Ligas Organometálicas

<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>Amantadine is an antiviral drug that is used to treat dyskinesia in patients with Parkinson’s disease. This drug’s mechanism is not fully understood however it is said to aid in releasing dopamine from the nerve ending in brain cells. Amantadine is also an NDMA antagonist.</p>

<p>H1-receptor antagonist</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>Sn(IV) mesoporphyrin IX dichloride is a synthetic porphyrin derivative, which is a metalloporphyrin complex formed by the incorporation of tin into the porphyrin structure. This compound originates from the modification of mesoporphyrin IX, a naturally occurring tetrapyrrole, and is further functionalized with chloride ligands. The mode of action of Sn(IV) mesoporphyrin IX dichloride primarily involves the inhibition of heme oxygenase, an enzyme responsible for the catabolism of heme into biliverdin, carbon monoxide, and free iron. This inhibition results in the modulation of heme metabolism, which can have broad implications in various physiological and pathological processes.</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>A potent inhibitor of ubiquitin activating enzyme E1. Lowers ubiquitin conjugates in cells, thereby disrupting cell signalling, cell cycle progression and repair of DNA damage. Anti-tumor effects have been demonstrated in vitro and in vivo. TAK 243 has been used to study the biology of ubiquitins and its potential as anti-cancer therapy.</p>

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

<p>Etoposide is a cytotoxic drug used in cancer chemotherapy. It inhibits DNA replication through inhibition of DNA topoisomerase II, thus catalysing cell cycle arrest and apoptosis. <br>Etoposide 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>Finasteride is an antiandrogenic drug that belongs to the group of 5-alpha reductase inhibitors, which are used for the treatment of benign prostatic hyperplasia and male pattern baldness. The conversion of testosterone to 5α-dihydrotestosterone (DHT) is blocked by type II 5α-reductase inhibition, which then results in significant increase in prostatic testosterone concentrations and minimal to moderate increases in serum and tissue DHT concentrations. A reduction in DHT concentration will cause a reduction in prostatic volume as DHT appears to be the main androgen responsible for stimulating prostatic growth.</p>

<p>Partial inverse agonist of benzodiazepine sites of the GABAA receptors with anxiogenic properties. FG 7142 is a pharmacological stressor which generates anxiety in humans and in experimental animals such as rhesus monkeys and rodents. FG 7142 also reduces food intake and frequency of feeding in male and female rats.</p>

<p>Farnesyl pyrophosphate synthase inhibitor</p>

<p>Increases VEGF via heme oxygenase-1 modulation; anti-ulcer agent</p>

<p>Fondaparinux sodium is an anticoagulant, which is a synthetic pentasaccharide based on the antithrombin-binding sequence of heparin. As a meticulously engineered compound, it is derived by chemical synthesis. Its mode of action involves the selective inhibition of factor Xa, a critical enzyme in the coagulation cascade. By binding specifically to antithrombin III, it enhances the inactivation of factor Xa, thereby interrupting the pathway that leads to thrombin formation and ultimately preventing fibrin clot formation.</p>

<p>Rofecoxib is a non-steroidal anti-inflammatory drug that is used to treat osteoarthritis, acute pain and migraine attacks. This drug is also a COX-2 inhibitor. As a result, it reduces inflammation and pain.</p>

<p>Apo-D human is a glycosylated lipocalin protein, which is primarily derived from human plasma. It plays a pivotal role in the regulation of lipid-related metabolic processes due to its ability to bind and transport various ligands, including steroids and lipids. The protein's mode of action involves its function as a shuttle for small hydrophobic molecules, impacting cholesterol metabolism and potentially influencing lipid-related signaling pathways.</p>

<p>Inhibitor of metalloendopeptidase neprilysin</p>

<p>Beta-adrenoceptor antagonist; anti-hypertensive</p>

<p>Lofexidine is a drug that belongs to the group of α2-adrenergic receptor antagonists. It has been shown to reduce the symptoms of withdrawal from opiates and cocaine, as well as alcohol and nicotine. This drug inhibits the enzyme cAMP which catalyzes the conversion of dopamine to norepinephrine by preventing it from binding to its receptor site on cells.</p>

<p>Moexipril is an angiotensin converting enzyme inhibitor that is used for the treatment of hypertension. This drug is a prodrug for moexiprilat and works by relaxing the blood vessels causing them to widen and lowering blood pressure. Moexipril has been shown to be effective in treating metabolic disorders such as congestive heart failure.</p>

<p>Muscarinic antagonist; bronchodilator</p>

<p>Muscarinic acetylcholine receptor agonist</p>

<p>N-Desmethyl ibandronate sodium is a white crystalline solid with a melting point of 238-240 °C. It has versatile building block, complex compound and research chemicals applications. It is an intermediate used in the synthesis of other compounds, such as speciality chemicals, useful intermediates and useful scaffolds. N-Desmethyl ibandronate sodium can be used in reactions that require high quality and high purity products.</p>

<p>VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic</p>

<p>Induces expression of Oct3/4 transcription factor</p>

<p>Antagonist of dopamine (D2), serotonin (5-HT2A) and histamine H1 receptors</p>

<p>Lestaurtinib is a multitarget tyrosine kinase inhibitor of the JAK, FLT-3 and TrkA families of tyrosine kinases at nanomolar concentrations. It inhibits proliferation and induces apoptosis in vitro. Lestaurtinib is a FDA approved orphan drug for acute myeloid leukemia.</p>

