Laflunimus

拉氟尼莫司

Laflunimus

L646152-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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 IC 50 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. In Vitro Ig secretion from mouse splenocytes was induced by lipopolysaccharide (LPS) for 5 days. Laflunimus inhibited the secretion of IgM and IgG with IC 50 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 (IC 50 = 415 and 4400 nM, respectively) and on isolated ovine PGHS-1 (IC 50 =64 and 742 µM) and PGHS-2 (IC 50 =100 and 2766 µM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 ID 50 values of 38 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid

Laflunimus（HR325）是一种免疫抑制剂，也是来氟米特活性代谢物 A77 1726 的类似物。Laflunimus 是一种口服活性的二氢烟酸脱氢酶（DHODH）抑制剂。Laflunimus 可抑制免疫球蛋白（Ig）分泌，其 IC

147076-36-6

C15H13F3N2O2

310.27 g/mol

O=C(NC1=CC=C(C(F)(F)F)C(C)=C1)/C(C#N)=C(C2CC2)\\O

DMSO : 50 mg/mL (161.15 mM; Need ultrasonic)