计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
Leflunomide是免疫抑制剂，其活性代谢产物为A77 1726(RS-61980)。An inhibitor of Cox-2 and tyrosine kinase.
Information
Leflunomide (HWA486) Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibit
In vitro
Leflunomide is actually a prodrug that is processed in vivo to the active metabolite A771726，which has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays. Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2. Leflunomide is an immunomodulatory drug that may exert its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of the pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide prevents the expansion of activated and autoimmune lymphocytes by interfering with the cell cycle progression due to inadequate production of rUMP and utilizing mechanisms involving p53.
In vivo
Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
RS-34821, SU101, Arava | 5-methyl-N-(4-(trifluoromethyl)phenyl)isoxazole-4-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Leflunomide (HWA486)
生化机理
来氟米特（HWA486、RS-34821、SU101、Arava）是一种嘧啶合成和蛋白酪氨酸激酶抑制剂，属于 DMARD，用作免疫抑制剂。来氟米特的活性代谢产物是 A77 1726，它能抑制二氢烟酸脱氢酶（DHODH）。来氟米特还是一种 AhR 激动剂。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
二氢烟酸脱氢酶抑制剂
名称和识别符
EC号
616-254-6
分子类型
小分子
Isomeric SMILES
CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F
分子量
270.21
Reaxy-Rn
4323174
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4323174&ln=
高级数据
产品属性
| ALogP | 2.5 |
|---|
关联靶点（人）
CYP1A2
Tchem
细胞色素 P450 1A2(Cytochrome P450 1A2)
(2 活性数据)
DHODH
Tclin
二氢乳清酸脱氢酶（醌），线粒体(Dihydroorotate dehydrogenase (quinone), mitochondrial)
(2 活性数据)
化学和物理性质
熔点
166.5°C
安全和危险性（GHS）
信号词
危险
危险声明
H301: 吞咽会中毒
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
WGK Germany
3
RTECS
NY2354200
Merck Index
5432
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）