2. Metabolic Enzyme/Protease
  3. Drug Metabolite
  4. Teriflunomide

Teriflunomide  (Synonyms: 特立氟胺; A77 1726)

目录号: HY-15405 纯度: 99.94%
COA 产品使用指南

摩尔计算器

Teriflunomide (A77 1726) 是来氟米特的活性代谢产物，可用于类风湿性关节炎的研究。 它抑制嘧啶合成，因此有效降低T细胞和B细胞增殖。

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Teriflunomide Chemical Structure

Teriflunomide Chemical Structure

CAS No. : 163451-81-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥500
In-stock
1 mg ￥109
In-stock
5 mg ￥218
In-stock
10 mg ￥350
In-stock
50 mg ￥700
In-stock
100 mg ￥980
In-stock
500 mg ￥2950
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Teriflunomide:

Teriflunomide 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

Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Jurkat IC50
26.65 μM
Compound: 2, A-771726
Cytotoxicity against human Jurkat cells after 4 days by MTT assay
Cytotoxicity against human Jurkat cells after 4 days by MTT assay
[PMID: 22984987]
Jurkat IC50
43.22 μM
Compound: Teriflunomide
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
43.22 μM
Compound: A771726
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method
[PMID: 28235702]
Jurkat IC50
60 μM
Compound: 25
Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay
Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay
[PMID: 26079043]
MDA-MB-231 IC50
14 μM
Compound: Teriflunomide
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
[PMID: 34516133]
MDA-MB-468 IC50
> 20 μM
Compound: Teriflunomide
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
[PMID: 34516133]
PBMC IC50
46 μM
Compound: 3
Antiproliferative activity against PHA-stimulated human PBMC assessed as inhibition of [3H]-thymidine incorporation after 72 hrs by BrdU-ELISA assay
Antiproliferative activity against PHA-stimulated human PBMC assessed as inhibition of [3H]-thymidine incorporation after 72 hrs by BrdU-ELISA assay
[PMID: 22078215]
PBMC IC50
54.3 μM
Compound: A771726
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 BrdU incorporation 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 BrdU incorporation assay
[PMID: 28235702]
Splenocyte IC50
6.7 μM
Compound: A-771726
Inhibition of Concanavalin A-stimulated cell proliferation in mouse splenocytes after 48 hrs by MTT assay
Inhibition of Concanavalin A-stimulated cell proliferation in mouse splenocytes after 48 hrs by MTT assay
[PMID: 11000020]
T-cell IC50
48.03 μM
Compound: 2, A-771726
Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay
Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay
[PMID: 22984987]
体外研究
(In Vitro)

Teriflunomide primarily acts as an inhibitor of dihydroorotate dehydrogenase (DHODH), a key mitochondrial enzyme involved in the de novo synthesis of pyrimidines in rapidly proliferating cells. By reducing the activity of high-avidity proliferating T lymphocytes and B lymphocytes, teriflunomide likely attenuates the inflammatory response to autoantigens in MS. Thus, teriflunomide can be considered a cytostatic rather than a cytotoxic drug to leukocytes[1].

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

Teriflunomide 相关抗体:
体内研究
(In Vivo)

Teriflunomide has demonstrated beneficial effects in two independent animal models of demyelinating disease. In the dark agouti rat model of experimental autoimmune encephalitis (EAE), teriflunomide administration results in clinical, histopathological, and electrophysiological evidence of efficacy both as a prophylactic and therapeutic agent. Similarly, in the female Lewis rat model of EAE, teriflunomide administration results in beneficial prophylactic and therapeutic clinical effects, with a delay in disease onset and symptom severity[1].

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

270.21

Formula

C12H9F3N2O2
CAS 号
性状

固体

颜色

White to off-white

中文名称

(Z)-2-氰基-3-羟基-N-(4-(三氟甲基)苯基)丁-2-烯酰胺
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 : 33.33 mg/mL (123.35 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 3.7008 mL 18.5041 mL 37.0083 mL
5 mM 0.7402 mL 3.7008 mL 7.4017 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.25 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。

    以 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.25 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

纯度: 99.94%

COA (284 KB) RP-HPLC (243 KB)

产品使用指南 (1538 KB)
参考文献

Teriflunomide 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 3.7008 mL 18.5041 mL 37.0083 mL 92.5206 mL
5 mM 0.7402 mL 3.7008 mL 7.4017 mL 18.5041 mL
10 mM 0.3701 mL 1.8504 mL 3.7008 mL 9.2521 mL
15 mM 0.2467 mL 1.2336 mL 2.4672 mL 6.1680 mL
20 mM 0.1850 mL 0.9252 mL 1.8504 mL 4.6260 mL
25 mM 0.1480 mL 0.7402 mL 1.4803 mL 3.7008 mL
30 mM 0.1234 mL 0.6168 mL 1.2336 mL 3.0840 mL
40 mM 0.0925 mL 0.4626 mL 0.9252 mL 2.3130 mL
50 mM 0.0740 mL 0.3701 mL 0.7402 mL 1.8504 mL
60 mM 0.0617 mL 0.3084 mL 0.6168 mL 1.5420 mL
80 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1565 mL
100 mM 0.0370 mL 0.1850 mL 0.3701 mL 0.9252 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:

Teriflunomide163451-81-8A77 1726(Z)-2-氰基-3-羟基-N-(4-(三氟甲基)苯基)丁-2-烯酰胺Drug MetaboliteInhibitorinhibitorinhibit

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