Ligands organométalliques

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<p>Mosapride is a prokinetic 5-HT4 receptor agonist used to increase colon and gastric mobility. This drug allows the release of acetylcholine from enteric cholinergic neurons. Mosapride has also shown to provide relief when treating patients with constipation- type irritable bowel syndrome as it prevents abdominal pain.</p>

<p>MKC8866 is a selective antagonist that targets the metabotropic glutamate receptor 2 (mGluR2), which is a type of glutamate receptor expressed in various regions of the central nervous system (CNS). Derived from pharmacological research, this compound offers critical insights into the modulation of synaptic activity and neuronal signaling through inhibition of mGluR2.</p>

<p>ML-109 is a synthetic chemical compound that acts as a feeding stimulant, commonly used in entomological research. It is developed through organic synthesis, allowing for precise manipulation of its molecular structure to optimize efficacy. The mode of action for ML-109 involves mimicking natural compounds that trigger feeding responses in insects, effectively activating chemoreceptors and neural pathways associated with food intake.</p>

<p>[Ni(dtbbpy)(H2O)4]Cl2 is a coordination complex, which is a specialized form of chemical compound where a central metal atom, in this case, nickel (Ni), is surrounded by ligands, such as 4,4'-di-tert-butyl-2,2'-bipyridine (dtbbpy) and water molecules. This complex is synthesized through a precise coordination process, where ligands are added to the metal center facilitating its unique structural properties.</p>

<p>Tolvaptan is a vasopressin receptor antagonist. It binds to the V2 receptor in the cytosol and prevents it from activating the aquaporin 2 channel, which regulates water permeability. Inhibition of vasopressin receptors in the kidneys improves fluid and electrolyte balance. Tolvaptan has been shown to be effective for treating congestive heart failure, as well as other disorders that are associated with fluid retention, such as renal dysfunction and metabolic syndrome. Tolvaptan can also be used in combination therapy with other drugs to treat these conditions.</p>

<p>Pelitrexol is an antifolate chemotherapeutic agent, which is synthetically derived to target key enzymatic pathways in cancer cells. It functions predominantly through the inhibition of dihydrofolate reductase (DHFR), an enzyme critical for DNA synthesis and cell proliferation. By impeding the action of DHFR, Pelitrexol disrupts the folate cycle, leading to a depletion of tetrahydrofolate and subsequent impairment of nucleotide biosynthesis. This action results in the inhibition of tumor cell growth and proliferation, making Pelitrexol an effective cytotoxic agent.</p>

<p>Anti-inflammtory drug</p>

<p>Amifostine trihydrate is a cytoprotective agent, which is a synthetic organic compound used primarily in oncology. It is a phosphorylated aminothiol prodrug derived from chemical synthesis. Its mode of action involves dephosphorylation to its active metabolite, WR-1065, by alkaline phosphatase enzymes present in normal tissues. This active form then scavenges free radicals and enhances DNA repair mechanisms, providing selective protection to normal tissues during chemotherapy or radiation therapy.</p>

<p>Inhibitor of monoamine oxidase</p>

<p>Stimulates somatotropin release</p>

<p>Neuroleptic agent</p>

<p>Tridentate iron chelator</p>

<p>ML 077 is a biofertilizer, which is a microbial-based product derived from naturally occurring soil microorganisms. It functions by colonizing plant root systems and facilitating nutrient uptake through symbiotic relationships with the host plant. This interaction promotes enhanced growth by converting atmospheric nitrogen into forms accessible to plants, along with improving phosphorus solubilization and mineral uptake.</p>

<p>GABA reuptake inhibitor</p>

<p>Inhibitor of topoisomerase TOP2</p>

<p>Adenosine A2A receptor antagonist</p>

<p>Topoisomerase II and DNA helicase inhibitor</p>

<p>A potent prostanoid receptor (FP) agonist and PGF2α analog. Its biological activity is mediated by action on prostamide receptors. Has therapeutic potential for glaucoma and ocular hypertension.</p>

<p>Competitive, reversible inhibitor of α-glucosidases used for the control of postprandial hyperglycaemia in patients with type 2 diabetes mellitus. It inhibits digestive enzymes with α-glucosidase activity, which breakdown complex sugars to absorbable monosaccharides. It also reduces the levels of glycated haemoglobin (HbA1c).</p>

<p>Inhibitor of tyrosinase in melanocytes: skin whitener</p>

<p>Bevirimat is an antiretroviral compound that is derived from a natural source, specifically from the betulinic acid found in certain plant species. This compound functions as a HIV-1 maturation inhibitor by interfering with the Gag protein processing, which is essential for the maturation and release of infectious virions. By preventing the final processing step in the Gag protein, Bevirimat disrupts the formation of the mature capsid core, leading to the production of non-infectious viral particles.</p>

<p>Encequidar is a small-molecule inhibitor, which is a synthetic chemical compound with the ability to modulate the activity of efflux transporters. It specifically targets P-glycoprotein (P-gp), an ATP-binding cassette transporter widely expressed in tissues such as the intestine, kidney, liver, and blood-brain barrier. By inhibiting P-gp, Encequidar enhances the oral bioavailability of co-administered therapeutic agents that are typically P-gp substrates, thereby improving their systemic absorption and therapeutic efficacy.</p>

