Ligands organométalliques

<p>Hypoglycemic agent</p>

<p>Inhibitor of protein tyrosine phosphatase PTP1B</p>

<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>9''-Methyl salvianolate B is a naturally derived phenolic acid compound, specifically a methylated derivative, extracted from the roots of Salvia miltiorrhiza. This plant, commonly known as Danshen, is widely used in traditional Chinese medicine. The compound’s primary source involves a meticulous extraction and purification process aimed at isolating its bioactive constituents.</p>

<p>VU0453379 is a chemical compound that functions as a positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor. It is synthetically derived through medicinal chemistry processes designed to selectively enhance receptor signaling pathways. VU0453379 acts by binding to an allosteric site on the M4 receptor, distinct from the orthosteric site where endogenous neurotransmitters bind. This binding potentiates receptor sensitivity and activity in response to acetylcholine, thereby amplifying receptor-mediated signaling pathways.</p>

<p>5-Hydroxymatrine is an alkaloid compound, which is derived from the roots of Sophora plants, notably Sophora flavescens. This compound is characterized by its structure as a quinolizidine alkaloid and is a modified form of matrine, with a hydroxyl group adding to its chemical complexity.</p>

<p>Liarozole is an imidazole derivative that functions as a non-specific inhibitor of cytochrome P450-dependent retinoic acid metabolism. It primarily acts by inhibiting the cytochrome P450 enzyme family, particularly affecting the 4-hydroxylation process. This inhibition increases the local concentration of retinoic acid in tissues, which can lead to a modulation of transcriptional activity by retinoic acid receptors and ultimately influence cellular proliferation and differentiation.</p>

<p>GW 3965 hydrochloride is a selective liver X receptor (LXR) agonist, which is a synthetic compound derived through pharmaceutical research aimed at modulating lipid metabolism. It functions by binding to and activating LXRs, which are nuclear receptors that regulate the expression of genes involved in cholesterol, fatty acid, and glucose homeostasis. Upon activation, these receptors influence the transcription of various target genes, leading to increased cholesterol efflux, decreased intestinal cholesterol absorption, and modulation of inflammatory responses.</p>

<p>GLP-1 (1-37) (human, bovine, guinea pig, mouse, rat) trifluoroacetate salt is a posttranslational modification of the endogenous human hormone GLP-1. It is a synthetic form of this hormone that has been modified to allow for improved stability and solubility. This peptide is found in the pancreatic alpha cells and intestinal L cells and stimulates the release of insulin from pancreatic beta cells. GLP-1 (1-37) (human, bovine, guinea pig, mouse, rat) trifluoroacetate salt has also been shown to increase glucose uptake by muscle tissue as well as stimulate the release of incretin hormones such as glucagon-like peptide 1 and gastric inhibitory polypeptide. GLP-1 (1-37) (human, bovine, guinea pig, mouse, rat) trifluoroacetate salt</p>

<p>Siponimod fumarate is a selective sphingosine 1-phosphate (S1P) receptor modulator, which is a synthetically derived agent with immunomodulatory properties. Its mode of action involves high affinity for S1P receptors 1 and 5, which plays a crucial role in immune cell signaling. By binding to these receptors, siponimod sequesters lymphocytes in lymphoid organs, reducing peripheral blood lymphocyte counts and thereby modulating immune responses.</p>

<p>IRAK4-IN-1 is a small molecule inhibitor, which is a synthetic compound designed to interfere with specific biological pathways. This product originates from extensive chemical synthesis and medicinal chemistry efforts, aimed at targeting key components of the immune signaling cascade. Its primary mode of action involves selective inhibition of interleukin-1 receptor-associated kinase 4 (IRAK4), a crucial kinase in the Toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) pathway. By inhibiting IRAK4, IRAK4-IN-1 effectively downregulates downstream inflammatory signaling processes.</p>

<p>Odevixibat is a pharmacological agent that functions as an ileal bile acid transport inhibitor, which is synthesized through complex organic chemistry methods to create a specific molecular structure targeting bile acid transport mechanisms. It works by inhibiting the apical sodium-dependent bile acid transporter (ASBT) in the terminal ileum. This action reduces the reabsorption of bile acids from the small intestine back into the liver, thereby reducing overall bile acid levels in the body.</p>

