(8S,10S,13S,14S,17S)-17-(2-(4-(2,6-二(吡咯烷-1-基)嘧啶-4-基)哌嗪-1-基)乙酰基)-10,13-二甲基-6,7,8,10,12,13,14,15,16,17-十氢-3H-环戊[a]菲-3-酮马来酸盐

用途

U-74389G(PNU74389G-melate)是一种抗氧化剂,可以抑制脂质过氧化反应。U-74389G对缺血再灌注损伤具有保护作用,广泛应用于缺血性损伤和高血压动物模型。U-74389G具有抗炎活性[1][2][3]。

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名称

[ 中文名 ]:
(8S,10S,13S,14S,17S)-17-(2-(4-(2,6-二(吡咯烷-1-基)嘧啶-4-基)哌嗪-1-基)乙酰基)-10,13-二甲基-6,7,8,10,12,13,14,15,16,17-十氢-3H-环戊[a]菲-3-酮马来酸盐

[ 英文名 ]:
U 74389G maleate

[英文别名 ]:

MFCD01074991

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 其他

信号通路 >> 其他 >> 其他

[体外研究]

U-74389G(12.5、25和50μM；24小时)抑制内毒素刺激的腹腔巨噬细胞产生亚硝酸盐[3]。细胞活力测定[3]细胞系：腹腔巨噬细胞浓度：12.5、25和50μM培养时间：24小时结果：以剂量依赖性方式降低LPS激发巨噬细胞上清液中的亚硝酸盐浓度。

[体内研究]

U-74389G(静脉注射；10 mg/kg；每日一次；6天)治疗显示出显著的抗炎活性,这与其降低结肠TNF-α、CMDI评分和改善体重变化的能力有关[2]。U-74389G(静脉注射；15或30 mg/kg)治疗可显著预防脂多糖诱导的致死,降低低血压,改善肝功能,降低血浆亚硝酸盐水平,将主动脉环的低反应性恢复到其控制值,并抑制肝脏和主动脉中诱导型NO合酶的活性[3]。动物模型：三硝基苯磺酸诱导的结肠炎大鼠模型[2]剂量：10mg/kg给药：静脉注射；10毫克/千克；每天一次；6d结果：TNF-α、粘膜损伤评分宏观指标(CMDI)降低,体重增加。动物模型：雄性Sprague-Dawley大鼠注射脂多糖[3]剂量：15或30 mg/kg给药：静脉注射；15或30 mg/kg结果：对脂多糖诱导的致命性有保护作用(在最高剂量下,脂多糖注射后24小时存活率为90%,72小时存活率80%)。

[参考文献]

[1]. A M Perna, et al. Protection of rat heart from ischaemia-reperfusion injury by the 21-aminosteroid U-74389G. Pharmacol Res. 1996 Jul-Aug;34(1-2):25-31.

[2]. Georgios Antonios Margonis, et al. Effectiveness of sildenafil and U-74389G in a rat model of colitis. J Surg Res. 2015 Feb;193(2):667-74.

[3]. D Altavilla, et al. The lazaroid, U-74389G, inhibits inducible nitric oxide synthase activity, reverses vascular failure and protects against endotoxin shock. Eur J Pharmacol. 1999 Mar 12;369(1):49-55.

物理化学性质

[ 沸点 ]:
811.6ºC at 760 mmHg

[ 分子式 ]:
C₄₁H₅₄N₆O₆

[ 分子量 ]:
726.904

[ 闪点 ]:
444.6ºC

[ 精确质量 ]:
726.410461

[ PSA ]:
147.48000

[ LogP ]:
5.05700

[ 蒸汽压 ]:
2.12E-26mmHg at 25°C

[ 储存条件 ]:
室温

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

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