trα

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.

Liothyronine (Tresitope) is a synthetic and highly active thyroid hormone that acts as an effective agonist of TRα and TRβ (Ki = 2.33 nM for both hTRα and hTRβ). It activates the TRβ1 receptor, promotes the metabolism of carbohydrates, proteins, and fats, accelerates the oxidative processes in tissue cells, maintains basal metabolic rate, and supports normal growth and development. Liothyronine can be used to induce hyperthyroidism models.

CO23 is a blood-brain barrier penetrant and selective TRα agonist and can be used in studies about the regulation of growth and development.

3,5-Diiodothyropropionic acid (C082182) is a thyroid hormone analog. It induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (Ka: 2.40/M and 4.06/M for TRα1 and TRβ1).

Liothyronine Sodium is the sodium salt form of liothyronine, a synthetic form of the levorotatory isomer of the naturally occurring thyroid hormone triiodothyronine (T3). Liothyronine sodium (3,3',5-Triiodo-L-thyronine sodium) binds to nuclear thyroid receptors which then bind to thyroid hormone response elements of target genes. As a result, liothyronine sodium induces gene expression that is required for normal growth and development. Liothyronine sodium is more potent and has a more rapid action than thyroxine (T4).

TR antagonist 2 (Compound 10a) is a competitive inhibitor of thyroid hormone receptors (TRα/β) with an IC50 of 47 nM. It works by competitively binding to the ligand-binding domain of the receptor with triiodothyronine (T3), thereby blocking the formation of the receptor-coactivator complex, inhibiting target gene transcription, and reducing thyroid hormone-mediated metabolic effects. TR antagonist 2 holds potential for research into hyperthyroidism (such as Graves' disease) and thyrotoxicosis.

Liothyronine sodium hydrate (Triiodothyronine sodium hydrate) is a TRα and TRβ agonist and a thyroxine analog with anticancer and antitumor activities. It can be used to study hypothyroidism, stroke and cognitive dysfunction.

Ganoderic acid TR is a broad-spectrum inhibitor of influenza neuraminidases (NAs), particularly H1N1 and H5N1 neuraminidases, with IC50 values of 4.6 and 10.9 μM, respectively.

Tr-PEG2-OH is a PEG-based PROTAC linker used in PROTAC synthesis[1] and a non-cleavable 2-unit PEG ADC linker for antibody-drug conjugate (ADC) synthesis[2].

Tr-PEG3-OH, a non-cleavable three-unit PEG ADC linker, is used in the synthesis of antibody-drug conjugates (ADCs).

Tr-PEG4-OH is a non-cleavable tetraethylene glycol ADC linker used in ADC synthesis for the conjugation of antibodies and drugs.

Tr-PEG5-OH is a non-cleavable 5-unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs).

Tr-PEG6-OH is a 6-unit polyethylene glycol (PEG) linker, which is non-cleavable and extensively employed in the synthesis of antibody-drug conjugates (ADCs).

Tr-PEG8-OH, a non-cleavable 8-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs).

Methoxy-Tr-NH-PEG7 is a PEG-based linker for PROTACs, joining two essential ligands crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

ONO-TR-772 (VU6018042) is a selective TREK inhibitor with an IC50 of 15 nM. It improves recognition memory in the NOR mouse model induced by MK-801. ONO-TR-772 is useful in research on diseases associated with cognitive impairment.

TR-100 is a small-molecule inhibitor that targets tumor-associated tropomyosin; it specifically binds to the C-terminus of tropomyosin 3.1, thereby disrupting its interaction with actin filaments and compromising cytoskeletal stability. TR-100 selectively affects Tpm3.1-dependent actin filament function in cancer cells while having minimal impact on normal tissues (such as cardiac muscle). It is primarily used to study mechanisms related to tumor cell proliferation, migration, and survival. Additionally, TR-100 inhibits Dynamin-1 with an IC50 value of 10.8 µM.

TR4161 is a prostaglandin bronchodilator of low tracheobronchial irritancy.

TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

TR-107 (Anticancer agent 230) is a selective and potent activator of the mitochondrial protease ClpP that inhibits tumor growth in the MDA-MB-231 xenograft model.

Nucleoside Derivatives –Morpholino nucleosides

3'-NH-Tr-2',3'-ddC(Bz)-5'-CE-Phosphoramidite is a phosphoramidite monomer utilized in the synthesis of nucleic acids, including oligonucleotides.

3'-NH-Tr-2',3'-DMF-ddA-5'-CE-Phosphoramidite serves as a precursor of adenosine nucleotide monomers used in the solid-phase synthesis of oligonucleotides, particularly for modifying oligonucleotides such as terminally modified DNA strands. It features Trityl (Tr), Cyanoethyl (CE), and Dimethylformamidine (DMF) protective groups, classifying it as a ddNTP adenosine nucleoside suitable for applications like oligonucleotide solid-phase synthesis, probe design, and chain termination sequencing.

3'-NH-Tr-2',3'-dT-5'-CE-Phosphoramidite is a specialized phosphoramidite compound used in the synthesis of oligonucleotides and nucleic acid analogs. It plays a role in research focused on antiviral and anticancer applications.