拉氟莫司
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- CAS号:
- 147076-36-6
- 英文名:
- Laflunimus
- 英文别名:
- Laflunimus;LCBOKWGFIPORJD-QBFSEMIESA-N;2-Propenamide, 2-cyano-3-cyclopropyl-3-hydroxy-N-[3-methyl-4-(trifluoromethyl)phenyl]-, (2Z)-
- 中文名:
- 拉氟莫司
- 中文别名:
- 拉氟莫司;化合物 T11813;13C3,15N]-拉氟尼司
- CBNumber:
- CB21118133
- 分子式:
- C15H13F3N2O2
- 分子量:
- 310.274
- MOL File:
- 147076-36-6.mol
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拉氟莫司化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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拉氟莫司性质、用途与生产工艺
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。
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).
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.
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Animal Model:
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Male CD-1 mice (20-24 g)
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Dosage:
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50 mg/kg
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Administration:
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Oral; days 14-18 after being injected with SRBC
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Result:
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The level of circulating anti-SRBC IgG in this model was inhibited dose relatedly by orally administered HR325.
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拉氟莫司
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-101813 | Laflunimus | | 1 mg | 1363元 |
| 2024/04/30 | HY-101813 | 拉氟莫司
Laflunimus | 147076-36-6 | 5mg | 3000元 |
147076-36-6, 拉氟莫司 相关搜索:
- 13C3,15N]-拉氟尼司
- 化合物 T11813
- 拉氟莫司
- 147076-36-6
- 2-Propenamide, 2-cyano-3-cyclopropyl-3-hydroxy-N-[3-methyl-4-(trifluoromethyl)phenyl]-, (2Z)-
- LCBOKWGFIPORJD-QBFSEMIESA-N
- Laflunimus