1. Immunology/Inflammation
  2. Interleukin Related
  3. NO-prednisolone

NO-prednisolone  (Synonyms: NO-泼尼松龙; NCX-1015)

目录号: HY-101757 纯度: 98.75%
COA 产品使用指南

NO-prednisolone 是释放一氧化氮 (NO) 的 Prednisolone 衍生物。NO-prednisolone 有效刺激体内 IL-10 产生。

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NO-prednisolone Chemical Structure

NO-prednisolone Chemical Structure

CAS No. : 327610-87-7

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10 mM * 1 mL in DMSO ¥3850
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1 mg ¥1590
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5 mg ¥3500
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10 mg ¥5600
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.

IC50 & Target[1]

IL-10

 

体外研究
(In Vitro)

NO-prednisolone (NCX-1015), an NO-releasing derivative of Prednisolone, is demonstrated to be more effective than Prednisolone in reducing inflammation, inhibiting cytokine and chemokine generation, and up-regulating the expression of the steroid-sensitive cell-surface marker CD163 in human peripheral blood mononuclear cells[1] Incubation of PBMCs with NO-prednisolone (NCX-1015) and Prednisolone produces a concentration-dependent activation of CD163. NO-prednisolone is more potent than Prednisolone at inducing CD163 cell surface expression. The increased efficacy of NO-prednisolone, compared with the parent molecule Prednisolone, is also observed when assessing inhibition of LPS induced IL-1β production[2].

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

体内研究
(In Vivo)

In vivo treatment with NO-prednisolone (NCX-1015) potently stimulates IL-10 production, suggesting that the NO steroid induces a regulatory subset of T cells that negatively modulates intestinal inflammation. The two doses of NO-prednisolone tested, 0.5 and 5 mg/kg/day (equivalent to 0.33 and 3.3 mg/kg/day prednisone, respectively) effectively attenuates the severity of the wasting syndrome, ameliorates the colitis score, and reduces the colonic myeloperoxidase (MPO) activity. NO-prednisolone administration also reduces the colonic mRNA and protein content of tumor necrosis factor-α, IL-12, and IFN-γ. NO-prednisolone also reduces the expression of inducible NO synthase and cyclooxygenase-2 but in contrast does not inhibit colonic expression of IL-10 mRNA or protein. In fact, IL-10 expression is enhanced in mice treated with NO-prednisolone[1].

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

分子量

539.57

Formula

C29H33NO9

CAS 号
性状

固体

颜色

White to yellow

中文名称

NO-泼尼松龙

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 : 25 mg/mL (46.33 mM; 超声助溶 (<60°C); 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 1.8533 mL 9.2666 mL 18.5333 mL
5 mM 0.3707 mL 1.8533 mL 3.7067 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (2.32 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 12.5 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。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.32 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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: ≥99.0%

参考文献
Kinase Assay
[2]

Peripheral blood mononuclear cells (PBMCs) are isolated from heparinized human whole venous blood using Ficoll-Hypaque (d=1.077 g). PBMCs are then washed three times with HEPES buffered RPMI 1640 containing 0.05% gentamycin and 10% donor serum. Cells (1×106, ~20% monocytes, the remainder having been lymphocytes) are transferred to a 48 well plate and pre-incubated for 1 h with Prednisolone, NO-prednisolone (10 μM-0.1 nM) or vehicle, followed by activation with LPS (1 μg/mL) for 24 h at 37°C and 5% CO2. Supernatants are removed and IL-1β production measured using a commercially available human IL-1β ELISA[2].

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

Animal Administration
[1]

Mice[1]
BALB/c and male Swiss Albino mice (6-8 weeks old) are used. Mice (12 per group) are injected intrarectally with 50% ethanol or 1, 1.5, 2, or 2.5 mg per mouse of TNBS. TNBS-treated mice then are treated s.c. with 5 mg/kg/day Prednisolone or NO-prednisolone for 7 days. Surviving mice are killed 8 days after TNBS administration, colonic inflammation is scored, and myeloperoxidase (MPO) activity is measured. After instillation of 1.5 mg per mouse of TNBS, animals are allocated randomly into one of three treatment groups [placebo, NO-prednisolone (5 or 0.5 mg/kg/day s.c.), or Prednisolone (10 or 5 mg/kg/day s.c.)] and followed for 7 days. Mice are monitored for the appearance of diarrhea, loss of body weight, and overall mortality. At the end of the experiment, surviving mice are killed, blood samples are collected by cardiac puncture, and a 7 cm segment of the colon is excised for macroscopic and microscopic damage evaluation. Colonic IL-2, IL-10, IFN-γ, and tumor necrosis factor-α (ELISA and RT-PCR) and MPO activity are assessed according to published methods. In duplicate experiments, the colons of surviving mice are excised for LPMC preparation.

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

参考文献

NO-prednisolone 相关分类

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 1.8533 mL 9.2666 mL 18.5333 mL 46.3332 mL
5 mM 0.3707 mL 1.8533 mL 3.7067 mL 9.2666 mL
10 mM 0.1853 mL 0.9267 mL 1.8533 mL 4.6333 mL
15 mM 0.1236 mL 0.6178 mL 1.2356 mL 3.0889 mL
20 mM 0.0927 mL 0.4633 mL 0.9267 mL 2.3167 mL
25 mM 0.0741 mL 0.3707 mL 0.7413 mL 1.8533 mL
30 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
40 mM 0.0463 mL 0.2317 mL 0.4633 mL 1.1583 mL
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    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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