radiolabeled

Isoxaben (EL 107) is a specific inhibitor of cell wall biosynthesis, often used as a herbicide, that inhibits the incorporation of radiolabeled glucose into acid-insoluble cell wall fractions.

Satoreotide (JR11) is an SSTR2 antagonist, typically conjugated with radiolabeled chelators for use in neuroendocrine tumor imaging [1].

Fet F-18 is an amino acid analog radiolabeled with fluorine F-18, a positron-emitting isotope, can be used as a tracer in positron emission tomography (PET).

Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.

Dotanoc is a ligand to make gallium Ga 68-DOTANOC, which is a gallium Ga 68-radiolabeled analog of somatostatin.

DOTA-JR11, a somatostatin receptor 2 (SSTR2) antagonist, can be radiolabeled with 68Ga and is used for paired imaging in neuroendocrine tumor (NET) studies [1].

L-689560 is widely used as a radiolabeled ligand in binding studies and used to study the roles of NMDA receptors in normal neurological processes as well as in diseases. At the GluN1 glycine binding site, L-689560 is an effective N-methyl-D-aspartate (NM

BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. BMY 42393 competed for radiolabeled iloprost and PGE1 binding to platelet membranes (IC50; 170 nM and 130 nM, respectively).

Cornigerine is a natural product analog of colchicine produced by Colchicum cornigerum that inhibited tubulin polymerization both with and without microtubule-associated proteins, inhibited the binding of radiolabeled colchicine to tubulin, and stimulated tubulin-dependent GTP hydrolysis.

GR65630 is an effective and selective antagonist of the 5-hydroxytryptamine (5-HT) type 3 receptor. It is utilized to investigate the expression patterns of 5-HT3 receptors across various brain regions and their potential functions in the central nervous system. Additionally, GR65630 and its radiolabeled form [3H]GR65630 are employed in studies examining receptor distribution, density, and affinity.

THK-5105, an arylquinoline derivative, demonstrates high binding affinity for tau fibrils, protein aggregates, and tau-rich Alzheimer's disease (AD) brain homogenates, indicating its potential as a tau imaging PET (Positron Emission Tomography) probe with the radiolabeled version, 18F-THK-5105 [1].

Icapamespib, also known as PU-HZ 151, is a heat shock protein 90 (HSP90) inhibitor. PU-HZ151 showed EC50 of 5 nM in the FP assay as compared to 11 nM for PU-H71 and a logD of 2.37 as compared to 1.21 for PU-H71. PU-HZ151 and radiolabeled PU-HZ151 showed selectivity for epichaperomes over the individual chaperome members. Icapamespib demonstrated the ability to productively engage the target in cells, mice, and humans.

NODAGA-LM3 TFA, a SSTR2 antagonist, can be radiolabeled with ^68Ga for PET imaging applications, particularly in the visualization of SSTR-positive paragangliomas [1] [2].

WL12 is a peptide that targets and binds specifically to programmed death ligand 1 (PD-L1). It can be radiolabeled with various radionuclides to produce radiotracers, enabling the evaluation of PD-L1 expression in tumors [1].

JTE-013 is an effective and specific antagonist of S1P2. JTE-013 suppresses the specific binding of radiolabeled S1P to human and rat S1P2 (IC50s: 17 nM and 22 nM, respectively).

2-Bromoestradiol, an estrogen 2-hydroxylase inhibitor, reduces the irreversible binding of radiolabeled estradiol metabolite(s) to microsomal proteins [1].

Gemcitabine triphosphate (dFdCTP), alongside its counterpart, the active diphosphate (dFdCDP), represents one of the two primary nucleoside metabolites of Gemcitabine within cellular structures. It serves as a benchmark in radiolabeled probe imaging investigations aimed at pinpointing tumors responsive to Gemcitabine. Furthermore, it is instrumental in assessing the compound's absorption and retention by cells [1] [2].

Asem F-18 is a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET .

MK-6884, a positive allosteric modulator (PAM) of M4 muscarinic receptors, exhibits a high affinity (Ki = 0.19 nM). It is a valuable compound for the investigation of neurodegenerative diseases. Additionally, MK-6884 can be efficiently radiolabeled with carbon-11, enabling its use as a PET imaging agent.

2,3-dinor-11β-Prostaglandin F2α (2,3-dinor-11β-PGF2α) was recovered from the urine of both normal monkeys and humans when infused with radiolabeled PGD2, where it represented approximately 1% and 4% of the infused radiolabeled dose, respectively. 2,3-dinor-11β-PGF2α has also been recovered from the urine of mastocytosis patients, where it is excreted in large amounts. In human asthmatic patients, 2,3-dinor-11β-PGF2α represents about 40% (as determined by GC/MS) of the immunoreactive 11β-PGF2α when measured using 's 11β-PGF2α EIA Kit . The excretion rate for 2,3-dinor-11β-PGF2α is approximately 200-250 ng/24 hours in a normal adult.

Iobenguane I 131 is a guanidine analog with specific affinity for tissues of the sympathetic nervous system and related tumors. The radiolabeled forms are used as antineoplastic agents and radioactive imaging agents. MIBG serves as a neuron-blocking agent which has a strong affinity for, and retention in, the adrenal medulla and also inhibits ADP-ribosyltransferase.

CCR4 antagonist 3-1 is a less active chemokine receptor 4 (CCR4) antagonist that inhibits [125I]TARC (thymus and activation-regulated chemokine) with an IC50 value of 1.7 μM. CCR4 antagonist 3-1 inhibits the binding of radiolabeled [125I]TARC and macrophage-derived chemokine ( MDC) to CEM cell surface and inhibits TARC-mediated CEM cell migration in vitro with an IC50 value of 6.4 μM. CCR4 antagonist 3 inhibited the binding of radiolabeled [125I]TARC and macrophage-derived chemokine (MDC) to the CCR4 receptor on the surface of CEM cells and inhibited TARC-mediated migration of CEM cells in vitro with an IC50 value of 6.4 μM.