Ataciguat

Ataciguat (CAS: 254877‑67‑3) is a highly valuable soluble guanylyl cyclase (sGC) activator widely used in cardiovascular pharmacology, drug discovery, and translational medicine. Featuring a unique molecular scaffold that sensitizes sGC to nitric oxide (NO) and directly activates the enzyme even under oxidative stress conditions, it offers potent vasodilatory, anti‑remodeling, and anti‑fibrotic properties. Its primary applications are outlined below:

1. Cardiovascular Pharmacology & Drug Discovery

Key Tool for sGC Activation Studies
Ataciguat is a well‑established pharmacological tool for investigating the sGC/cGMP signaling pathway. It is used to study heart failure, pulmonary arterial hypertension (PAH), systemic hypertension, and vascular remodeling in both in vitro and in vivo models.

NO‑Independent and NO‑Sensitizing Mechanisms
Unlike NO donors, Ataciguat directly stimulates sGC in its oxidized or heme‑free form, while also enhancing the enzyme’s sensitivity to low NO concentrations. This dual mechanism makes it invaluable for research on endothelial dysfunction, oxidative stress‑related cardiovascular diseases, and conditions with reduced NO bioavailability.

2. Preclinical Efficacy & Mechanistic Studies

Anti‑Remodeling and Anti‑Fibrotic Effects
Ataciguat has been shown to reduce cardiac hypertrophy, interstitial fibrosis, and vascular smooth muscle proliferation. Researchers use it to validate sGC as a therapeutic target for heart failure with preserved ejection fraction (HFpEF), hypertensive heart disease, and chronic kidney disease.

Vasodilation and Hemodynamic Regulation
The compound induces concentration‑dependent relaxation of pre‑constricted arteries (e.g., aortic, pulmonary, coronary). It is widely applied in ex vivo organ bath assays, pressure myography, and in vivo hemodynamic measurements to assess vascular function and test combination therapies.

3. Research & Development Applications

Target Validation and Pathway Analysis
Ataciguat serves as a selective pharmacological probe to confirm sGC involvement in phenotypic responses. It is used alongside genetic knockdown/knockout models and other sGC modulators (e.g., Riociguat, Cinaciguat) to dissect cGMP‑dependent signaling cascades.

High‑Throughput Screening (HTS) and Lead Optimization
With its well‑defined mechanism and established activity benchmarks, Ataciguat is employed as a positive control in HTS campaigns for novel sGC activators and in medicinal chemistry programs aiming to improve oral bioavailability or tissue selectivity.

4. Handling & Storage

Storage Conditions
Store as supplied at –20°C in tightly sealed, light‑protected containers. Protect from moisture and repeated freeze‑thaw cycles. Stock solutions in DMSO should be aliquoted and stored at –80°C for long‑term stability.

Intended Use
Ataciguat is intended for laboratory research, preclinical studies, and chemical development only. It is not for human therapeutic, diagnostic, or food use without appropriate regulatory approval.

Summary

The value of Ataciguat lies in its unique ability to activate sGC independently of NO and under oxidative stress conditions, combined with its well‑characterized vasodilatory and anti‑remodeling actions. This pharmacological profile supports innovative research in cardiovascular diseases, pulmonary hypertension, and fibrosis. Its reliable bioactivity and defined mechanism make it an indispensable tool for modern cardiovascular drug discovery and translational science.

For more information, please contact: selina@coreychem.com