in the iminosugar treated mice as compared to the vehicle control[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

319.44

Formula

C16H33NO5

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (313.05 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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 6.2610 mL
查看完整储备液配制表

* 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。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.83 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.83 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.30%

参考文献
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1305 mL 15.6524 mL 31.3048 mL 78.2620 mL
5 mM 0.6261 mL 3.1305 mL 6.2610 mL 15.6524 mL
10 mM 0.3130 mL 1.5652 mL 3.1305 mL 7.8262 mL
15 mM 0.2087 mL 1.0435 mL 2.0870 mL 5.2175 mL
20 mM 0.1565 mL 0.7826 mL 1.5652 mL 3.9131 mL
25 mM 0.1252 mL 0.6261 mL 1.2522 mL 3.1305 mL
30 mM 0.1043 mL 0.5217 mL 1.0435 mL 2.6087 mL
40 mM 0.0783 mL 0.3913 mL 0.7826 mL 1.9565 mL
50 mM 0.0626 mL 0.3130 mL 0.6261 mL 1.5652 mL
60 mM 0.0522 mL 0.2609 mL 0.5217 mL 1.3044 mL
80 mM 0.0391 mL 0.1957 mL 0.3913 mL 0.9783 mL
100 mM 0.0313 mL 0.1565 mL 0.3130 mL 0.7826 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
HY-U00160
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