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A-771726 (Synonyms: 特立氟胺; A77 1726)
目录号: PC12796 纯度: ≥98%
CAS No. :163451-81-8
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中文名称
A-771726
中文别名
N -(4 - 三氟甲基)- 2 -氰基-3 - 羟基巴豆酰胺;[ 13C6 ] - 特立氟胺标准品;Teriflunomide 特立氟胺;阿特拉通;来氟米特杂质B(EP) 标准品;特立氟胺;(2Z)-2-氰基-3-羟基-N-[4-(三氟甲基)苯基]丁-2-烯酰胺;(Z)-2-氰基-3-羟基-N-(4-(三氟甲基)苯基)丁-2-烯酰胺;1-环丙基-7-(3-甲氨基-1-哌啶基)-8-甲氧基-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸;巴洛沙星二水合物;来氟米特代谢物(特立氟胺,来氟米特杂质B);N-[4-(三氟甲基)苯基]-2-氰基-3-羟基丁烯酰胺;(Z)-2-氰基-3-羟基-N-[4-(三氟甲基)苯基]-2-丁烯酰胺;来氟米特杂质1;来氟米特EP杂质B
英文名称
A-771726
英文别名
(Z)-2-Cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)but-2-enamide;Teriflunomide;A77 1726;A-771726;Flucyamide;(2Z)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide;A 77-1726;Aubagio;(Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide;A 1726;HMR 1726;N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide;SU 20;N-[4-(Trifluoromethyl)phenyl]-2-cyano-3-hydroxycrotonamide;A77 1726 (Teriflunomide);LeflunoMide EP IMpurity B;HMR1726;A 771726;teriflunomida;teriflunomidum;RS 61980;A771726;2-Cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)-2-butenamide;(Z)-2-cyano-alpha,alpha,alpha-trifluoro-3-hydroxy-p-crotonotoluidide;1C058IKG3B;N-(4-Trifluoromethylphenyl)-2-cyano-2-hydroxycrotonamide;(Z)-2-cyano-3-hydroxy-N-[4-(trifluoro
Cas No.
163451-81-8
分子式
C12H9F3N2O2
分子量
270.21
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.

性状

Solid

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.

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

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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 33.33 mg/mL (123.35 mM; Need ultrasonic)

配制储备溶液
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
10 mM 0.3701 mL 1.8504 mL 3.7008 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.25 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.25 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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