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147076-36-6

中文名稱 拉氟莫司
英文名稱 Laflunimus
CAS 147076-36-6
分子式 C15H13F3N2O2
分子量 310.27
MOL 文件 147076-36-6.mol
147076-36-6 結構式 147076-36-6 結構式

基本信息

中文別名
拉氟莫司
英文別名
Laflunimus
LCBOKWGFIPORJD-QBFSEMIESA-N
2-Propenamide, 2-cyano-3-cyclopropyl-3-hydroxy-N-[3-methyl-4-(trifluoromethyl)phenyl]-, (2Z)-

物理化學性質

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色Yellow to khaki

常見問題列表

生物活性
Laflunimus (HR325) 是一種免疫抑制劑和 Leflunomide 活性代謝物 A771726 的類似物。Laflunimus 是一種口服的二氫硼酸脫氫酶 (DHODH) 抑制劑。Laflunimus 抑制免疫球蛋白 (Ig) 分泌,抑制 Ig M 和 IgG 分泌的 IC50 值分別為 2.5 和 2 μM。Laflunimus 也是前列腺素內過氧化物合酶 (PGHS) -1 和 -2 抑制劑。
體外研究

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).

體內研究

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.
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