Organometallic Ligands

<p>Cis/trans-form of GK 563 [2351820-19-2]</p>

<p>Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.</p>

<p>Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) and its negative regulator Kelch-Like ECH-Associated Protein 1 (Keap1) provide vital protection in maintaining cellular redox. In parallel, Nrf2 also aids the resolution of inflammation and also tissue repair. In homeostatic conditions, the transcription factor Nrf2 is controlled in a cytoplasmic complex with Keap1 with ubiquitination and protein degradation. Nrf2 has been linked to numerous cancers due to mutations affecting the binding region of Nrf2 to Keap1, resulting in Nrf2 dissociating from the complex. Nrf2 constitutively accumulates in the nucleus and activation of prosurvival genes that promote cancer cell proliferation.The Neh2 region of Nrf2 interacts with Keap1, as shown by nuclear magnetic resonance spectroscopy. The 16 amino acid peptide (AFFAQLQLDEETGEFL) (69-84) flanks the conserved ETGE motif and can replicate the binding to keap1.Therapeutics targeting the Nrf2 signalling pathway and activation of Nrf2 is a keen area of research, with many cancers being linked to Nrf2, particularly pancreatic cancer. Additionally, activation of Nrf2 has become a possible target as a treatment for COVID. Nrf2 (69-84) replicating full-length Nrf2 binding has been helpful in all cases.</p>

<p>Irbesartan is an angiotensin II receptor antagonist that is used to treat hypertension and congestive heart failure. It is also used to delay the progression of diabetic nephropathy. This drug works to works to relax smooth muscles and lower blood pressure.</p>

<p>R-(-)-Arundic acid is a chiral compound, which is a derivative of arundic acid specifically designed for enantiomeric purity. It is sourced through synthetic organic chemistry processes, allowing for precise control over its stereochemistry. The mode of action of R-(-)-Arundic acid involves the inhibition of astrocyte activation by modulating the synthesis of certain cytokines and inflammatory mediators. This mechanism provides a neuroprotective effect, making it a valuable tool in the study of neurodegenerative diseases and brain injuries.</p>

<p>Imipramine is a drug that belongs to the class of tricyclic antidepressant drugs. It is used in the treatment of depression and childhood enuresis. It is a potent inhibitor of serotonin and norepinephrine reuptake. Imipramine blocks D-2 receptors, H1 receptors, α-1 and α-2 adrenergic receptors and muscarinic receptors. Also, it is indicated for dysthymia, attention-deficit disorders, agoraphobia and it is effective in treating anxiety and panic disorders.</p>

<p>Tetrabenazine is a drug that has been used for the treatment of Parkinson's disease. It acts by inhibiting dopamine release and reducing the activity of nerve cells in the brain. Tetrabenazine Bio-X is used to treat dyskinesias, that are abnormal and involuntary muscle movements by inhibiting the monoamine transporter (VMAT2).<br>Tetrabenazine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use."</p>

<p>Inhibits DNA topoisomerase II; antineoplastic; immunomodulatory; antimicrobial</p>

<p>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.<br>Sorafenib is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Albuterol is a selective beta-2 adrenergic receptor agonist drug that is used to prevent and treat wheezing, shortness of breath, and other breathing difficulties caused by asthma. It relaxes the muscles in the airways, making them more open. Albuterol also has an anti-inflammatory effect.</p>

<p>Pitolisant is an inverse agonist and antagonist of the histamine (H3) receptor. It acts as an allosteric modulator of the H3 receptor to increase the activity of histamine at the M1 receptor. Pitolisant has been used in the treatment of narcolepsy, schizophrenia and Alzheimer's disease. Its mechanism of action involves binding to the amide group on histamine, which increases its affinity for the H3 receptor and enhances its activity at this site. Pitolisant has been shown to improve cognitive ability and reduce fatigue in patients with Alzheimer's disease.<br>Pitolisant is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Inhibitor of clathrin-mediated endocytosis (CME) and ligand to the clathrin heavy chain (CHC). ES9-17 is an inhibitor of the CHC function with EC50 of 13 μM in plant model Arabidopsis thaliana. ES9-17 is a non-protonophoric CME inhibitor and it does not alter the cytoplasmic pH levels substantially. In a mammalian cell line HeLa, ES9-17 reduced the uptake of transferrin, which is a CME-driven process.</p>

<p>Padsevonil is an investigational antiseizure medication, which is a synthetic pharmaceutical compound. It is derived from extensive medicinal chemistry research aiming to address complex seizure disorders resistant to conventional treatments. Padsevonil functions by exhibiting a dual mechanism of action. It binds to synaptic vesicle protein 2A (SV2A) with high affinity, similar to levetiracetam but with additional modulation of the benzodiazepine-sensitive gamma-aminobutyric acid-A (GABA-A) receptor. This combined activity potentiates its efficacy in stabilizing neuronal hyperactivity and dampening excitatory neurotransmission, providing a novel angle to tackle refractory seizures.</p>

<p>Substrate for proline-rich tyrosine kinase 2 (Pyk2)- can be used for substrate phosphorylation assays. Pyk2 is a member of the focal adhesion kinase (FAK) subfamily of cytoplasmic tyrosine kinases. Pyk2 is also known as: calcium-dependent tyrosine kinase (CADTK)- cellular adhesion kinase β- related adhesion focal tyrosine kinase (RAFTK)- or FAK2.Pyk2 functions as a scaffold protein, and it interacts with cytoplasmic proteins at focal adhesion sites to integrate different environmental signals. Pyk2 is activated by several stimuli, including elevated intracellular calcium levels, protein kinase C activation, and exposure to stress factors. Recently, Pyk2 has become a potentially important new therapeutic target or prognostic marker because overexpression of Pyk2 has been found in many human tumours.</p>

<p>Sparteine hydroiodide is the salt form of sparteine. This compound acts as an inhibitor of voltage-gated sodium channels. In organic chemisty, it is used for chiral synthesis.</p>

<p>Toceranib phosphate is a receptor tyrosine kinase inhibitor. Toceranib phosphate has been shown to be effective in the treatment of skin cancer and other types of cancer, including lung cancer and breast cancer. It is approved in the US as a treatment for canine mastocytoma (mast cell tumours).</p>

<p>Lacidipine is a lipophilic dihydropyridine calcium channel blocker that is used in the treatment of hypertension. This drug acts as an antihypertensive agent to dilate peripheral arteries and reduces blood pressure. Lacidipine blocks voltage-dependent L-type calcium channels.</p>

<p>Cyamemazine is a neuroleptic medication, which is a member of the phenothiazine class of compounds. It is synthesized from derivatives of phenothiazine, a group of agents primarily found in pharmaceuticals. The mode of action of cyamemazine involves antagonism at dopamine D2 receptors in the central nervous system. This inhibition of dopamine activity is the principal mechanism through which it exerts its antipsychotic effects. Due to its receptor activity, cyamemazine is used primarily in the management of various psychotic disorders, including schizophrenia and acute psychoses. It also exhibits anxiolytic properties, making it effective in treating anxiety associated with these conditions. By modulating neurotransmitter pathways, cyamemazine helps to alleviate symptoms such as hallucinations, delusions, and agitation, offering therapeutic benefit in complex neuropsychiatric cases. As an atypical antipsychotic, it provides an option for patients who may not respond adequately to other treatments. Although primarily used in a clinical setting, ongoing research continues to investigate potential wider applications and efficacy in treating other mental health issues.</p>

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

<p>H1-receptor antagonist</p>