拉氟莫司

生物活性体外研究体内研究拉氟莫司试剂级价格

拉氟莫司

CAS号:147076-36-6
英文名:Laflunimus
中文名:拉氟莫司
CBNumber:CB21118133
分子式:C15H13F3N2O2
分子量:310.274
MOL File:147076-36-6.mol

拉氟莫司化学性质

储存条件 :Store at -20°C
溶解度 :Soluble in DMSO
形态 :Solid
颜色 :Yellow to khaki

拉氟莫司性质、用途与生产工艺

生物活性 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。
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 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).

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 ID ₅₀ 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.