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. |