<p>p38α MAP kinase inhibitor; JNK2α2 protein kinase inhibitor</p>

<p>Cl2A-SN-38 is an innovative antibody-drug conjugate (ADC), which is derived from a targeted delivery system designed to enhance the therapeutic index of chemotherapeutic agents. The product is synthesized through the chemical conjugation of the monoclonal antibody Cl2A with the potent topoisomerase I inhibitor, SN-38. This conjugation is achieved using a stable linker that facilitates selective delivery of SN-38 to cancer cells expressing the target antigen, thus minimizing systemic toxicity.</p>

<p>ARQ 531 is a small molecule inhibitor specifically designed to target Bruton's tyrosine kinase (BTK), which is a type of enzymatic protein. This compound is meticulously developed within a laboratory setting to disrupt key pathways involved in cancer cell survival. Its mode of action involves the selective and reversible inhibition of BTK, thereby obstructing signal transduction that promotes malignant cell proliferation and survival.</p>

<p>1-(7Z-Pentadecenoyl)-rac-glycerol is a glycerol derivative, which is typically synthesized or isolated from natural fats and oils. This compound is part of the monoacylglycerol family, characterized by a glycerol backbone esterified with a single fatty acid chain. The source of 1-(7Z-Pentadecenoyl)-rac-glycerol can be varied, stemming from enzymatic processes that occur in biological systems, or through chemical synthesis that mimics these natural interactions.</p>

<p>Imidazole ketone erastin is a small molecule compound, which is a synthetic analog derived from erastin. The origin of this compound is rooted in the study of ferroptosis, a form of regulated cell death characterized by iron-dependent lipid peroxidation. Imidazole ketone erastin functions by inhibiting the cystine/glutamate antiporter system Xc–, leading to the accumulation of lethal reactive oxygen species (ROS) within cells.</p>

<p>AM 4668 is a biochemical compound, which is derived from synthetic origins with complex organic synthesis processes. Its primary mode of action involves targeted enzymatic inhibition, effectively interacting with specific enzyme active sites to modulate biochemical pathways.</p>

<p>PRI-724 is an investigational small molecule known as a selective inhibitor of the Wnt/β-catenin signaling pathway. It is derived from extensive research into targeting dysregulated cellular pathways implicated in oncogenesis. PRI-724 operates by binding to the transcriptional co-activator CBP, thereby disrupting the interaction between CBP and β-catenin, which is crucial for the transcription of genes involved in cell proliferation and survival.</p>

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

<p>A β2-adrenoceptor agonist that is structurally related to salbutamol. Ellicits β-adrenergic stimulatory effects on smooth muscles in trachea and bronchi. More effective (1.5 to 2 times more) as a bronchodilator than salbutamol.</p>

<p>Puromycin is an aminonucleoside antibiotic, derived from the bacterium Streptomyces albus, with its primary mode of action involving the inhibition of protein synthesis. During translation, puromycin mimics the aminoacyl end of tRNA, enabling its incorporation into the growing polypeptide chain within the ribosome. This incorporation disrupts further chain elongation, ultimately leading to premature termination of protein synthesis.</p>

<p>Please enquire for more information about ML191 including the price, delivery time and more detailed product information at the technical inquiry form on this page</p>

<p>p38 MAP kinase antagonist</p>

<p>PAF, short for Platelet-activating factor, is a mediator of platelet aggregation and a ligand for PAF receptors. It has roles in many other leukocyte functions around inflammation and immune response, as well as, chemotaxis and vasuclar changes. The PAF signaling system can trigger significant inflammatory and thrombotic cascades, and has been show to have roles in septic shock.</p>

<p>an orally active, reversible and selective CXCR4 (CD184, fusin) antagonist</p>

<p>Miransertib (ARQ 092) HCl is a selective inhibitor, which is a synthetic small molecule specifically targeting the AKT pathway. It is sourced through specialized chemical synthesis designed to interfere with key signaling pathways implicated in the proliferation and survival of cancer cells. The mode of action involves the inhibition of the serine/threonine kinase AKT, an integral part of the PI3K/AKT/mTOR signaling pathway that is frequently dysregulated in various cancers.</p>

