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

Teriflunomide  (Synonyms: 特立氟胺; A77 1726)

目錄號: HY-15405 純度: 99.94%
COA 產(chǎn)品使用指南

Teriflunomide (A77 1726) 是來氟米特的活性代謝產(chǎn)物,可用于類風(fēng)濕性關(guān)節(jié)炎的研究。 它抑制嘧啶合成,因此有效降低T細胞和B細胞增殖。

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Teriflunomide Chemical Structure

Teriflunomide Chemical Structure

CAS No. : 163451-81-8

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥324
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1 mg ¥109
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5 mg ¥218
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10 mg ¥350
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25 mg ¥500
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50 mg ¥700
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100 mg ¥980
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500 mg ¥2450
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Customer Review

Other Forms of Teriflunomide:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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.

細胞效力
(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]
體外研究
(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.

體內(nèi)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 號
性狀

固體

顏色

White to off-white

中文名稱

(Z)-2-氰基-3-羥基-N-(4-(三氟甲基)苯基)丁-2-烯酰胺

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 33.33 mg/mL (123.35 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.25 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.25 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.94%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱:
Teriflunomide
目錄號:
HY-15405
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