<p>Inhibitor of vacuolar-type proton pump</p>

<p>Timolol is an ophthalmic beta-adrenergic blocker that is used to lower the intraocular pressure in patients with glaucoma. It is also used to treat hypertension, as well as other conditions, such as arrhythmias, thyrotoxicosis and angina pectoris. The drug acts by blocking β1-receptors on the surface of heart muscle cells and blood vessels, thereby reducing the workload on the heart and lowering blood pressure.</p>

<p>Thyrotropin-releasing hormone (TRH) receptor agonist; TRH analogue</p>

<p>Inhibitor of proteaseγ‐secretase, which allows to modulate of the activity of γ‐secretase substrates Notch, E-cadherin, ErbB4, and amyloid precursor protein (APP). The compound can inhibit the growth of tongue carcinoma cells by arresting cell cycle in G0–G1 phase, modulate the activity of Notch1 receptor and Caspase-3 protease and induce apoptosis. It was also demonstrated that this inhibitor reduces the levels of β-amyloid peptide in the brain of mice model for Alzheimer’s disease. This compound also enhances the neuronal differentiation embryonic cells.</p>

<p>Antagonist of platelet activating factor</p>

<p>Endothelin A receptor antagonist</p>

<p>A potent small-molecule activator of UNC-51-like kinase 1 (ULK1), a serine-threonine kinase involved in autophagy. Promotes cytoprotective autophagy in MPP+-treated SH-SY5Y cells, via the ULK complex. Improves motor dysfunction and reduces loss of dopaminergic neurons, mediated by MPTP, in in vivo models of Parkinson’s disease.</p>

<p>GnRH super-agonist</p>

<p>Dexrazoxane is a cytoprotective drug that is used in chemotherapy to provide cardio-protection against anthracycline toxicity. It is an antimitotic agent with immunosuppressive properties. Dexrazoxane works by binding to iron in the cell, preventing it from being released. Dexrazoxane is also a catalytic inhibitor of topoisomerase II.</p>

<p>Selective antagonist of the serotonin receptors 5-HT2A with subnanomolar affinity. The compound has clozapine-like anti-psychotic properties and more favourable CNS safety profile than traditional anti-psychotics. MDL 100907 has been used in studies on antisocial behaviour in mice and shown that the blockage of 5-HT2A receptors leads to decreased post-traumatic aggression and bradycardia.</p>

<p>Inhibitor of protein kinase CK1</p>

<p>Azilsartan is an angiotensin II receptor blocker that is used to treat hypertension. It blocks the binding of angiotensin II receptors to the AT1 receptor by selectively binding to AT1 receptors as an antagonist, blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.</p>

<p>Selective vasopressin receptor V2 agonist</p>

<p>Selective inhibitor of the transforming growth factor beta receptor TGFβ1. RepSox can replace Sox, a transcriptional factor required for cell self-renewal, in reprogramming of adult cells to induced pluripotent stem cells (iPSCs). In the cloned interspecies embryos, RepSox induced expression of pluripotency regulatory genes Oct4 and Nanog, improved viability and developmental potential of embryos in the pre-implantation stage.</p>

<p>Tandospirone is a psychotropic drug that acts as a selective serotonin receptor partial agonist. It is derived from a synthetic source, specifically targeting the 5-HT1A receptors in the brain. Tandospirone modulates serotonergic neurotransmission by binding to these receptors, which are associated with mood regulation. This action results in the anxiolytic and antidepressant effects observed with the drug.</p>

<p>Eltrombopag is an agonist of thrombopoietin receptor TpoR, which triggers activation of the JAK2/STAT5 signalling pathway. This drug is indicated in individuals with thrombocytopenia since it leads to increased proliferation of megakaryocyte progenitor cells and increased production of platelets. Eltrombopag also enhances expansion of human umbilical cord blood hematopoietic stem/primitive progenitor cells and promotes hematopoiesis.</p>

<p>VE 822 is a potent and selective inhibitor of ATR protein kinase, which is derived through chemical synthesis with a high specificity for ATR over related kinases. ATR, or ataxia telangiectasia and Rad3-related kinase, plays a critical role in the cellular response to DNA damage and replication stress. VE 822 achieves its mode of action by interfering with ATR’s catalytic activity, thereby halting the DNA damage response and rendering cancer cells more susceptible to DNA-damaging agents.</p>

<p>RIPK2 protein kinase inhibitor; EGFR inhibitor</p>

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

<p>Pidotimod is a small molecule (dipeptide) that acts as immunomodulator. It activates the immune system by binding to Toll-like receptor (TLR) 4 and TLR2 and it is involved in the regulation of TLRs signaling pathways. Pidotimod has chemokine activity on CXC chemokine receptor 3 (CXCR3) that triggers monocyte adhesion and migration by activation of tyrosine phosphorylation-based cell signaling. Recent studies showed that pidotimod can be used to treat acute respiratory tract infections (RTIs) and its pharmacokinetic studies has shown its ability to boost the immunoresponse and favouring the increase in the level of immunoglobulins (IgA, IgM, IgG) and T-lymphocytes (CD3+, CD4+). Pidotimod also exhibits anti-inflammatory properties by inhibiting the production of pro-inflammatory molecules such as IL-6 and TNF-α, which are linked to autoimmune diseases.</p>

<p>Inhibitor of PDE4 enzyme</p>

<p>Amoxapine is a dibenzoxazepine- derivative tricyclic antidepressant or TCA. It is used in the treatment of depressive disorders and psychotic depression. Amoxapine is a potent serotonin and norepinephrine reuptake inhibitor. It works on the central nervous system to increase levels of the chemicals in the brain.</p>