<p>Perakine is an indole alkaloid, which is a naturally occurring compound obtained primarily from the plant Rauvolfia species. As an indole alkaloid, it is synthesized through complex biosynthetic pathways within the plant, involving the secondary metabolism that characterizes many biochemical systems in flora.</p>

<p>AZD4205 is an investigational therapeutic agent, which is a small molecule inhibitor developed by AstraZeneca. It is designed to target specific signaling pathways involved in cancer cell proliferation and survival. The source of AZD4205 lies in the meticulous synthesis of a compound specifically engineered to interfere with aberrant molecular processes within cancer cells.</p>

<p>Berubicin is an anthracycline-based chemotherapeutic agent, which is a semi-synthetic derivative sourced primarily from the bacterium Streptomyces peucetius. It operates by intercalating into DNA strands, disrupting the replication and transcription processes, which ultimately induces apoptosis in rapidly dividing tumor cells.</p>

<p>A non-metabolizable allolactose analogue, widely used in molecular biology for overexpression of recombinant proteins from inducible systems under the control of lac promoter. IPTG binds to the LacI repressor and causes its release from the lac operator, allowing gene expression to take place. Present in vectors of pGEX, pGEM-T, pET, pRSET, pMAL class and others.</p>

<p>DT2216 is a small-molecule anticancer compound, which is a product of rational drug design originating from advanced chemical synthesis techniques. The primary mode of action of DT2216 involves selectively targeting and disrupting BCL-XL interactions with pro-apoptotic proteins. By specifically degrading BCL-XL, DT2216 enhances the induction of apoptosis in cancer cells, thereby addressing the challenge of resistance associated with conventional therapies.</p>

<p>Azilsartan medoxomil is an antihypertensive drug, which is a prodrug of the angiotensin II receptor blocker azilsartan. It is synthesized through a chemical process involving the modification of the medoxomil ester, converting it into its active form upon absorption in the gastrointestinal tract. The primary mode of action of azilsartan medoxomil involves selective antagonism of the angiotensin II type 1 (AT1) receptor. By blocking the effects of angiotensin II—a potent vasoconstrictor—azilsartan medoxomil effectively reduces vascular resistance, leading to decreased blood pressure.</p>

<p>Rosuvastatin is a synthetic lipid-lowering agent, which is a product of pharmaceutical manufacturing derived from extensive research in cardiovascular pharmacology. It functions as an HMG-CoA reductase inhibitor, effectively blocking the enzyme responsible for cholesterol biosynthesis in the liver. By inhibiting this enzyme, Rosuvastatin reduces the production of cholesterol, especially low-density lipoprotein (LDL) cholesterol, which is known to contribute to atherosclerosis.</p>

<p>Oltipraz metabolite M2 is a pharmacologically active compound, which is derived from the metabolism of Oltipraz, a well-known chemopreventive agent. This metabolite is produced through hepatic biotransformation processes and plays a critical role in mediating the biological effects associated with its parent compound.</p>

<p>First generation PI 3-kinase inhibitor</p>

<p>Mozavaptan is a pharmacological agent that acts as a vasopressin V2 receptor antagonist. It is derived through synthetic chemical processes designed to target specific neurohormonal pathways in the body. Mozavaptan exerts its effects by inhibiting the action of vasopressin, a hormone that promotes water reabsorption in the kidneys. By blocking the vasopressin receptors, it enhances water excretion and corrects imbalances in electrolyte levels, particularly addressing conditions like hyponatremia.</p>

<p>KUNB31 is a synthetic enzyme inhibitor, which is an engineered compound designed to interfere with the activity of specific enzymes in various biochemical pathways. This product is synthesized through a series of complex chemical reactions, ensuring high specificity and activity against target enzymes. Its mode of action involves binding to the active sites of enzymes, thereby preventing substrates from interacting and altering enzymatic activity.</p>

<p>Dooku1 is a synthetic biochemical compound designed for advanced research applications. It is derived through a complex series of organic synthesis processes that utilize specialized reactants and catalysts to achieve high purity and specificity. The compound functions by selectively binding to molecular targets, allowing researchers to investigate cellular pathways and molecular interactions with greater precision.</p>

