Ligas Organometálicas

<p>ABTL-0812 is an investigational anticancer compound, which is a synthetic small molecule with a novel mechanism of action. It is derived from the research efforts focused on targeting key metabolic pathways in cancer cells. The mode of action of ABTL-0812 involves the modulation of the Akt/mTOR pathway, leading to the induction of autophagy-mediated cell death, a process that is selectively cytotoxic to cancer cells.</p>

<p>Orally available and central nervous system-penetrant inhibitor of GlyT1 glycine transporter SLC6A9. PF 03463275 was shown to enhance neuroplasticity and cognitive remediation in schizophrenia patients. In animal studies, PF 03463275 also influenced retina as changes in electroretinogram were detected in albino rats.</p>

<p>Prostaglandin F2α receptor agonist</p>

<p>CLP257 is a synthetic compound characterized as an inhibitor of chloroplastic RNA polymerase. It is derived from a systematic chemical synthesis process involving the rational design of inhibitory molecules targeting chloroplastic transcriptional machinery. This product acts by binding to the RNA polymerase complex, effectively disrupting the transcription process within chloroplasts. The inhibition occurs through allosteric modulation, where CLP257 induces conformational changes that impede the enzyme's ability to synthesize RNA.</p>

<p>Decitabine is a synthetic cytosine analogue that incorporates into DNA and prevents DNA methylation via DNA (cytosine-5)-methyltransferase 1 (DNMT1) inhibition. It has demonstrated potent anti-leukaemic effects attributed to cell cycle arrest and induction of apoptosis. Also, it has anti-growth effects on solid tumor cell lines.<br>Decitabine 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>Apraclonidine is an alpha adrenoreceptor agonist that is used in the treatment of raised intraocular pressure. This drug’s mechanism of action is not fully understood however, animal and human studies suggested that Apraclonidine reduces aqueous humor production and increases uveoscleral outflow.</p>

<p>Enzastaurin is a synthetic small molecule inhibitor, which is derived from chemical synthesis with a primary mode of action as an inhibitor of protein kinase C beta (PKCβ). As a potent pathway modulator, it disrupts signal transduction pathways involved in cell proliferation and survival. The inhibition of PKCβ is particularly important as this enzyme is linked to the progression and survival of certain cancer types. Through this mechanism, Enzastaurin impedes the downstream activities that promote tumor growth and angiogenesis.</p>

<p>Parecoxib is a COX-2 inhibitor and belongs to the group of pharmacological agents. It is a prodrug of valdecoxib that is used for the treatment of osteoarthritis and rheumatoid arthritis, as well as other conditions where the reduction in pain and inflammation are desired.</p>

Flupirtine is a pyridine derivative that is used as a non-opioid analgesic. Flupirtine promotes Bcl-2, raises glutathione levels, activates an inward rectifying potassium channel, and reverses the effect of calcium on neuronal cell death by inhibiting its release from intracellular stores. Although it doesn't attach to the receptor, flupirtine functions as an NMDA receptor antagonist. It is used for the treatment of fibromyalgia.

<p>TAS-120 is a small-molecule inhibitor, which is an orally bioavailable therapeutic agent. This product is sourced through synthetic chemistry, specifically designed to target fibroblast growth factor receptors (FGFRs) that harbor genetic alterations. The mode of action of TAS-120 involves irreversible binding to FGFR, disrupting downstream signaling pathways crucial for tumor cell proliferation and survival. By selectively inhibiting these aberrant FGFRs, TAS-120 impedes oncogenic signaling and thereby induces cancer cell apoptosis, effectively controlling tumor growth.</p>

<p>Acipimox is a niacin derivative that is used as a hypolipidemic agent. Acipimox prevents the liver from producing triglycerides and from secreting VLDL, which indirectly results in a slight decrease in LDL and an increase in HDL. Also, it stimulates leptin release and improves insulin sensitivity.</p>

<p>NBD 18:0 ceramide is a synthetic fluorescent lipid analogue, which is derived from the naturally occurring sphingolipid, ceramide. This product is characterized by the attachment of a nitrobenzoxadiazole (NBD) fluorophore to the ceramide backbone, allowing it to serve as a tool for visualizing and studying lipid dynamics within biological membranes.</p>

