CAS NO: | 163451-81-8 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 163451-81-8 |
别名 | 特立氟胺; A77 1726 |
化学名 | 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2Z-butenamide |
Canonical SMILES | O=C(/C(C#N)=C(O)/C)NC1=CC=C(C(F)(F)F)C=C1 |
分子式 | C12H9F3N2O2 |
分子量 | 270.2 |
溶解度 | ≤10.7mg/ml in DMSO;21.6mg/ml in dimethyl formamide |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | A771726 is dihydroorotate dehydrogenase inhibitor. The dihydroorotate dehydrogenase (DHODH) is a mitochondrial protein. Inhibitors of DHODH can be used to treat autoimmune diseases such as rheumatoid arthritis. A771726, leflunomide's active metabolite, showed significantly inhibitory effect on TNF-α and IL-1 at protein and transcription levels, and reduced production of IL-1 in monocultures of Kupffer cells (KCs) [1]. A-771726 reversibly inhibited dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. A-771726 prevented activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis with the IC50 values of 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively [2]. A-771726 inhibited the activity of tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle at higher doses [2]. A-771726 also inhibited the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α with the IC50 values of 7 and 3 μM, respectively. A771726 also inhibited MMP-1 and IL-6 production at concentrations >10 μM [3]. A771726 is a novel immunosuppressive compound that has been shown to be a powerful antiproliferative agent for mononuclear and T-cells. A771726 potently inhibited the activity of DHODase with the Ki of 179 ± 19 nM. A771726 was a competitive inhibitor of the ubiquinone binding site [4]. References: |