中文名称: SP187
英文名称: SP187
CAS No: 615253-61-7
分子式: C16H33NO5
分子量: 319.44
S10628 SP187 ≥98% (psaitong)
包装规格:
1mg 5mg 10mg 20mg 50mg 100mg in glass bottle
产品描述:

基本信息

产品编号:S10628 

产品名称:SP187

CAS:

615253-61-7

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C16H33NO5

溶于液体

-80℃

六个月

分子量

319.44

-20℃

一个月

化学名: 

(2R,3R,4R,5S)-2-(hydroxymethyl)-1-(9-methoxynonyl)piperidine-3,4,5-triol

 

Solubility (25°C)

 

体外

DMSO

 

Ethanol

 

Water

 

体内

现配现用

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

生物活性

产品描述

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。

靶点/IC50

EBOV

IC50: 29.97μM

MARV

47.72μM

 

体外研究

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 47.72μM for EBOV and MARV, respectively.

 

体内研究

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

 

推荐实验方法(仅供参考)

细胞实验:

 

Cell Assay

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 62.5μM). 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 1mL 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.

 

动物实验:

 

Animal Administration

Mice 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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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摩尔浓度计算公式

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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    C8=C7/X C8: LOG(C8):