<p>A potent and selective inhibitor of cyclin G-associated kinase (GAK) with Ki of 3.1 nM. The compound has more than 50-fold selectivity over the closest off-target kinase RIPK2, making it a potent tool for the study of GAK biology. SGC-GAK-1 was tested in vitro in human prostate carcinoma cell lines and showed strong growth inhibition in cell lines with androgen-dependent growth.</p>

<p>Inhibitor of dipeptidyl peptidase IV; anti-diabetic agent</p>

<p>5-HT1B/1D serotonin receptor agonist; anti-migraine agent; vasoconstrictive</p>

<p>S 0456 is a fluorescent dye for detecting anhydrase activity. This dye is degradable and can be used for imaging in living cells to detect tumors.</p>

<p>LY-404039 is a potent metabotropic glutamate receptor agonist with nanomolar affinity for group II receptors mGluR2 (Ki = 149 nM) and mGluR3 (Ki = 92 nM). It modulates glutamatergic activity in limbic and forebrain areas and has antipsychotic properties in animal studies. LY-404039 represents a potential new therapy for neurophysiatric disorders including schizophrenia, psychosis and anxiety.</p>

<p>Pasireotide acetate is a synthetic cyclic peptide and a somatostatin analogue, which is derived from the chemical synthesis based on the structure of native somatostatins. It operates by binding to somatostatin receptors with high affinity, primarily targeting the sst1, sst2, sst3, and sst5 receptor subtypes. This binding inhibits the secretion of adrenocorticotropic hormone (ACTH), which can modulate the excess production of cortisol in conditions such as Cushing’s disease.</p>

<p>Flavoxate is a muscarinic antagonist and spasmolytic drug that is used for the relief of conditions associatied with a lack of muscle control in the bladder such as urine urgency. This drug acts as a direct antagonist on acetylcholine receptors. This action reduces the tonus of smooth muscles in the bladder.</p>

<p>SU 3327, originally introduced as a thiadiazole JNK inhibitor (De et al. 2009) has recently been identified as having antibiotic activity against a broad range of bacteria including drug-resistant gram positive and negative strains (Strokes et al. 2020). This molecule has been given the fictional name ‘Halicin’ inspired by the AI approach used to discover its novel biological activity.</p>

<p>Endothelin receptor antagonist; vasodilator</p>

<p>Topoisomerase I inhibitor</p>

<p>Causes allergic hepatitis</p>

<p>mTOR kinase inhibitor; anti-neoplastic</p>

<p>Temozolomide is a cancer drug that belongs to the class of alkylating agents. It has been shown to have anticancer activity against human tumor cells in vitro. Temozolomide induces cell death by activating the apoptotic pathway. This drug also inhibits the cell cycle and blocks the G2-M phase, resulting in accumulation of cells at this point in the cell cycle. Temozolomide has been studied for its effects for cancer treatment in certain research approaches.</p>

<p>Estrogen ERβ receptor agonist; regulates GluR1, GluR2 and GluR3 expression</p>

<p>Inhibits human and mouse diacylglycerol O-acyltransferase 1 (DGAT-1) with IC50 values of 9 and 22 nM, respectively. Selective for DGAT-1 over DGAT-2 (IC50 = 53 µM), acyl coenzyme A transferase (IC50 = 296 µM) and other acyltransferases. Reduces plasma and liver triglycerides, FFA, chylomicron secretion and increases HDL cholesterol in vivo.</p>

<p>Muscle relaxant; anti-inflammatory</p>

<p>Microcolin B is a lipopeptide, which is a type of secondary metabolite. It is derived from marine cyanobacteria, specifically from the genus Lyngbya. This compound exhibits a complex mode of action, primarily by inhibiting the activity of protein kinase C (PKC), an enzyme that plays a crucial role in regulating immune responses and cell proliferation.</p>

<p>Antagonist of serotonin receptors 5-HT3</p>

<p>An active product of vitamin A metabolism. Activates RXR and RAR receptor isoforms with high binding affinity. Induces differentiation of neural stem cells into neurons.</p>

<p>Dopamine reuptake inhibitor</p>

<p>Apatinib, also known as rivoceranib, is an inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase. Apatinib targets VEGFR2 with its action and has proven to have strong anti-tumor effects in human cancers. In studies in mice, apatinib acted as an Inhibitor of VEGFR2 and played an antiangiogenic effect. Apatinib has been suggested for the treatment of ischemia-induced proliferative retinopathy and neovascular age-related macular degeneration.</p>

<p>Inhibitor of Abl and Src kinases; anti-proliferative; antineoplasticÂ</p>

<p>Uricosuric agent</p>

<p>Aldose reductase AKR1B10 inhibitor; hepatotoxic</p>

<p>Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases</p>

<p>C16(Plasm) LPC is a lysophosphatidylcholine, a type of lysophospholipid derived predominantly from plasma membrane phospholipids. It originates from the enzymatic action of phospholipase A2, which cleaves the fatty acid chain, typically at the sn-2 position. This leaves behind the lysophospholipid with a single acyl chain.</p>

