Vamorolone 是一种首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。它抑制 (NF-Κb) 抑制作用,并降低了激素的影响。它改善肌营养不良,无副作用。
产品描述
Vamorolone is an orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone displays effective NF-κB inhibition and substantially decreases hormonal effects.
体外活性
Vamorolone is a first-in-class mineralocorticoid receptor antagonist/dissociative glucocorticoid receptor ligand. Vamorolone inhibits TNFα-induced pro-inflammatory NF-κB signaling in C2C12 muscle cells at 1 nM or more. Vamorolone binds the glucocorticoid receptor and mineralocorticoid receptor. Vamorolone (0.1, 1μM; 30 minutes) decreases the production of IL1βand CCL5 inflammatory mediators in primary human macrophages [1][2][3].
体内活性
Vamorolone (30 mg/kg; p.o.; daily for 20 days) decreases CNS Inflammation in murine experimental autoimmune encephalomyelitis. Vamorolone (5-30 mg/kg; cherry syrup) displays a superior side effect profile compared to pharmacological glucocorticoids in mdx mice [1][2].
Cas No.
13209-41-1
分子式
C22H28O4
分子量
356.46
别名
地塞米松EP杂质E;VBP15
储存和溶解度
DMSO:62.5 mg/mL (175.34 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years