406228-55-5

Usage

Uses

Used in Pharmaceutical Industry:
A-385358 is used as a PDE inhibitor for the treatment of erectile dysfunction. Its ability to increase blood flow by inhibiting the breakdown of cyclic nucleotides makes it a potential therapeutic agent for improving erectile function in patients.
Used in Cardiovascular Medicine:
A-385358 is used as a PDE inhibitor for the management of cardiovascular diseases. By promoting vasodilation and smooth muscle relaxation, it may help in treating conditions such as hypertension, angina, and other related cardiovascular disorders.
Used in Drug Development Research:
A-385358 is used as a research compound for further exploration of its potential applications in medicine. Its mechanism of action as a PDE inhibitor provides a basis for investigating its effects on various physiological processes and its possible use in treating other conditions that may benefit from enhanced cyclic nucleotide signaling.

Upstream product

• 4160-82-1 3,3-dimethylglutaric anhydride 
• 94-09-7 p-aminoethylbenzoate 
• 1493-27-2 ortho-nitrofluorobenzene 
• 872866-36-9 (S)-3-(2-nitro-4-sulfamoylphenylamino)-4-phenylsulfanylbutyric acid tert-butyl ester 
• 872866-38-1 (S)-N,N-dimethyl-3-(2-nitro-4-sulfamoylphenylamino)-4-phenylsulfanylbutyramide 
• 872866-37-0 (S)-3-(2-nitro-4-sulfamoylphenylamino)-4-phenylsulfanylbutyric acid 
• 279692-22-7 4-(4-carboxy-3,3-dimethyl-butyrylamino)-benzoic acid ethyl ester 
• 279692-23-8 ethyl 4-(4,4-dimethyl-2,6-dioxopiperidin-1-yl)benzoate 
• 406233-25-8 ethyl 4-(4,4-dimethylpiperidin-1-yl)benzoate 
• 406233-31-6 4-fluoro-3-nitrobenzenesulfonamide 
• 406233-26-9 4-(4,4-dimethylpiperidin-1-yl)benzoic acid 
• 872866-39-2 4-((S)-3-dimethylamino-1-phenylsulfanylmethylpropylamino)-3-nitrobenzenesulfonamide 
• 406233-32-7 (R)-3-(2-nitro-4-sulfamoylphenylamino)-4-phenylsulfanylbutyric acid tert-butyl ester 
• 406233-34-9 (R)-N,N-dimethyl-3-(2-nitro-4-sulfamoylphenylamino)-4-phenylsulfanylbutyramide 

Relevant academic research and scientific papers

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo

Development of a rationally designed potentiator of cancer chemotherapy, via inhibition of Bcl-XL function, is described. Lead compounds generated by NMR screening and directed parallel synthesis displayed sub-μM binding but were strongly deactivated in the presence of serum. The dominant component of serum deactivation was identified as domain III of human serum albumin (HSA); NMR solution structures of inhibitors bound to both Bcl-X L and HSA domain III indicated two potential optimization sites for separation of affinities. Modifications at both sites resulted in compounds with improved Bcl-XL binding and greatly increased activity in the presence of human serum, culminating in 73R, which bound to Bcl-XL with a Ki of 0.8 μM. In a cellular assay 73R reversed the protection afforded by Bcl-XL overexpression against cytokine deprivation in FL5.12 cells with an EC50 of 0.47 μM. 73R showed little effect on the viability of the human non small cell lung cancer cell line A549. However, consistent with the proposed mechanism, 73R potentiated the activity of paclitaxel and UV irradiation in vitro and potentiated the antitumor efficacy of paclitaxel in a mouse xenograft model.