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Ataciguat

  Cat. No.:  DC21121   Featured
Chemical Structure
254877-67-3
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More than 5000 active chemicals with high quality for research!
Field of application
Ataciguat (HMR-1766) is a potent, specific soluble guanylate cyclase (sGC) activator with EC50 of 0.51 uM, preferentially activates the NO-insensitive heme-oxidized form of sGC.
Cas No.: 254877-67-3
Chemical Name: 5-chloro-2-[(5-chlorothiophen-2-yl)sulfonylamino]-N-(4-morpholin-4-ylsulfonylphenyl)benzamide
Synonyms: HMR-1766;HMR1766
SMILES: ClC1=CC(C(NC2C=CC(S(N3CCOCC3)(=O)=O)=CC=2)=O)=C(NS(C2=CC=C(Cl)S2)(=O)=O)C=C1
Formula: C21H19Cl2N3O6S3
M.Wt: 576.478
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Stasch, J.P., Pacher, P., and Evgenov, O.V. Soluble guanylate cyclase as an emerging therapeutic target in cardiopulmonary disease. Circulation 123(20), 2263-2273 (2011). 2. Schindler, U., Strobel, H., Schönafinger, K., et al. Biochemistry and pharmacology of novel anthranilic acid derivatives activating heme-oxidized soluble guanylyl cyclase. Molecular Pharmacology 69(4), 1260-1268 (2006). 3. Zhou, Z., Pyriochou, A., Kotanidou, A., et al. Soluble guanylyl cyclase activation by HMR-1766 (ataciguat) in cells exposed to oxidative stress. American Journal of Physiology.Heart and Circulatory Physiology 295(4), H1763-H1771 (2008).
Description: Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects[1][2][3].
Target: soluble guanylate cyclase[1]
In Vitro: Ataciguat (1-100 μM) induces the relaxation in aortic rings or coronary rings[2]. Ataciguat (0.1-10 μM; 30 min) increases NO production in HUVEC cells[2]. Ataciguat (1 nM-100 μM) induces concentration-dependent relaxations in sphincter of Oddi (SO) rings pre-contracted by Carbachol[3].
References: [1]. Schindler U, et, al. Biochemistry and pharmacology of novel anthranilic acid derivatives activating heme-oxidized soluble guanylyl cyclase. Mol Pharmacol. 2006 Apr;69(4):1260-8. [2]. Martinelli AM, et, al. In Endothelial Cells, the Activation or Stimulation of Soluble Guanylyl Cyclase Induces the Nitric Oxide Production by a Mechanism Dependent of Nitric Oxide Synthase Activation. J Pharm Pharm Sci. 2018;21(1):38-45. [3]. Çakmak E, et, al. Comparative Relaxant Effects of Ataciguat and Zaprinast on Sheep Sphincter of Oddi. Balkan Med J. 2016 Jul;33(4):453-7.
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