779989-61-6

Usage

Molecular weight

388.47 g/mol

Chemical structure

1-Piperazinecarboxylic acid, 4-[(4-methylphenyl)methyl]-, 1,1-dimethylethyl ester

Purpose

To treat erectile dysfunction and benign prostatic hyperplasia

Mechanism of action

Inhibits the phosphodiesterase type 5 enzyme, allowing for increased blood flow to the penis during sexual stimulation

Classification

Phosphodiesterase inhibitor

Duration of action

Longer than other similar medications, up to 36 hours

Route of administration

Orally taken

Upstream product

• 23173-57-1 1-(4-methylbenzyl)piperazine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 104-87-0 4-methyl-benzaldehyde 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 

Downstream Products

• 23173-57-1 1-(4-methylbenzyl)piperazine 

Relevant academic research and scientific papers

Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer

Poly (ADP-ribose) polymerase-1 (PARP-1) is a potential target for the discovery of chemosensitizers and anticancer drugs. Amentoflavone (AMF) is reported to be a selective PARP-1 inhibitor. Here, structural modifications and trimming of AMF have led to a series of AMF derivatives (9a-h) and apigenin-piperazine/piperidine hybrids (14a-p, 15a-p, 17a-h, and 19a-f), respectively. Among these compounds, 15l exhibited a potent PARP-1 inhibitory effect (IC50 = 14.7 nM) and possessed high selectivity to PARP-1 over PARP-2 (61.2-fold). Molecular dynamics simulation and the cellular thermal shift assay revealed that 15l directly bound to the PARP-1 structure. In in vitro and in vivo studies, 15l showed a potent chemotherapy sensitizing effect against A549 cells and a selective cytotoxic effect toward SK-OV-3 cells through PARP-1 inhibition. 15l·2HCl also displayed good ADME characteristics, pharmacokinetic parameters, and a desirable safety margin. These findings demonstrated that 15l·2HCl may serve as a lead compound for chemosensitizers and the (BRCA-1)-deficient cancer therapy.

BICYCLIC PIPERAZINE COMPOUND AND USE THEREOF

The present invention provides a compound represented by the formula: wherein R1 is an acyl group, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.