| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L408176-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 二氢烟酸脱氢酶抑制剂 |
| 产品介绍 |
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 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 lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 2.156 |
|---|---|
| hba_count | 3 |
| HBD Count | 1 |
| Rotatable Bond | 3 |
| 分子类型 | 小分子 |
|---|---|
| Canonical 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= |
| DMSO(mg / mL) Max Solubility | 54 |
|---|---|
| DMSO(mM) Max Solubility | 199.84 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 4323174 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4323174&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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