radiolabeled

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

D-Lysine is the D-isomer of L-Lysine, prepared by chemical racemization and microbial asymmetric degradation of L-Lysine.D-Lysine reduces renal uptake of radiolabeled peptides and decreases nephrotoxicity.

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).

PSMA-D5 exhibits a binding affinity for PSMA with a Ki of 0.21 nM and becomes useful for PSMA tracing following radiolabeling. When marked with [68Ga], PSMA-D5 contains a DOTA chelator, facilitating the convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. Additionally, [68Ga]-labeled PSMA-D5 demonstrates exceptional pharmacokinetic properties and significant tumor uptake in 22Rv1 tumors. This compound can be employed in the synthesis and research of radiolabeled conjugates (RDC).

Martinostat is an HDAC inhibitor that can be radiolabeled for quantitative imaging of HDACs within the central nervous system and major peripheral organs.

AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.

PB94 is a selective inhibitor of HDAC11 with an IC50 value of 108 nM. This compound can be radiolabeled as [11C]-PB94 for use in positron emission tomography (PET) to study brain uptake and metabolic characteristics in living animals. Furthermore, PB94 has been shown to alleviate neuropathic pain in mice and is applicable for research into neurological indications.

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

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).

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.

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.

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.

OncoFAP acetate is the highest-affinity small organic fibroblast activation protein (FAP) ligand reported to date, exhibiting a dissociation constant of 680 pM as measured by fluorescence polarization. OncoFAP derivatives, when administered intravenously in both fluorescent and radiolabeled forms, selectively accumulate in FAP-positive tumors while sparing normal tissues, enabling OncoFAP acetate to serve as modular components for targeted therapeutic delivery of radionuclides, CAR-T cells, or cytotoxic agents in oncology studies.

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.

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].

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.

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.

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.

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

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).

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].

ω-Conotoxin MVIIC TFA is a peptide and neurotoxin with 26 residues that preferentially blocks P-type and Q-type Ca ++ currents by binding with high affinity to voltage-sensitive neuronal Ca ++ channels (VGCCs) and can be radiolabeled and used in immunoprecipitation assays.

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].

Rosopatamab is a humanized monoclonal antibody targeting prostate-specific membrane antigen (PSMA) for the treatment of prostate cancer. It can be conjugated with radiolabeled isotopes (e.g., 177Lu) via DOTA-NHS ester to form radiopharmaceuticals for targeted therapy. In preclinical studies, 177Lu-DOTA-Rosopatamab combined with the DNA-PK inhibitor Peposertib achieved a 75% complete response rate in prostate cancer mouse models.