Ligas Organometálicas

<p>Positive allosteric modulator of the metabotropic glutamate receptor mGluR5 with EC50 in submicromolar range. The compound is able to increase mGluR5 function in vitro and in vivo. A study showed that ADX-47273 enhanced fear extinction learning as well as improved reversal learning in experimental animals.</p>

Prilocaine is a drug used as a local anaesthetic in dental procedures. It has been shown to reduce the incidence of pain caused. This drug is also a sodium channel blocker that blocks the influx of sodium into cells.

<p>3-Hydroxy-5-{[(naphthalen-2-yl)carbamoyl]amino}benzoic acid is a synthetic compound characterized by its complex molecular structure incorporating naphthalene and benzoic acid moieties. As a derivative of benzoic acid, it is typically synthesized through a series of chemical reactions designed to introduce the 3-hydroxy and carbamoyl functional groups, creating a compound with potentially unique bioactive properties.</p>

Potent and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor mGlu4. Valiglurax is orally bioavailable and CNS-penetrant mGlu4 PAM in preclinical development for the Parkinson’s disease therapy and alleviation of the motor symptoms.

Inhibitor of NLRP3 inflammasome and suppressor of the inflammatory cytokine IL-1β secretion. The compound was tested in diabetic mice and was shown to decrease the incidence of cardiac arrythmias, which are common secondary complications in diabetes mellitus. MCC 950 has potential to reverse diabetes-induced pathologies in cardiac electrophysiology.

<p>Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).</p>

Irsogladine is a gastroprotective drug that is used for the treatment of GERD and gastric ulcers. This drug also has antioxidant properties. Irsogladine is a phosphodiesterase-4 inhibitor and increases levels of cAMP. It helps to prevent and heal damage to the stomach lining.

Potent inhibitor of γ-secretase. LY 411575 inhibited production of amyloid β (Aβ) peptides with IC50 of 0.078 nM in vitro as well as decreased levels of Aβ40 and Aβ42 amyloids in brain of a mouse model for Alzheimer’s disease. In vitro studies confirmed that LY 411575 inhibited cleavage of Notch receptor at S3 site with IC50 of 0.39 nM, which blocked Notch activation and downstream signalling, leading to apoptosis in primary and immortalized Kaposi's sarcoma cells.

<p>Regaloside D is a natural product derived from plant sources, specifically isolated from certain species known for their bioactive properties. It functions as a glycoside, a compound in which a sugar is bound to a non-carbohydrate moiety, potentially influencing a variety of cellular processes through its interaction with specific molecular targets.</p>

<p>Crizotinib is a drug that belongs to the group of tyrosine kinase inhibitors. It is used in the treatment of cancers, including non-small cell lung cancer, small cell lung cancer, and other types of solid tumours. Crizotinib inhibits the activity of the tyrosine kinase ALK or anaplastic lymphoma kinase, which is involved in many signalling pathways and biological processes. The inhibition of this enzyme leads to decreased energy metabolism, reduced mitochondrial membrane potential and increased susceptibility to apoptosis.</p>

<p>Azumolene is a muscle relaxant drug, which is a synthetic derivative of dantrolene originating from hydantoin. The mode of action of Azumolene involves the inhibition of calcium ion release from the sarcoplasmic reticulum of skeletal muscle fibers. By impeding this release, Azumolene effectively reduces muscle contraction, thereby acting as a potent muscle relaxant.</p>

<p>Inhibitor of human neutrophil elastase</p>

Acetylcholinesterase inhibitor; therapy for Alzheimer's disease

A selective inhibitor of MEK1/2 kinase. Anti-proliferative and pro-apoptotic in multiple myeloma (MM) cells via G0/G1 cell cycle arrest and caspase 3 and PARP cleavage, respectively. Synergistic with other anti-MM therapies. Has anti-tumor effects in some solid tumors, such as in K-ras mutated colorectal cancer.

<p>AZD9567 is a selective glucocorticoid receptor modulator (SGRM), which is a synthetic pharmaceutical compound. Its source is rooted in medicinal chemistry efforts to design ligands that selectively interact with glucocorticoid receptors. The mode of action of AZD9567 involves binding to glucocorticoid receptors with high specificity, modulating their activity to trigger anti-inflammatory and immunomodulatory responses while minimizing common side effects associated with traditional glucocorticoids.</p>

Loratadine is a non-sedating, inverse agonist antihistamine used for the treatment of allergic rhinitis, an IgE (immunoglobulin E) mediated disease. Loratadine binds to histamine H1 receptors, preventing histamine from binding and causing an allergic reaction.It has been found to inhibit the release of eosinophil cationic protein by acting on different components of allergic inflammation, in particular in the modulation of ICAM-1 expression on nasal epithelial cells as a mechanism of protective for the epithelium, and therefore, the damage of mucosa is reduced. In recent studies, it was found that loratadine is a potent HR1 antagonist with in vitro inhbitory effect on human mast-cell lines, HMC-1 (from mast cell leukaemia) with an IC50 between 10 and 50 μM.Loratadine 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&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>K02288 is a small molecule inhibitor, which is derived from extensive chemical synthesis and compound screening techniques. It functions as a selective antagonist of the activin receptor-like kinase (ALK) pathway, specifically inhibiting Transforming Growth Factor-beta (TGF-β) superfamily receptor signaling. This pathway is crucial in a variety of cellular processes including proliferation, differentiation, and apoptosis, thereby making K02288 an important tool in cell signaling and cancer research.</p>

Vanilloid receptor 1 antagonist

<p>Nilutamide is an antineoplastic agent that is used to treat prostate cancer. This drug is an androgen receptor antagonist and binds with androgen receptors thus blocking its action and resulting in growth arrest.</p>

A selective antagonist of serotonin 5-HT2B receptors, inhibiting inositol phosphate formation and calcium release. Blocks 5-HT-induced contraction in rat stomach fundus. Reduces fecal output in vivo, upon inhibition of 5-HT2B by RS 127445, demonstrating a potential role for this receptor in colonic motility. Inhibits visceral hypersensitivity induced by restraint stress or colonic inflammation.