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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
202 Results for "
binding properties
" in MedChemExpress (MCE) Product Catalog:
Products (202)
202 Results for "binding properties" in MCE Product Catalog:
Cat. No.: HY-W040176
CAS No.: 799268-45-4
Synonyms: N-Palmitoyl-tyrosine phosphoric acid ammonium
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
N-PTyrosine PA (N-Palmitoyl-tyrosine phosphoric acid) ammonium is a lysophosphatidic acid (LPA) receptor modulator, which exhibits weak inhibitory activity against LPA1 and partial agonist properties towards LPA5. N-PTyrosine PA ammonium inhibits the activation of LPA receptors and downstream responses by competing with agonists for binding sites. N-PTyrosine PA ammonium can induce morphological changes and aggregation, and also inhibit LPA-induced morphological changes through receptor desensitization caused by pre-incubation. N-PTyrosine PA ammonium can be used in the research of related diseases such as atherosclerosis and acute ischemic syndromes (e.g., unstable angina, myocardial infarction, stroke) .
Cat. No.: HY-L0115V
10,091 compounds
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.
Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.
Cat. No.: HY-P992081
Target:
Research Areas:
Cat. No.: HY-L934
122 compounds
CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein.
These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins.
MCE compiles 122 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.
Research Areas:
Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
Synonyms: N-Acetyl-L-serine
Cat. No.: HY-158252S
CAS No.: 1253297-72-1
Synonyms: NO050328-d5 hydrochloride; NO328-d5 hydrochloride; TGB-d5 hydrochloride
Cat. No.: HY-182500A
CAS No.: 3020765-70-9
Target:
Research Areas:
(S,S)-SARM1-IN-9 (Compound MY-13A) is a stereoselective SARM1 inhibitor with covalent binding properties. (S,S)-SARM1-IN-9 covalently modifies Cys311 in the autoregulatory ARM domain of wild-type SARM1, thereby blocking NADase activity, without inhibiting the SARM1 C311A or SARM1 C311S mutants. (S,S)-SARM1-IN-9 blocks vacor- and vincristine-induced axon degeneration in primary rodent dorsal root ganglion neurons. (S,S)-SARM1-IN-9 can be used for research on axon degeneration-dependent neurological disorders, including chemotherapy-induced peripheral neuropathy .
Cat. No.: HY-B1390AR
CAS No.: 128-44-9
Target:
Research Areas:
Saccharin (sodium) (Standard) is the analytical standard of Saccharin (sodium). This product is intended for research and analytical applications. Saccharin sodium is an orally active, non-caloric artificial sweetener (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties. Saccharin binds to and signals via specific taste receptors, not only in the oral cavity but also alongside the gastrointestinal tract. Saccharin has been reported to bind the human and rodent heteromeric guanine nucleotide-binding protein (G protein) coupled sweet taste receptors T1R2/T2R3 as well as the human bitter taste receptor T2R43 and T2R44. Saccharin can inhibit bacterial growth in vitro .
Research Areas:
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly .
Cat. No.: HY-P992449
Synonyms: PRLR ADC antibody
Target:
Research Areas:
Cat. No.: HY-W663179
CAS No.: 681492-17-1
Target:
Research Areas:
DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .
Cat. No.: HY-182685
CAS No.: 2446681-27-0
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Research Areas:
MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC50 of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .
Cat. No.: HY-187618
CAS No.: 1508276-29-6
Target:
Research Areas:
GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx .GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity .GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses .GRC-17536 exhibits antitussive activity .GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study .GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough .
Cat. No.: HY-B0696AR
CAS No.: 145821-59-6
Synonyms: NO050328 hydrochloride (Standard); NO328 hydrochloride (Standard); TGB hydrochloride (Standard)
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Research Areas:
Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
Cat. No.: HY-B0696AS
Synonyms: NO050328-d4 hydrochloride; NO328-d4 hydrochloride; TGB-d4 hydrochloride
Cat. No.: HY-B0696S
CAS No.: 1217672-34-8
Synonyms: NO050328-d6; NO328-d6; TGB-d6
Cat. No.: HY-B0696S1
Synonyms: NO050328-d4; NO328-d4; TGB-d4
Research Areas:
Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
Cat. No.: HY-B2169S2
CAS No.: 1219798-80-7
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
