2. Metabolic Enzyme/Protease
  3. Lactate Dehydrogenase
  4. MEDS433

MEDS433 是人二氢乳清酸脱氢酶 (hDHODH) 的有效抑制剂，IC50 为 1.2 nM。MEDS433 在纳摩尔范围内对 RSV-A 和 RSV-B 发挥有效的抗病毒活性。MEDS433 诱导干扰素刺激基因编码的抗病毒蛋白表达，能够减少 RSV 复制。

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MEDS433

MEDS433 Chemical Structure

CAS No. : 2241027-61-0

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规格 价格 是否有货 数量
1 mg ￥4900
In-stock
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Customer Review

MEDS433 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Jurkat IC50
0.75 μM
Compound: 4
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
Jurkat IC50
68.69 μM
Compound: 4
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
PBMC IC50
0.78 μM
Compound: 4
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
PBMC IC50
57.15 μM
Compound: 4
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay
[PMID: 29939742]
THP-1 EC50
0.0397 μM
Compound: 1
Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis
[PMID: 33844533]
THP-1 EC50
0.0723 μM
Compound: 1
Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry
[PMID: 33844533]
THP-1 EC50
40 nM
Compound: MEDS433
Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis
Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis
[PMID: 36162075]
THP-1 EC50
72 nM
Compound: MEDS433
Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
[PMID: 36162075]
U-937 EC50
0.026 μM
Compound: 1
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
[PMID: 33844533]
U-937 EC50
0.0404 μM
Compound: 1
Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry
Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry
[PMID: 33844533]
U-937 EC50
26 nM
Compound: MEDS433
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
[PMID: 36162075]
U-937 EC50
40 nM
Compound: MEDS433
Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis
[PMID: 36162075]
分子量

401.31

Formula

C20H11F4N3O2
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
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (249.18 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 2.4918 mL 12.4592 mL 24.9184 mL
5 mM 0.4984 mL 2.4918 mL 4.9837 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

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.23 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，此方案实验周期在半个月以上的动物实验酌情使用。

    以 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

只
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
参考文献

MEDS433 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 2.4918 mL 12.4592 mL 24.9184 mL 62.2960 mL
5 mM 0.4984 mL 2.4918 mL 4.9837 mL 12.4592 mL
10 mM 0.2492 mL 1.2459 mL 2.4918 mL 6.2296 mL
15 mM 0.1661 mL 0.8306 mL 1.6612 mL 4.1531 mL
20 mM 0.1246 mL 0.6230 mL 1.2459 mL 3.1148 mL
25 mM 0.0997 mL 0.4984 mL 0.9967 mL 2.4918 mL
30 mM 0.0831 mL 0.4153 mL 0.8306 mL 2.0765 mL
40 mM 0.0623 mL 0.3115 mL 0.6230 mL 1.5574 mL
50 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2459 mL
60 mM 0.0415 mL 0.2077 mL 0.4153 mL 1.0383 mL
80 mM 0.0311 mL 0.1557 mL 0.3115 mL 0.7787 mL
100 mM 0.0249 mL 0.1246 mL 0.2492 mL 0.6230 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.

Keywords:

MEDS4332241027-61-0MEDS 433MEDS-433Lactate DehydrogenaseLDHdihydroorotate dehydrogenasehDHODHantiviralRSV-ARSV-BInterferon Stimulated GenesRSV replicationInhibitorinhibitorinhibit

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产品名称：
MEDS433
目录号：
HY-156442
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