1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Glucocorticoid Receptor Endogenous Metabolite
  3. Prednisolone

Prednisolone  (Synonyms: 泼尼松龙)

目录号: HY-17463 纯度: 99.85%
COA 产品使用指南 技术支持

Prednisolone 是一种有效的,口服活性的皮质类固醇和糖皮质激素。Prednisolone 的抗炎活性约为氢化可的松的四倍,同时减少了盐和水的保留。Prednisolone 可用于眼部抗炎研究。

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Prednisolone Chemical Structure

Prednisolone Chemical Structure

CAS No. : 50-24-8

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Other Forms of Prednisolone:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 EC50
0.002 nM
Compound: 2, pred
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
[PMID: 21899328]
A549 EC50
13.6 nM
Compound: 2, pred
Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 21073190]
A549 EC50
13.6 nM
Compound: pred
Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 19321341]
A549 EC50
14.4 nM
Compound: 2, pred
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 21899328]
A549 EC50
15.8 nM
Compound: 2, pred
Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay
Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay
[PMID: 21073190]
A549 EC50
16.1 nM
Compound: 2, pred
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
[PMID: 21899328]
A549 IC50
5.8 nM
Compound: Prednisolone
Antiinflammatory activity in human A549 cells assessed as inhibition of IL1beta-induced IL6 production preincubated for 30 mins followed by IL1beta-stimulation and measured after 20 hrs by AlphaLisa assay
Antiinflammatory activity in human A549 cells assessed as inhibition of IL1beta-induced IL6 production preincubated for 30 mins followed by IL1beta-stimulation and measured after 20 hrs by AlphaLisa assay
[PMID: 30384041]
C2C12 EC50
3.4 nM
Compound: Prednisolone
Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
[PMID: 15808489]
CV-1 ED50
4 nM
Compound: prednisolone
Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay
Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay
[PMID: 18032610]
HeLa EC50
16 nM
Compound: 1b
Activation of MMTV in HeLa cells measured by luciferase activity
Activation of MMTV in HeLa cells measured by luciferase activity
[PMID: 17181172]
HeLa EC50
21 nM
Compound: 2, pred
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
[PMID: 21899328]
HeLa EC50
73.9 nM
Compound: 2, pred
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
[PMID: 21899328]
HeLa EC50
82.7 nM
Compound: 2, pred
Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
[PMID: 21073190]
HepG2 IC50
23 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA
Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA
[PMID: 21115247]
HepG2 EC50
26 nM
Compound: 1
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with PEPCK assessed as GRE activation by luciferase reporter gene assay
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with PEPCK assessed as GRE activation by luciferase reporter gene assay
[PMID: 21324689]
HepG2 IC50
4.1 nM
Compound: 1
Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay
Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay
[PMID: 21349714]
HepG2 IC50
4.1 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-selectin repression by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-selectin repression by luciferase reporter gene assay
[PMID: 21324689]
HepG2 IC50
4.1 nM
Compound: 1
Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone
Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone
[PMID: 21316964]
HepG2 IC50
4.1 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 21115247]
HepG2 EC50
5.3 nM
Compound: 1
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as GRE activation by luciferase reporter gene assay
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as GRE activation by luciferase reporter gene assay
[PMID: 21324689]
HepG2 EC50
5.3 nM
Compound: 1
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay
[PMID: 21115247]
HFF EC50
19 nM
Compound: 1b
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
[PMID: 17181172]
Huh-7 EC50
57.4 nM
Compound: 2, pred
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs
[PMID: 21073190]
Huh-7 EC50
64 nM
Compound: 2, pred
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
[PMID: 21899328]
L1210 ED50
100 μM
Compound: Prednisolone
Cytotoxicity against mouse L1210 cells assessed as growth inhibition measured at 72 hrs by trypan blue exclusion assay
Cytotoxicity against mouse L1210 cells assessed as growth inhibition measured at 72 hrs by trypan blue exclusion assay
[PMID: 118258]
MG-63 EC50
19 nM
Compound: 2, pred
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
[PMID: 21899328]
NHDF IC50
23 nM
Compound: 1
Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA
Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA
[PMID: 21349714]
NHDF IC50
23 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression by ELISA
Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression by ELISA
[PMID: 21324689]
NHDF IC50
23 nM
Compound: 1
Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone
Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone
[PMID: 21316964]
OVCAR-3 IC50
1.1 μM
Compound: 35
Cytotoxicity against human OVCAR-3 cells incubated for 72 hrs by SRB assay
Cytotoxicity against human OVCAR-3 cells incubated for 72 hrs by SRB assay
[PMID: 32283298]
OVCAR-4 IC50
1.1 μM
Compound: 35
Cytotoxicity against human OVCAR-4 cells incubated for 72 hrs by SRB assay
Cytotoxicity against human OVCAR-4 cells incubated for 72 hrs by SRB assay
[PMID: 32283298]
PBMC IC50
13 nM
Compound: Pred
Antiinflammatory activity in Wistar rat PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
Antiinflammatory activity in Wistar rat PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
[PMID: 27810243]
PBMC IC50
45 nM
Compound: Pred
Antiinflammatory activity in human primary PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
Antiinflammatory activity in human primary PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
[PMID: 27810243]
RAW264.7 IC50
25.4 μM
Compound: Prednisolone
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
[PMID: 11000020]
T47D IC50
> 1000 nM
Compound: Prednisolone
Displacement of [3H]progesterone from progesterone receptor in human T47D cells after 20 hrs by scintillation counting method
Displacement of [3H]progesterone from progesterone receptor in human T47D cells after 20 hrs by scintillation counting method
[PMID: 30384041]
U-937 IC50
0.033 μM
Compound: Prednisolone
Antiinflammatory activity in human U937 cells assessed as inhibition of PMA/LPS-stimulated TNFalpha production after 24 hrs by ELISA
Antiinflammatory activity in human U937 cells assessed as inhibition of PMA/LPS-stimulated TNFalpha production after 24 hrs by ELISA
[PMID: 32631542]
U-937 IC50
0.44 μM
Compound: Prednisolone
Inhibition of LPS-induced IL-1beta expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
Inhibition of LPS-induced IL-1beta expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
[PMID: 31883489]
U-937 IC50
0.64 μM
Compound: Prednisolone
Inhibition of LPS-induced TNF-alpha expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
Inhibition of LPS-induced TNF-alpha expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
[PMID: 31883489]
U-937 IC50
8.2 nM
Compound: pred
Antiinflammatory activity in PMA-differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 60 mins prior to LPS challenge measured after 24 hrs
Antiinflammatory activity in PMA-differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 60 mins prior to LPS challenge measured after 24 hrs
[PMID: 24446728]
体外研究
(In Vitro)

