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  • Candoxatril (UK 79300)
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Candoxatril (UK 79300)

Candoxatril (UK 79300) 是一种中性肽链内切酶 (NEP) 抑制剂。

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  • 货号: ajcx12626
  • CAS: 123122-55-4
  • 别名: 坎沙曲,UK 79300
  • 分子式: C29H41NO7
  • 分子量: 515.64
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

Candoxatril is a neutral endopeptidase (NEP) inhibitor.


While the NEP inhibitors have no significant effect on body weight, food and water intake, mean blood pressure or creatinine levels, they do increase cGMP levels in the urine and affected hematopoiesis in an anti-inflammatory way. Moreover, a-SMA deposition in the kidney cortex is inversely correlated with cGMP elevation suggesting a NEP dependent antifibroti effect. High quality mRNA profiles are obtained with at least 8 independent samples per treatment group. The data confirms the cGMP dependent anti-fibrotic action of Sol-1 and further supports the potential therapeutic actions of this neutral endopeptidase inhibitor[2].


[1]. Bevan EG, et al. Candoxatril, a neutral endopeptidase inhibitor: efficacy and tolerability in essential hypertension. J Hypertens. 1992 Jul;10(7):607-13. [2]. M Aleksinskaya, et al. Neutral endopeptidase inhibitors SOL-1 and candoxatril counteract kidney fibrosis by reducing myofibroblast formation in mouse UUO model. Bmc Pharmacology & Toxicology , 2013 , 14 (1) :1-2.

Protocol

Animal experiment:

Mice[2]Mice (n=10 per group) subjected to UUO are treated for 1 week with either Solvent, SOL-1 (NEP-/ECE-inhibitor two doses), Candoxatril (reference NEP inhibitor) or losartan (angiotensin AT1-receptor antagonist) and compared to sham operated animals[2].

参考文献:

[1]. Bevan EG, et al. Candoxatril, a neutral endopeptidase inhibitor: efficacy and tolerability in essential hypertension. J Hypertens. 1992 Jul;10(7):607-13.
[2]. M Aleksinskaya, et al. Neutral endopeptidase inhibitors SOL-1 and candoxatril counteract kidney fibrosis by reducing myofibroblast formation in mouse UUO model. Bmc Pharmacology & Toxicology , 2013 , 14 (1) :1-2.

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