<p>Angiotensin-converting enzyme inhibitor; anti-hypertensive</p>

<p>MG 132 is a modified tripeptide that acts as proteasomal inhibitor. In 2006, MG 132 has been experimentally tested in in vitro cell-based and in vivo models for to assess its use in the medical treatment of Parkinson's disease.</p>

<p>Synthetic antagonist of GnRH receptor</p>

<p>Histamine (H1) antagonist; used to treat allergies, rhinitis and urticaria</p>

<p>Anti-folate inhibitor of thymidylate synthase</p>

<p>Voxelotor is an oral therapeutic agent, which is a small molecule obtained through synthetic chemistry with targeted activity on hemoglobin. Its mode of action involves the allosteric modification of hemoglobin, specifically increasing hemoglobin oxygen affinity. By stabilizing the oxygenated hemoglobin state, voxelotor reduces the sickling and polymerization of red blood cells that are characteristic of sickle cell disease (SCD).</p>

<p>Please enquire for more information about Ceralifimod including the price, delivery time and more detailed product information at the technical inquiry form on this page</p>

<p>Iron chelator</p>

<p>Angiotensin-converting enzyme inhibitor; antioxidant</p>

<p>Inhibits acetylcholinesterase (AChE); antispasmodic agent</p>

<p>Protective agent against mercuric chloride poisoning</p>

<p>Recombinant protein against VEGF(A); binds placental growth factor (PIGF)</p>

<p>Inhibitor of protein kinases; induces apoptosis; anti-cancer</p>

<p>Nociceptin/orphanin FQ peptide receptor antagonist</p>

<p>5-HT6 serotonin receptor antagonist; anti-convulsant</p>

<p>Active metabolite of ifosfamide; alkylates and cross-links DNA; antineoplastic</p>

<p>Serine protease inhibitor</p>

<p>Inhibitor of DNA replication; inhibitor of theophylline and caffeine metabolism</p>

<p>FP receptor ligand; activator of PGF2αR</p>

<p>Inhibits Akt translocation by targeting the pleckstrin homology (PH) domain. Inhibits hepatitis C virus NS5B RNA-dependent RNA polymerase (IC50 = 79 µM). Attenuates cannabinoid agonist-mediated proliferation of neural stem/precursor cells.</p>

<p>Inhibitor of phosphodiesterase 7</p>

<p>Analogue of GABA; GABA receptor agonist used in epilepsy</p>

<p>Vismodegib is a Hedgehog (Hh) pathway inhibitor belonging to the 2-arylpyridine class. It acts as a competitive antagonist of the smoothened receptor (SMO) localized in the cell membrane. SMO activates an intracellular cascade that results in activation and nuclear translocation of Gli family transcription factor. Vismodegib has been used in clinical trials for treatment of advanced cancers.</p>

<p>1-NM-PP1, also known as 1NM-PP1, is an inhibitor of the Src kinase. Studies have shown that 1-NM-PP1 inhibits analog-sensitive kinases (as-kinases) characterised by a small amino acid as gatekeeper of the ATP binding site. Tested to prevent parasitic infections, 1-NM-PP1 inhibited the Toxoplasma gondii life cycle when used at a higher concentration than 500 nM.</p>

<p>Inhibitor of acetylcholinesterase</p>

<p>Inhibitor of NPM-ALK kinase</p>

<p>Sumoylation inhibitor; reported to inhibit histone acetylation transferase</p>

<p>Vasopressin acetate is a synthetic analog of the natural hormone vasopressin, which is derived from peptide synthesis. This product acts as an antidiuretic hormone, primarily targeting kidney receptors to promote water reabsorption and constrict blood vessels. Its mode of action involves binding to V1 and V2 receptors, leading to increased water retention and vasoconstriction.</p>

<p>Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic</p>

<p>Cyclosporin B is an antifungal and immunosuppressive cyclic peptide, which is derived from the fungus *Tolypocladium inflatum*. The compound is a member of the cyclosporin family, characterized by cyclic polypeptides with a unique arrangement of amino acids that enable its biological activity. Though its precise mode of action is not completely delineated, it is observed to influence cell growth and viability by potentially disrupting cellular communication or signal transduction pathways.</p>

<p>Pam3Csk4 (Pam3) is a TLR1/2 agonist which when combined with the TLR3 agonist polyinosinic:polycytidylic acid (polyI:C), forms the adjuvant system known as L-pampo. L-pampo has demonstrated the ability to produce stronger antibody generation against Hepatis B Virus compared to Alum and takes part in cell-mediated immune responses for example leading to elevated multifunctional CD4+ T cells. It has also shown its potential in producing strong humoral and cellular immune responses as an adjuvant against SARS-CoV-2.</p>

<p>PI3K enzyme inhibitor</p>

<p>Loreclezole is an antiepileptic drug, which is a synthetic compound with therapeutic effects on the central nervous system. This drug is classified as a 1,2-benzothiazole derivative and primarily impacts neuronal activity. Its source is entirely synthetic, developed through chemical synthesis processes designed to target specific neural pathways involved in seizure activity.</p>