特立氟胺

中文名称:

特立氟胺

中文同义词:

特立氟胺;N -(4 - 三氟甲基)- 2 -氰基-3 - 羟基巴豆酰胺;来氟米特EP杂质B;来氟米特杂质1;来氟米特相关化合物B(USP);来氟米特杂质B(EP/BP);A 1726:特立氟胺;特立氟胺杂质

英文名称:

A77 1726

英文同义词:

A77 1726 (Teriflunomide);A 1726;Flucyamide;HMR 1726;(Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide;LeflunoMide EP IMpurity B;Leflunomide Impurity 2(Leflunomide EP Impurity B);A-771726;A 771726;A771726

CAS号:

163451-81-8

分子式:

C12H9F3N2O2

分子量:

270.21

EINECS号:

642-273-4

相关类别:

医药原料;中药对照品;医药原料药;医药中间体;药物杂质及中间体;化学试剂-科研试剂;定制产品;医药原料;Metabolites Impurities;Tyrosine Kinase Inhibitors

Mol文件:

163451-81-8.mol

熔点 

229-232°C

沸点 

410.8±45.0 °C(Predicted)

密度 

1.424±0.06 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

DMSO: soluble5mg/mL, clear (warmed)

酸度系数(pKa)

5.20±0.50(Predicted)

形态

powder

颜色

white to beige

最大波长(λmax)

203nm(MeOH)(lit.)

Merck 

14,9165

InChIKey

UTNUDOFZCWSZMS-YFHOEESVSA-N

生物活性

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。

体外研究

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.

体内研究

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.

用途 

A77 1726 is the active metabolite of Leflunomide, a potent disease-modifying antirheumatic drug used in the treatment of rheumatoid arthritis. LEF-M interferes with dendritic cell function. The second Phase III study evaluating the efficacy of Genzyme鈥檚 teriflunomide therapy against relapsing forms of multiple sclerosis found the once-daily oral drug to be no less effective than聽injectable interfe ron beta 1a (Rebif庐).聽

用途 

一种来氟米特的活性代谢产物，它抑制嘧啶合成，因此有效降低T细胞和B细胞增殖。 Teriflunomide is the active metabolite of leflunomide. Teriflunomide is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase. It is uncertain whether this explains its effect on MS lesions. Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. It has been found that teriflunomide blocks the transcription factor NF-κB.

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3