Organometallic Ligands

<p>Etodolac is a non-steroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis and rheumatoid arthritis. It is also used to treat acute pain. This drug works by inhibiting prostaglandin synthesis from the inhibition of the enzyme cyclooxygenase.</p>

<p>NAP is a neuroprotective peptide, which is derived from activity-dependent neuroprotective protein (ADNP), with a mechanism involving microtubule stabilization and neuronal protection. It exhibits the ability to protect neurons from various types of damage, including oxidative stress and conditions mimicking neurodegenerative diseases. NAP enhances axonal transport and increases the resilience of neurons to insults that would typically result in cell death. This peptide has shown promise in preclinical studies for its potential to halt or reverse cognitive decline, making it a focal point for research into therapeutic strategies for disorders like Alzheimer's disease and other tauopathies. The peptide operates by binding to microtubules, promoting stability, and facilitating efficient transport of cellular components. Studies have highlighted its role in traversing the blood-brain barrier, which makes it a viable candidate for central nervous system-targeted therapies. Researchers continue to explore its efficacy and possible applications in improving cognitive function and providing neuroprotection in aging populations.</p>

<p>Racemic mixture of AMG 510</p>

<p>Agonist of alpha7 subtype of nural nicotinic acetylcholine receptor</p>

<p>(2R)-Arimoclomol maleate is an investigational pharmaceutical compound, which is an orally bioavailable small molecule with pharmacological activity primarily targeting cellular protein homeostasis mechanisms. This therapeutic agent is derived from molecular chaperones and operates by selectively enhancing the expression of heat shock proteins (HSPs). The mechanism of action involves the modulation of the heat shock response, wherein (2R)-Arimoclomol maleate amplifies the natural cellular defense pathways against protein misfolding and aggregation.</p>

<p>Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.</p>

<p>Inhibitor of EIF2AK3/PERK kinases</p>

<p>AZD-7648 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), which is a pivotal enzyme involved in the non-homologous end joining (NHEJ) pathway of DNA repair. This product is derived from extensive chemical synthesis and optimization, designed for its specificity and efficacy in inhibiting DNA-PK activity. The mode of action involves binding to the ATP-binding site of DNA-PK, thereby obstructing its ability to facilitate the repair of double-strand DNA breaks.</p>

<p>Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin receptors. It was designed to treat mood disorders, such as depression. It has been shown to improve mood by increasing the levels of certain neurotransmitters in the brain such as dopamine and noradrenaline. Agomelatine has beneficial phase-shifting effects in humans; it causes a sleep phase advance, a drop in body temperature, and an initial release of melatonin. According to controlled human studies, Agomelatine is equally effective at treating severe depression as the SSRI antidepressants paroxetine and sertraline.</p>

<p>Inhibits p38 MAP kinase; anti-inflammatory; neuroprotective</p>

<p>Zileuton is an inhibitor of the 5-lipoxygenase enzyme, thus preventing the leukotrienes LTE4, LDT4, LTB4 and LTC4 from being formed. This in turn reduces inflammation, bronchoconstriction and mucus secretion in the airways. As a result, Zileuton can be used in the treatment and management of asthma and allergic rhinitis. Studies have shown that Zileuton has the potential to reverse dementia-related brain damage.</p>

<p>17:0-20:4Pi (4) P is a synthetic phosphoinositide, which is a type of phospholipid. It is typically sourced from laboratory synthesis, often incorporating stable isotopes or specific fatty acid chains to mimic natural compounds found in cell membranes. This product functions primarily as a probe in biochemical experiments, particularly for studying lipid signaling pathways within cells.</p>

<p>Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic</p>

<p>Antagonist of cardiac potassium channel HERG; anti-psychotic</p>

<p>3-Hydroxy-5-{[(naphthalen-2-yl)carbamoyl]amino}benzoic acid is a synthetic compound characterized by its complex molecular structure incorporating naphthalene and benzoic acid moieties. As a derivative of benzoic acid, it is typically synthesized through a series of chemical reactions designed to introduce the 3-hydroxy and carbamoyl functional groups, creating a compound with potentially unique bioactive properties.</p>

<p>Inhibitor of ABC transporters; oral bioenhancer for anti-cancer therapy</p>

<p>Dapagliflozin is a sodium-glucose cotransporter subtype 2 (SGLT2) inhibitor that can be used in the treatment of diabetes mellitus type 2. It inhibits glucose reabsorption in the proximal tubule of the nephron and results in glycosuria, which helps to improve glycaemic control. Also, Dapagliflozin is used to lower the risk of sustained eGFR decline, end-stage renal disease, cardiovascular death, and hospitalization for heart failure in patients with chronic kidney disease who are at risk of progression.</p>

<p>Cetilistat is a drug that is used to treat obesity. This drug inhibits the enzyme pancreatic lipase and so it prevents triglycerides from being hydrolyzed into absorbable free fatty acids.</p>

<p>Potent and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor mGlu4. Valiglurax is orally bioavailable and CNS-penetrant mGlu4 PAM in preclinical development for the Parkinson’s disease therapy and alleviation of the motor symptoms.</p>

<p>Activater of the Nrf2 pathway and an inhibitor of the NF-κB pathway.  Possible applications have extended to anti-viral treatment of COVID-19.</p>