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Candoxatril

Names

[ CAS No. ]:
123122-55-4

[ Name ]:
Candoxatril

[Synonym ]:
4-[[1-[(2S)-3-(2,3-dihydro-1H-inden-5-yloxy)-2-(2-methoxyethoxymethyl)-3-oxopropyl]cyclopentanecarbonyl]amino]cyclohexane-1-carboxylic acid
Candoxatril

Biological Activity

[Description]:

Candoxatril is a neutral endopeptidase (NEP) inhibitor.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin
Research Areas >> Metabolic Disease

[Target]

NEP[1].


[In Vivo]

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].

[Animal admin]

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].

[References]

[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.


[Related Small Molecules]

Sacubitril/valsartan (LCZ696) | AHU 377 | Sacubitrilat | Phosphoramidon disodium salt | Racecadotril | NEP-In-1 | NEP-IN-2 | SQ28603

Chemical & Physical Properties

[ Density]:
1.21g/cm3

[ Boiling Point ]:
718.4ºC at 760mmHg

[ Molecular Formula ]:
C29H41NO7

[ Molecular Weight ]:
515.63800

[ Flash Point ]:
388.3ºC

[ Exact Mass ]:
515.28800

[ PSA ]:
114.65000

[ LogP ]:
4.91030

Safety Information

[ Hazard Codes ]:
Xi


Related Compounds