Laflunimus (HR325) 是一种免疫抑制剂和 Leflunomide 活性代谢物 A771726 的类似物。Laflunimus 是一种口服的二氢硼酸脱氢酶 (DHODH) 抑制剂。Laflunimus 抑制免疫球蛋白 (Ig) 分泌，抑制 Ig M 和 IgG 分泌的 IC50 值分别为 2.5 和 2 μM。Laflunimus 也是前列腺素内过氧化物合酶 (PGHS) -1 和 -2 抑制剂。
| Cas No. | 147076-36-6 |
| 别名 | 拉氟莫司,HR325 |
| Canonical SMILES | O=C(NC1=CC=C(C(F)(F)F)C(C)=C1)/C(C#N)=C(C2CC2)\O |
| 分子式 | C15H13F3N2O2 |
| 分子量 | 310.27 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| 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 | Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor[1][2]. [1]. Thomson TA, et al. In vitro and in Vivo inhibition of immunoglobulin secretion by the immunosuppressive compound HR325 is reversed by exogenous uridine. Scand J Immunol. 2002 Jul;56(1):35-42.
[2]. Curnock AP, et al. Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti-inflammatory drugs. J Pharmacol Exp Ther. 1997 Jul;282(1):339-47. |
