gp 2.5

CGP 25454A is a novel and selective antagonist of the presynaptic dopamine autoreceptor (CGP 25454A).

Formoterol fumarate (Eformoterol Hemifumarate), an effective, specific and long-acting β2-adrenoceptor agonist, is utilized in the treatment of chronic obstructive pulmonary disease(COPD) and asthma.

KGP-25 is an inhibitor of the voltage-gated sodium channel 1.8 (Nav1.8), utilized for analgesia by targeting the peripheral nervous system (PNS). Additionally, it targets the γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for use as a general anesthetic.

P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor, reducing P-gp activity by a factor of 2.5 and 3.0 at 1.25 μM and 2.5 μM, respectively. It exhibits anti-proliferative effects on certain cancer cells and restores cellular sensitivity to Vincristine and Paclitaxel, reversing the multidrug resistant (MDR) phenotype of ABCB1/Flp-InTM-293 and KBvin.

Indium (III) thiosemicarbazone 5b is an anticancer compound demonstrating cytotoxicity against various cancer cell lines including A549, MCF-7 breast, cisplatin-resistant MCF-7/DDP breast, and Hl 7702 liver cancer cells, with IC50 values of 2.41, 1.97, 2.11, and 8.95 µM, respectively. It effectively lowers PI3K, Akt, mTOR, P-gp, and GSH levels in MCF-7/DDP cells. In vivo studies show that at a dosage of 2.5 µmol/kg, indium (III) thiosemicarbazone 5b significantly reduces tumor weight and volume in MCF-7/DDP mouse xenograft models. Furthermore, liposomes formulated with this compound promote apoptosis and pro-death autophagy in MCF-7/DDP cells, alongside notable reductions in tumor volume and weight, showcasing its potential as a therapeutic agent in cancer treatment.