产品
编 号:F170991
分子式:C15H13F3N2O2
分子量:310.27
产品类型
结构图
CAS No: 147076-36-6
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产品详情
生物活性:
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.
体内研究:
HR325 (50 mg/kg; p.o.; days 14-18 after being injected with SRBC) inhibits the secondary anti-sheep red blood cell (SRBC) antibody response with ID50 values of 38 mg/kg.Animal Model:Male CD-1 mice (20-24 g)
Dosage:50 mg/kg
Administration:Oral; days 14-18 after being injected with SRBC
Result:The level of circulating anti-SRBC IgG in this model was inhibited dose relatedly by orally administered HR325.
体外研究:
Ig secretion from mouse splenocytes was induced by lipopolysaccharide (LPS) for 5 days. Laflunimus inhibited the secretion of IgM and IgG with IC50 values of 2.5 and 2 μM , respectively. Adding Uridine (50 μ M) increased these values to 70 and 60 μ M, respectively. Laflunimus inhibits LPS-induced kappa light-chain cell surface expression on 70Z/3 cells, a property also reversed by uridine.Laflunimus (HR325) is more potent than A77 1726 as an inhibitor of PGHS in guinea pig polymorphonuclear leukocytes (IC50= 415 and 4400 nM, respectively) and on isolated ovine PGHS-1 (IC50=64 and 742 μM) and PGHS-2 (IC50=100 and 2766 μM).