Ataciguat (Synonyms: HMR 1766) |
Catalog No.GC11361
One-Click Copy Product Info
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Ataciguat is a nitric oxide-independent soluble guanylate cyclase (sGC) activator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 254877-67-3
Sample solution is provided at 25 µL, 10mM.
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Ataciguat is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat activates the oxidized heme iron redox form of sGC to stimulate cGMP production. Ataciguat can be used in research related to heart failure and aortic valve stenosis[1-4].
In vitro, Ataciguat (0.1–10μM) was used to treat HUVEC cells for 30 minutes. Ataciguat significantly increased NO production in the cells[5]. Rat aortic smooth muscle cells were pretreated with H₂O₂ (500μM) for 1 hour, followed by treatment with Ataciguat (10μM) for 15 minutes. Ataciguat significantly increased cGMP production in the cells[6].
In vivo, Ataciguat (10mg/kg; twice daily) was administered by gavage to adult male Wistar rats with chronic myocardial infarction induced by coronary ligation for 10 weeks. Ataciguat significantly improved vascular function and reduced platelet activation[7]. Ataciguat (10mg/kg; once daily) was subcutaneously injected into C57Bl/6J mice with pulmonary arterial hypertension induced by chronic hypoxia for 14 days (from day 21 to day 35 of hypoxia). Ataciguat significantly reduced pulmonary arterial hypertension and right ventricular hypertrophy[8].
References:
[1] Schindler U, Strobel H, Schönafinger K, 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] Çakmak E, Yönem Ö, Saraç B, et al. Comparative Relaxant Effects of Ataciguat and Zaprinast on Sheep Sphincter of Oddi. Balkan Med J. 2016 Jul;33(4):453-7.
[3] Zhang B, Enriquez-Sarano M, Schaff HV, et al. Reactivation of Oxidized Soluble Guanylate Cyclase as a Novel Treatment Strategy to Slow Progression of Calcific Aortic Valve Stenosis: Preclinical and Randomized Clinical Trials to Assess Safety and Efficacy. Circulation. 2025 Apr;151(13):913-930.
[4] Fraccarollo D, Galuppo P, Motschenbacher S, et al. Soluble guanylyl cyclase activation improves progressive cardiac remodeling and failure after myocardial infarction. Cardioprotection over ACE inhibition. Basic Res Cardiol. 2014 Jul;109(4):421.
[5] Martinelli AM, Rodrigues CNDS, Moraes TF, 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.
[6] Zhou Z, Pyriochou A, Kotanidou A, et al. Soluble guanylyl cyclase activation by HMR-1766 (ataciguat) in cells exposed to oxidative stress. Am J Physiol Heart Circ Physiol. 2008 Oct;295(4):H1763-71.
[7] Schäfer A, Fraccarollo D, Werner L, et al. Guanylyl cyclase activator ataciguat improves vascular function and reduces platelet activation in heart failure. Pharmacol Res. 2010 Nov;62(5):432-8.
[8] Weissmann N, Hackemack S, Dahal BK, et al. The soluble guanylate cyclase activator HMR1766 reverses hypoxia-induced experimental pulmonary hypertension in mice. Am J Physiol Lung Cell Mol Physiol. 2009 Oct;297(4):L658-65.
| Cell experiment [1]: | |
Cell lines | Rat aortic smooth muscle cells (RASMCs) and COS7 cells |
Preparation Method | RASMCs were pretreated with H₂O₂ (500μM) for 1 hour, then incubated with Ataciguat in the presence of IBMX (1mM) for 15 minutes. |
Reaction Conditions | 10μM; 15 minutes |
Applications | Ataciguat significantly increased cGMP production in cells exposed to oxidative stress. Ataciguat was more effective in stimulating heme-free soluble guanylyl cyclase (sGC) compared to the wild-type enzyme. Exposure of cells to Ataciguat did not lead to the development of tolerance. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Chronic myocardial infarction was induced by coronary ligation in male Wistar rats. Animals were treated with Ataciguat (10mg/kg/twice; daily by gavage) starting from day 10 after surgery for 10 weeks. |
Dosage form | 10mg/kg; oral gavage; twice daily for 10 weeks |
Applications | Ataciguat improved endothelium-dependent vasorelaxation and normalized vascular sensitivity to exogenous NO. Ataciguat reduced aortic superoxide production and increased in vivo platelet VASP phosphorylation. Ataciguat decreased platelet P-selectin surface-expression and attenuated ADP-induced platelet aggregation. |
References: | |
| Cas No. | 254877-67-3 | SDF | |
| Synonyms | HMR 1766 | ||
| Chemical Name | 5-chloro-2-[[(5-chloro-2-thienyl)sulfonyl]amino]-N-[4-(4-morpholinylsulfonyl)phenyl]-benzamide | ||
| Canonical SMILES | O=S(N1CCOCC1)(C2=CC=C(NC(C3=CC(Cl)=CC=C3NS(C4=CC=C(Cl)S4)(=O)=O)=O)C=C2)=O | ||
| Formula | C21H19Cl2N3O6S3 | M.Wt | 576.5 |
| Solubility | ≤1mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7346 mL | 8.673 mL | 17.3461 mL |
| 5 mM | 346.9 μL | 1.7346 mL | 3.4692 mL |
| 10 mM | 173.5 μL | 867.3 μL | 1.7346 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)