49697-38-3

• 常用中文名：瑞美松龙
• 常用英文名：Rimexolone
• CAS号：49697-38-3
• 分子式：C₂₄H₃₄O₃
• 分子量：370.525
• 相关类别： 研究领域 炎症/免疫
• 发布时间：2018-09-14 18:03:01
• 更新时间：2024-01-10 12:06:47
• 利美索酮(Org 6216)是一种具有抗炎活性的糖皮质激素类固醇。利美索酮可用作1%眼用混悬液,用于治疗眼部炎症[1][2]。

名称

• 中文名: 瑞美松龙
• 英文名: Rimexolone
• 英文别名: Rimexolone; (11β,16α,17β)-11-Hydroxy-16,17-dimethyl-17-(1-oxopropyl)androsta-1,4-dien-3-one; 11β-Hydroxy-16α,17α-dimethyl-17-propionylandrosta-1,4-dien-3-one; 11b-Hydroxy-16a,17a-dimethyl-17-propionylandrosta-1,4-dien-3-one; (8S,9S,10R,11S,13S,14S,16R,17S)-11-Hydroxy-10,13,16,17-tetramethyl-17-propionyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one; (8S,9S,10R,11S,13S,14S,16R,17S)-11-Hydroxy-10,13,16,17-tetramethyl-17-propanoyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-on; (8S,9S,10R,11S,13S,14S,16R,17S)-11-hydroxy-10,13,16,17-tetramethyl-17-propanoyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one; (11b,16a,17b)-11-Hydroxy-16,17-dimethyl-17-(1-oxopropyl)androsta-1,4-dien-3-one; Asoprisnil ecamate; Androsta-1,4-dien-3-one, 11-hydroxy-16,17-dimethyl-17-(1-oxopropyl)-, (11β,16α,17β)-; (8S,9S,10R,11S,13S,14S,16R,17S)-11-hydroxy-10,13,16,17-tétraméthyl-17-propanoyl-6,7,8,9,10,11,12,13,14,15,16,17-dodécahydro-3H-cyclopenta[a]phénanthrén-3-one; 11β-Hydroxy-16α,17,21-trimethyl-1,4-pregnadien-3,20-dion; (8S,9S,10R,11S,13S,14S,16R,17S)-11-hydroxy-10,13,16,17-tetramethyl-17-propanoyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one (non-preferred name); (8S,9S,10R,13S,14S,16R,17S)-11-Hydroxy-10,13,16,17-tetramethyl-17-propionyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one (non-preferred name); VEXOL

物化性质

• 密度: 1.1±0.1 g/cm3
• 沸点: 507.0±50.0 °C at 760 mmHg
• 熔点: 258-268ºC
• 分子式: C₂₄H₃₄O₃
• 分子量: 370.525
• 闪点: 274.5±26.6 °C
• 精确质量: 370.250793
• PSA: 54.37000
• LogP: 4.01
• 蒸汽压: 0.0±3.0 mmHg at 25°C
• 折射率: 1.559
• 储存条件: 室温

生物活性

• 描述: 利美索酮(Org 6216)是一种具有抗炎活性的糖皮质激素类固醇。利美索酮可用作1%眼用混悬液,用于治疗眼部炎症[1][2]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 炎症/免疫
• 体外研究: 利美索酮(Org 6216)在注射部位显示出高度增强的持久性,最小的系统效应,几乎不会诱发皮肤营养不良[1]。
• 体内研究: 利美索酮(Org 6216)(0-450μg/只小鼠；关节内注射；一次)在单关节抗原诱导的关节炎小鼠中显示出延长的抗炎作用[1]。动物模型：雄性,8-12周龄C57Black/6小鼠,具有抗原诱导的关节炎[1]剂量：5、25、50、150、250、450μg/小鼠给药：关节内注射,一次结果：以剂量依赖性方式抑制关节炎。在450和150μ。导致软骨细胞蛋白多糖合成的抑制减少。
• 参考文献:

  [1]. Joosten LA, et al. Protective effect of rimexolone on cartilage damage in arthritic mice: a comparative study with triamcinolone hexacetonide. Agents Actions. 1990 Aug;31(1-2):135-42.

  [2]. Foster CS, et al. Efficacy and safety of rimexolone 1% ophthalmic suspension vs 1% prednisolone acetate in the treatment of uveitis. Am J Ophthalmol. 1996 Aug;122(2):171-82.

合成路线

220983-31-3 ~97% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

50-24-8 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

49757-06-4 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

110558-70-8 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

20423-99-8 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

60124-50-7 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

60124-51-8 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

207346-24-5 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044

226712-41-0 ~% 49697-38-3

文献：Conrow, Raymond E. Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 1042 - 1044