13209-41-1

• 常用中文名：Vamorolone
• 常用英文名：Vamorolone
• CAS号：13209-41-1
• 分子式：C₂₂H₂₈O₄
• 分子量：356.45500
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 糖皮质激素受体
• 发布时间：2017-07-01 10:58:18
• 更新时间：2026-07-15 11:35:22
• Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。

名称

• 中文名: 16α-甲基-9,11-脱氢泼尼松龙
• 英文名: 16α-Methyl-9,11-dehydro Prednisolone
• 中文别名: 地塞米松杂质E; 地塞米松杂质杂质E; 妥布霉素地塞米松杂质C; 糠酸莫米松杂质22; (8S,10S,13S,14S,16R,17R)-17-羟基-17-(2-羟基乙酰基)-10,13,16-三甲基-6,7,8,10,12,13,14,15,16,17-十氢-3H-环戊并[A]菲-3-酮; 地塞米松杂质5(地塞米松杂质E); 艾美龙; 地塞米松杂质E,10 MM DMSO 溶液; (16Α)-17,21-二羟基-16-甲基预浸基-1,4,9-三烯-3,20-二酮; 地塞米松磷酸钠杂质F; 地塞米松磷酸钠杂质E; 16Α-甲基-9,11-脱氢泼尼松龙; 瓦莫洛龙
• 英文别名: 16Alpha-Methyl-9,11-dehydro Prednisolone; (16α)-17,21-Dihydroxy-16-Methylpregna-1,4,9-triene-3,20-dione; Dexamethasone Imp E; Cbamazine Impurity 22; 17, 21-dihydroxy-16α-methylpregna- 1, 4, 9-triene-3,20-dione; inhibit,rair,Mineralocorticoid Rector,VBP 15,Glucocorticoid Rector,NF-κB,inflammation,Duchenne,Inhibitor,membrane,dystrophy,Vamorolone,Nuclefactor-κB,Nuclefactor-kappaB,muscul,VBP-15,glucocorticoid; 17,21-dihydroxy-16alpha-methylpregna-1,4,9-triene-3,20-dione; Pregna-1,4,9-triene-3,20-dione, 17,21-dihydroxy-16-methyl-, (16α); (16alpha)-17,21-dihydroxy-16-methylpregna-1,4,9-triene-3,20-dione; Dexamethasone Impurity 5(Dexamethasone Impurity E); Dexamethasone impurity E; (8S,10S,13S,14S,16R,17R)-17-hydroxy; Tobramycin and dexamethasone impurity C; ((2R,3R,4aS,4bS,10aS,10bR,11S,12aS)-10b-fluoro-2,11-dihydroxy-3,10a,12a-trimethyl-1,8-dioxo-1,2,3,4,4a,4b,5,6,8,10a,10b,11,12,12a-tetradecahydrochrysen-2-yl)methyl dihydrogen phosphate; VBP15; (8S,10S,13S,14S,16R,17R)-17-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,10,12,13,14,15,16,17-decahydro-3H-cyclopenta[a]phenanthren-3-one; (8S,10S,13S,14S,16R,17R)-17-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-7,8,12,14,15,16-hexahydro-6H-cyclopenta[a]phenanthren-3-one; Vamorolone, 10 mM in DMSO; 16a-Methyl-9,11-dehydro prednisolone - Bio-X; Dexamethasone Impurity L; ethyl (8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-cboxylate; 17.alpha.,21-Dihydroxy-16.alpha.-methylpregna-1,4,9-triene-3,20-dione

物化性质

• 密度: 1.24g/cm3
• 沸点: 548.3ºC at 760 mmHg
• 分子式: C₂₂H₂₈O₄
• 分子量: 356.45500
• 闪点: 299.4ºC
• 精确质量: 356.19900
• PSA: 74.60000
• LogP: 2.75290
• 外观性状: 固体
• 蒸汽压: 2.63E-14mmHg at 25°C
• 折射率: 1.603
• 储存条件: 2-8°C，密封，干燥

生物活性

• 描述: Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 盐皮质激素受体
  研究领域 >> 炎症/免疫
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体
• 体外研究: Vamorolone(VBP15)抑制肿瘤坏死因子α(TNFα)诱导的C2C12肌肉细胞在1nm及以上的促炎性NF-κB信号传导。Vamorolone以相似的亲和力结合糖皮质激素受体(GR)和盐皮质激素受体(MR)。Vamorolone(0.1,1μM；30分钟)可减少人巨噬细胞IL1β和CCL5炎症介质的产生[2]。Vamorolone是第一类盐皮质激素受体(MR)拮抗剂/游离糖皮质激素受体(GR)配体[3]。
• 体内研究: 与mdx小鼠的药理性糖皮质激素相比,Vamorolone(5-30 mg/kg；樱桃糖浆)显示出更好的副作用[1]。Vamorolone(30mg/kg；口服；每日20天)可减轻小鼠实验性自身免疫性脑脊髓炎的中枢神经系统炎症[2]。动物模型：C57BL/6小鼠(实验性自身免疫性脑脊髓炎)[2]剂量：30mg/kg,口服；每日20天(从MOG 33-55肽免疫前1天开始,持续)结果：小鼠实验性自身免疫性脑脊髓炎中枢神经系统炎症减轻。
• 参考文献:

  [1]. Heier CR, et al. VBP15, a novel anti-inflammatory and membrane-stabilizer, improves muscular dystrophy without side effects. EMBO Mol Med. 2013 Oct;5(10):1569-85.

  [2]. Dillingham BC, et al. VBP15, a novel anti-inflammatory, is effective at reducing the severity of murine experimental autoimmune encephalomyelitis. Cell Mol Neurobiol. 2015 Apr;35(3):377-387.

  [3]. Heier CR, et al. Vamorolone targets dual nuclear receptors to treat inflammation and dystrophic cardiomyopathy. Life Sci Alliance. 2019 Feb 11;2(1). pii: e201800186.

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