Prednisolone(0.002-10 μg/mL;3 天)可抑制人类白细胞有丝分裂[4]

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

体内研究
(In Vivo)

Prednisolone(5 mg/kg/天;口服;每周 6 天,持续 72 周)可显著预防小鼠因肾病死亡[3]

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

Animal Model: NZB/NZW mice, immune nephritis model[3]
Dosage: 5 mg/kg/day
Administration: Oral, 6 days a week for 72 weeks
Result: Significantly lowered mortality rate and prolonged life significantly.
Clinical Trial
分子量

360.44

Formula

C21H28O5

CAS 号
性状

固体

颜色

White to off-white

中文名称

泼尼松龙; 氢化可松EP杂质A

结构分类
初始来源
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 1 year
-20°C 6 months
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 62.5 mg/mL (173.40 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)

H2O 中的溶解度 : 0.1 mg/mL (0.28 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7744 mL 13.8719 mL 27.7439 mL
5 mM 0.5549 mL 2.7744 mL 5.5488 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

动物实验:

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: ≥ 2.08 mg/mL (5.77 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.77 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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。

    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: 99.85%

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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 2.7744 mL 13.8719 mL 27.7439 mL 69.3597 mL
5 mM 0.5549 mL 2.7744 mL 5.5488 mL 13.8719 mL
10 mM 0.2774 mL 1.3872 mL 2.7744 mL 6.9360 mL
15 mM 0.1850 mL 0.9248 mL 1.8496 mL 4.6240 mL
20 mM 0.1387 mL 0.6936 mL 1.3872 mL 3.4680 mL
25 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7744 mL
30 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3120 mL
40 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7340 mL
50 mM 0.0555 mL 0.2774 mL 0.5549 mL 1.3872 mL
60 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8670 mL
100 mM 0.0277 mL 0.1387 mL 0.2774 mL 0.6936 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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  • 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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Prednisolone
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