<p>Bifluranolum is a synthetic nonsteroidal antiandrogen, which is synthesized in laboratory settings and not derived from natural sources. Its mode of action involves competitive inhibition of androgen receptors. By occupying these receptor sites, Bifluranolum inhibits the binding of endogenous androgens, effectively blocking their physiological actions. This property makes it a valuable tool in studies related to androgen-dependent biological processes.</p>

<p>Uprifosbuvir is an investigational antiviral compound, which is a nucleotide analog prodrug of uridine. It functions by targeting the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, an essential enzyme for viral RNA replication. As an uridine nucleotide analog, Uprifosbuvir interferes with the viral replication process by incorporating itself into the viral RNA, leading to chain termination.</p>

<p>JDQ-443 is a synthetic chemical compound, which is a product of organic synthesis, with a precise mode of action targeting specific cellular enzymes. This compound functions as an enzymatic inhibitor, designed to interfere with the activity of a specific class of enzymes critical to cellular proliferation pathways. JDQ-443 exerts its effects by binding to the active sites of these enzymes, thereby preventing substrate access and subsequent catalysis.</p>

<p>E3 Ligase Ligand 1a is a small molecule ligand, which is typically synthesized in a laboratory setting. The ligand acts as a recruiter for E3 ubiquitin ligases, proteins that play a pivotal role in the ubiquitin-proteasome pathway. By binding to an E3 ligase, the ligand can facilitate the ubiquitination and subsequent degradation of target proteins. This mechanism is central to modulating protein levels within a cell, enabling researchers to study protein function and regulation dynamically.</p>

<p>rac Enterolactone -13C3 is a stable isotope-labelled lignan, which is a type of compound derived from plant sources. It is biosynthesized through the conversion of dietary lignans by intestinal microbiota. The -13C3 label indicates that three carbon atoms in the compound have been replaced with the carbon-13 isotope, facilitating precise analytical tracking. This product acts as a tracer, allowing scientists to study metabolic pathways and the bioavailability of lignans in biological systems.</p>

<p>Heat shock protein 90 (HSP90) inhibitor</p>

<p>μ- and κ- opioid receptor antagonist; partial agonist of δ- opioid receptors</p>

<p>UM729 is an advanced surface coating, which is a chemical formulation with the aim of enhancing surface durability and protection. Sourced from novel polymeric materials, UM729 is designed to form a robust and resilient layer when applied to various substrates. Its mode of action involves cross-linking at the molecular level, creating a cohesive barrier that offers resistance to environmental factors such as abrasion, moisture, and UV radiation.</p>

<p>ROPA or resiniferonol 9,13,14-orthophenylacetate is an analogue of resiniferatoxin that has been shown to have synergistic interactions with detergents, such as Tween-80, in the removal of wheat germ agglutinin (WGA) from Brucella. ROPA is also active against herpes simplex virus and tumour necrosis factor-alpha (TNF-α). When combined with a basic protein, it can activate the receptor and inhibits the formation of dry weight. ROPA has been shown to be able to inhibit the growth of infectious bacteria, such as those that cause tuberculosis or brucellosis. The mechanism for this inhibition is not clear, but may be due to its ability to bind to water molecules and inhibit their binding with bacterial cytoplasmic membranes.</p>

<p>Benzoic acid 5-amino-1-(4-methoxy-benzenesulfonyl)-1H-pyrazol-3-yl ester is a synthetic chemical compound used primarily in advanced organic synthesis. It is derived from benzoic acid and functionalized with a pyrazole moiety, enhancing its reactivity and versatility in chemical transformations. This compound acts as an intermediate in the synthesis of more complex molecules, playing a crucial role as a precursor or reagent due to its unique structure, which facilitates targeted chemical modifications.</p>

<p>ALX-1393 is a synthetic compound that acts as an inhibitor, specifically targeting the glycine transporter 1 (GlyT1). As a small molecule inhibitor derived from chemical synthesis, it modulates neurotransmitter systems by blocking the reuptake of glycine, an important co-agonist of the NMDA receptor, in the central nervous system. The mode of action of ALX-1393 involves binding to the GlyT1 transporter, thereby increasing the synaptic concentration of glycine. This elevation in glycine levels enhances NMDA receptor function, which is crucial for synaptic plasticity, learning, and memory.</p>