<p>Inhibitor of CETP exchange protein</p>

<p>5-HT2C receptor agonist; antipsychotic</p>

<p>Idelalisib is a pharmaceutical drug that functions as a PI3Kδ inhibitor, developed through synthetic chemical processes. Its mode of action involves selectively targeting and inhibiting phosphatidylinositol 3-kinase delta (PI3Kδ), a lipid kinase that plays a crucial role in the signaling pathways responsible for cell proliferation, survival, and differentiation. By inhibiting this enzyme, Idelalisib effectively impedes pathways that are often hyperactivated in certain hematologic malignancies, thereby exerting antitumor effects.</p>

<p>Modulator of S1P receptor</p>

<p>Agonist of H3 and H4 receptors</p>

<p>Bexarotene is a retinoid and antineoplastic agent that is used for the treatment of solid tumours and t-cell lymphomas. It inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin and research has shown that it induces tumor regression in vivo in some animal models.</p>

<p>Moracin C is a prenylated flavonoid, which is a type of naturally occurring compound. It is derived from the Morus genus, commonly known as mulberry trees. This compound functions primarily as an antioxidant, showing activity that may protect cells from oxidative stress by neutralizing free radicals.</p>

<p>Cladribine is a purine nucleoside analogue that interferes with DNA synthesis by acting as a false building block in the DNA chain during replication. Cladribine is incorporated into the growing DNA chain, causing chain termination and leading to DNA damage, apoptosis (programmed cell death), and ultimately cell death. Cladribine is structurally similar to adenosine, but is partially resistant to breakdown by adenosine deaminase due to a chlorine molecule at position 2. This causes it to accumulate in cells and interfere with the targeted cell's ability to process DNA. This mechanism of action makes cladribine an effective treatment for certain types of cancer and autoimmune diseases, where it targets rapidly dividing cells.</p>

<p>LW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor used for cancer treatment.</p>

<p>NADPH oxidase inhibitor; anti-inflammatory</p>

<p>Bremelanotide acetate is a synthetic peptide therapeutic, which is derived from the melanocortin receptor agonist class. Its primary source involves chemical synthesis designed to mimic endogenous hormone analogs that target specific receptors in the body. The mode of action of bremelanotide acetate involves activating melanocortin receptors, particularly the MC4 receptor in the central nervous system. This activation leads to modulation of brain pathways involved in sexual arousal and desire.</p>

<p>Carmustine is a DNA alkylating agent which also cross-links DNA. As a result, Carmustine disrupts the function of DNA, resulting in the arrest the cell cycle and apoptosis. Consequently these properties of Carmustine, in addition to its ability to easily transmit through the blood-brain barrier, means it can be used as a cancer treatment, treating cancers such as, breast, ovarian and pancreatic as well as lymphomas and leukemias. Furthermore Carmustine can contribute to cytotoxic effects through its ability to carbamoylate DNA repair enzymes and proteins.</p>

<p>Promestriene is a synthetic estrogen derivative, which is sourced from modifications of the natural hormone estradiol. It functions by binding to estrogen receptors, primarily focusing on the mucosal and epithelial tissues. This interaction stimulates cellular proliferation and increases the thickness of the epithelial layers, thereby promoting tissue regeneration and hydration.</p>

<p>Specific inhibitor of the phosphoinositide 3-kinase (PI3K) alpha subunit with IC50 of 32 nM. In heart muscle it negatively regulates hypertrophic growth, causes increase in late sodium current and leads to arrhythmias. In tumours it inhibits the p110α subunit of PI3K and blocks growth factor signalling resulting in reduced tumour growth.</p>

<p>Maprotiline is a tetracyclic antidepressant that is used for the treatment of major depressive disorder and anxiety that is associated with depression. This drug inhibits noradrenaline reuptake and has anticholinergic properties. Additionally, Maprotiline inhibits the amine transporter which allows for a delay in the reuptake of noradrenaline.</p>

Inhibitor of COX-1 and COX-2 cyclooxygenases

<p>A specific inhibitor of Bone Morphogenetic Protein (BMP) type 1 receptors ALK2 and ALK3 (IC50  &lt; 0.5 µM). Dorsomorphin analog that exclusively targets the BMP but not VEGF signaling. It is able to inhibit the BMP-induced Smad1/5/8 activation but not the p38/MAP kinase signaling or Activin A-induced Smad2 activation.</p>

<p>Lapatinib is an antineoplastic agent used to treat breast and lung cancer. This drug is also a tyrosine kinase inhibitor and inhibits human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1). Lapatinib has shown to inhibit ERBB-driven tumor cell growth in vitro and in various animal models.</p>

