Ligas Organometálicas

<p>Irdabisant is a novel small-molecule therapeutic, which functions as a histamine H3 receptor antagonist or inverse agonist. This compound is chemically synthesized and designed to target the central nervous system. The mode of action involves the selective inhibition of presynaptic H3 receptors, which are primarily responsible for modulating the release of histamine and other neurotransmitters such as acetylcholine, norepinephrine, and dopamine. By inhibiting these receptors, Irdabisant enhances neurotransmitter release, facilitating improved synaptic transmission.</p>

<p>SR8278 is a synthetic, chemical compound that functions as a highly selective inverse agonist of the Rev-Erb nuclear receptors, which is derived from extensive biochemical research. It operates by binding to these orphan nuclear receptors, Rev-Erbα and Rev-Erbβ, inhibiting their activity. This antagonistic action disrupts the regulation of circadian rhythms, metabolism, and inflammatory responses that these receptors typically control. This modulation occurs at the transcriptional level, where SR8278 interferes with gene expression governed by Rev-Erb receptors.</p>

<p>Sparstolonin B is a natural anti-inflammatory compound, which is derived from the Chinese herb *Sparganium stoloniferum*. It primarily functions as a selective antagonist of Toll-like receptors 2 and 4 (TLR2 and TLR4), thereby inhibiting the activation of these pathways which are crucial in mediating inflammatory responses.</p>

<p>AZD5069 is a small molecule that serves as a potent and selective antagonist of the CXC chemokine receptor 2 (CXCR2). It is derived from synthetic pharmaceutical research efforts aimed at targeting key signaling pathways in inflammatory diseases. This compound functions by inhibiting the CXCR2 receptor, which plays a critical role in the recruitment and activation of neutrophils, a type of white blood cell involved in inflammation and immune responses.</p>

<p>C26 Carnitine-d9 is a stable isotopically labeled form of carnitine, which is a quaternary ammonium compound naturally synthesized from amino acids lysine and methionine in the human body. Its isotopic labeling with deuterium enhances its application in various analytical techniques while retaining the biological properties of natural carnitine. The mode of action involves carnitine's essential role in the transport of long-chain fatty acids into the mitochondrial matrix for β-oxidation, facilitating energy production. C26 Carnitine-d9 is used primarily in metabolic research and diagnostics, particularly in studying fatty acid metabolism, assessing metabolic disorders, and quantifying carnitine levels in biological samples through techniques such as mass spectrometry. Its stable isotopic label allows for precise tracking and quantitation, offering insights into metabolic pathways and biochemical assays crucial for understanding metabolic functions and potential dysfunctions.</p>

<p>SB743921 HCl is a synthetic small-molecule compound, which is a derivative of the well-known kinesin spindle protein (KSP) inhibitors. Originating from sophisticated medicinal chemistry, it acts by selectively binding to the KSP, a motor protein essential for the mitotic spindle formation during cell division.</p>

<p>Inhibitor of EGFR, HER2 and HER4 tyrosine kinases</p>

<p>Antagonist of Aurora A serine/threonine protein kinase; antineoplastic</p>

<p>(±)-Carazolol-d7 is a deuterated beta-adrenergic receptor antagonist, often used for pharmacological and biochemical studies. This isotopically labeled compound is a synthetic derivative of carazolol, sourced through precise deuterium exchange techniques designed to ensure high isotopic purity.</p>

<p>MRTX849 is a small molecule inhibitor, which is derived through rational drug design targeting specific oncogenic mutations. It acts as a covalent inhibitor that selectively targets the KRAS G12C mutation, a prevalent alteration in various cancers such as non-small cell lung cancer and colorectal cancer. The mode of action involves binding to the mutated KRAS G12C protein, locking it in an inactive GDP-bound state, thereby inhibiting downstream signaling pathways crucial for tumor cell proliferation and survival.</p>

<p>Cyclosporine U is a cyclic polypeptide immunosuppressant, which is a derivative of the natural product Cyclosporine A, produced by the fermentation process involving the filamentous fungus *Tolypocladium inflatum*. It primarily acts by inhibiting the activity of calcineurin, a phosphatase enzyme, which in turn blocks the transcription of interleukin-2 and other cytokines. This mechanism suppresses the activation of T-lymphocytes, a crucial component in the immune response.</p>

<p>Lanabecestat is an investigational drug, classified as a beta-secretase (BACE) inhibitor, which is derived from synthetic chemical processes. Its mode of action involves inhibiting the enzyme beta-secretase, which plays a crucial role in the amyloidogenic pathway by cleaving amyloid precursor protein (APP) into amyloid-beta peptides. The accumulation of these peptides is a hallmark of Alzheimer's disease pathology.</p>

<p>A2A adenosine receptor antagonist</p>

<p>HMG-CoA reductase antagonist</p>

<p>nAChRs nicotinic receptor antagonist; neuromuscular-blocking agent</p>

<p>Inactive enantiomer of the inhibitor of myosin II-ATPase</p>

<p>Peroxy Orange 1 is an advanced cleaning agent, which is a hydrogen peroxide-based product enriched with surfactants and orange oil extracts. This formulation originates from a blend of both synthetic and natural sources, integrating the oxidizing power of hydrogen peroxide with the cleaning efficacy of citrus oils.</p>

<p>Cyclosporin G is an immunosuppressive agent, which is derived from fungal sources with a specific mode of action that involves inhibiting calcineurin. The source of Cyclosporin G is primarily from the fermentation of the fungus *Tolypocladium inflatum*. Its mode of action involves binding to the cytosolic protein cyclophilin in T-lymphocytes, which subsequently inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby reducing the transcription of interleukin-2 and other cytokines critical for T-cell activation.</p>

<p>TNO155 is an innovative therapeutic agent, commonly classified as a small-molecule inhibitor, which is derived from rational drug design based on precision oncology principles. Its mode of action involves selective inhibition of a specific protein tyrosine phosphatase, which plays a critical role in cellular signaling pathways that are often dysregulated in cancer. This inhibition effectively disrupts aberrant signaling, thereby suppressing tumor cell proliferation and inducing apoptosis in malignant cells.</p>

<p>Inverse agonist of cannabinoid receptor CB1R. Taranabant was studied for its effect on smoking cessation and inducing weight loss. Serious adverse effects associated with this compound prevented further development as a drug in the clinic.</p>