Yonkenafil(CAS:804518-63-6)

Yonkenafil Hydrochloride (alias Tunodafil, CAS 804518-63-6) is a novel independently innovated and synthesized high-selectivity phosphodiesterase 5 (PDE5) small-molecule inhibitor in China. Breaking the single andrological application limitation of traditional PDE5 inhibitors, it possesses multiple superior pharmacological properties including ultra-high enzymatic inhibitory activity, excellent target selectivity, unique cerebral ischemic neuroprotection and myocardial repair effects, becoming an indispensable core research API for andrological pharmacology, stroke neuroprotection, neurodegenerative diseases and cardiovascular injury repair. With molecular formula C₂₄H₃₃N₅O₄S and molecular weight of 487.61, it appears as white crystalline powder with stable physicochemical properties and good solubility in common experimental solvents such as DMSO and methanol. Strict quality control over related substances, residual solvents and heavy metals ensures outstanding batch uniformity and experimental repeatability, fully supporting full-range research workflows including PDE enzyme activity screening, cavernous smooth muscle function tests, cerebral ischemia-reperfusion injury modeling, cognitive impairment intervention and myocardial infarction protection experiments.

In terms of core pharmacological mechanisms, Yonkenafil exerts dual independent functional pathways with better overall activity and safety than traditional analogs. Its peripheral andrological mechanism is clear and definite: it competitively binds to the catalytic site of PDE5 with an ultra-low IC50 of 2.0 nM, strongly inhibits cGMP hydrolysis, continuously elevates cGMP concentration in penile cavernous smooth muscle cells, mediates vascular dilation and blood flow surge, and stably improves moderate and severe erectile dysfunction caused by organic lesions, functional disorders and complications, featuring stable onset, moderate duration and fewer off-target side effects. Its most differentiated advantage lies in central neural and cardiovascular protection. It efficiently penetrates the blood-brain barrier and regulates multiple key cerebral signaling pathways: inhibiting excessive microglial activation after ischemia, reducing inflammatory factor release and cerebral edema; blocking neuronal apoptosis, upregulating BDNF and synaptophysin expression to repair damaged synaptic structures; restraining the negative regulatory Nogo-R pathway to lift neurogenesis inhibition, thereby significantly reducing cerebral infarct volume and improving post-stroke neurological behavioral deficits, with remarkable protective effects even under delayed administration after stroke onset.

In scientific research applications, Yonkenafil covers four core research fields with far broader application scenarios than conventional PDE5 compounds. Firstly, andrological pharmacological research: serving as a novel PDE5 positive control for efficacy evaluation of diabetic ED, postoperative ED and elderly sexual dysfunction models, guiding structural optimization of high-safety lead molecules. Secondly, ischemic stroke research: acting as a benchmark tool compound for exploring cerebral ischemia-reperfusion injury, nerve repair and cerebral edema intervention mechanisms, widely used in screening innovative neuroprotective stroke drugs. Thirdly, neurodegenerative disease research: improving cerebral microcirculation, promoting neurogenesis and inhibiting neuroinflammation to support mechanistic exploration of cognitive decline in Alzheimer’s disease and activity verification of candidate compounds. Fourthly, cardiovascular protection research: improving vascular endothelial function, inhibiting cardiomyocyte apoptosis, reducing myocardial fibrosis and infarct area, providing critical experimental support for the study of acute myocardial infarction and cardiac remodeling mechanisms.

In terms of raw material supply and industrial research value, Yonkenafil Hydrochloride is produced via mature total synthetic routes with refined purification technology that efficiently removes synthetic intermediates and isomeric impurities, ensuring stable biological activity without obvious batch differences. Available in milligram to kilogram specifications, it fully meets the R&D demands of university basic research, CRO preclinical efficacy evaluation, pharmaceutical structural optimization and generic drug development. It exhibits favorable in vivo administration tolerance with a wide safety window, suitable for long-term intervention experiments on chronic nerve injury and cardiovascular disease animal models. With the growing research demand for cardiovascular and cerebrovascular diseases, neurodegenerative disorders and male sexual dysfunction, multi-functional PDE5 modulators integrating andrological activity, central neuroprotection and myocardial protection have become a new hotspot in innovative drug R&D. Endowed with original domestic structure, clarified multi-target pharmacological pathways and abundant literature support, Yonkenafil maintains irreplaceable core research value in multidisciplinary small-molecule drug development and pharmacological research, promising broad and stable long-term application prospects in the global pharmaceutical research industry.