<p>6-OAU is a chemical compound categorized as a cytokinin-like molecule, which is derived from natural plant sources. It functions by modulating gene expression and hormone pathways involved in various plant growth and developmental processes. The mode of action of 6-OAU largely revolves around mimicking the activity of cytokinins, essential plant hormones that regulate cell division, shoot and root growth, as well as delay senescence.</p>

2-Amino-3-phosphonopropanoic acid is a chemical compound classified as a phosphonic acid derivative, which is obtained through synthetic processes in a laboratory setting. It acts as a selective antagonist of metabotropic glutamate receptors (mGluRs), specifically inhibiting the function of these receptors by blocking the normal action of the neurotransmitter glutamate, which is a critical excitatory neurotransmitter in the central nervous system. This blockade affects synaptic transmission and modulates neurological signals.

<p>Gonadotropin-releasing hormone agonist</p>

<p>Gestodene is a progestogen hormonal contraceptive. It is an agonist of the progesterone receptor. Additionally, this drug is used in menopausal hormone therapy.</p>

<p>Carmofur is an antineoplastic agent that is used to treat various cancers such as breast and colorectal cancer. This drug is a derivative of fluorouracil. Carmofur is an inhibitor of the human acid ceramidase, a lysosomal amidase involved in the development of cancer cells.</p>

Ticagrelor is a P2Y12 receptor antagonist that has been shown to reduce the risk of myocardial infarction. It inhibits the formation of thromboses. Ticagrelor binds to the adenosine diphosphate (ADP) site on the platelet P2Y receptor and prevents ADP from activating this receptor. It is used for the prevention of myocardial infarctions, strokes and cardiovascular disease.

<p>Inhibits actin polymerization</p>

<p>Cilastatin is a renal dehydropeptidase inhibitor drug that is used to prevent degradation of imipenem. It is used to treat a variety of infections in combination with imipenem. This drug blocks the mechanism of imipenem which is hydrolyzed by dehydropeptidase-I.</p>

<p>Inhibitor of dihydroorotate dehydrogenase; anti-inflammatory; immunomodulatory</p>

<p>A metabolite of arachidonic acid, synthesised by COX enzymes and prostaglandin E synthases (PGEs). Binds to EP1, EP2, EP3 and EP4 receptors with high affinity (Kd &lt; 10 nM). Therapeutic potential for analgesia, pain relief and arthritic diseases. Enhances differentiation and expansion of iPSC-derived hematopoietic progenitor cells.</p>

<p>Inhibitor of BACE1 protease</p>

<p>Inhibitor of CK2 protein kinase; anti-proliferative</p>

<p>L-type calcium channel blocker; anti-hypertensive</p>

<p>BI-0115 is a highly selective inhibitor for the lectin-like oxidised low-density lipoproteins (LDL) receptor 1 (LOX-1). In vitro, BI-0115 inhibits internalisation of oxidised LDL (oxLDL) with IC50 of 5.4?µM. The crystal studies revealed that BI-0115 glues two LOX-1 dimers together, resulting in blocked access of oxLDL. LOX-1 is a Ctype lectin-like receptor expressed on endothelial cells, macrophages and vascular smooth muscle. It is responsible for the regulation, internalisation and degradation of oxidised low-density lipoproteins (oxLDL). BI-0115 is a novel inhibitor to LOX-1 and is a valuable tool to study LOX-1 biology, and their role in diseases, such as, cancer and atheroschelerosis.</p>

<p>Microtubule-stabilizing agent; antineoplastic;</p>

<p>A selective P2X7 receptor antagonist with an IC50 value of 11.2 nM. Prevents breast cancer resistance protein (BCRP)-mediated transport of methotrexate. Has therapeutic potential for osteoarthritis due to its anti-proliferative and pain-relieving effects.</p>

Losartan is an angiotensin receptor drug that is used to treat hypertension. It works by blocking the activity of angiotensin II binding to the AT1 receptor. As a result, this causes vascular smooth muscle relaxation and lowers blood pressure.

<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 tosylate 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.</p>

<p>Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic</p>

<p>Tabernanthalog fumarate is a synthetic derivative of ibogaine, a naturally occurring indole alkaloid, which is synthesized through chemical modifications to enhance its therapeutic profile. The source of Tabernanthalog fumarate is the laboratory synthesis of ibogaine analogs, designed to retain beneficial effects while reducing undesirable properties such as toxicity. Its mode of action involves modulation of multiple neurotransmitter systems, including serotonin receptors, as well as the NMDA receptor pathway, potentially altering neural plasticity and connectivity in a favorable manner.</p>