Ataciguat

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 5-chloro-2-[[(5-chloro-2-thienyl)sulfonyl]amino]-N-[4-(4-morpholinylsulfonyl)phenyl]-benzamide
• Correlated keywords
  • 254976-06-2 sGC agonists activators oxidized hemes ferric cGMP vasorelaxation solubles guanylates cyclases nitric oxides signaling NO cyclic GMP hypertensions hyperlidemia cardiovascular diseases diabetes anthranilic acids derivatives oxidized heme-free free oxidizes purified bovine lungs crude humans corpus cavernosum binding binds pockets mimicking functions levels cultured rats aorta smooth muscles cells induces isolated porcine coronary arteries activates primary cellular receptors groups conversions GTP seconds messengers cascades inhibiting inhibits inhibitors proliferations leukocytes recruitments platelets aggregations oxidations dissociations impairments nucleotides biochemistry vasculars isolates
• Product Overview:
  Soluble guanylate cyclase (sGC) is the primary cellular receptor for NO. NO binds and activates a heme group in sGC, initiating the conversion of GTP to the second messenger cGMP. cGMP subsequently mediates a number of signaling cascades leading to vasorelaxation and inhibiting smooth muscle proliferation, leukocyte recruitment, and platelet aggregation. Oxidation of the heme results in its dissociation from sGC and an impairment of NO signaling, which has been linked to hypertension, hyperlidemia, cardiovascular disease, and diabetes.{26751} Ataciguat is an anthranilic acid derivative that activates the oxidized (heme-free) form of sGC (EC50 = 0.5-10 µM in purified bovine lung or crude human corpus cavernosum isolates) by binding to the heme pocket and mimicking its function.{26751,26750,26752} It has been shown to increase cGMP levels in cultured rat aorta smooth muscle cells and to induce vasorelaxation of isolated rat aorta, porcine coronary arteries, and human corpus cavernosum (EC50 = 1-10 µM).{26750}