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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
99 Results for "
spatial
" in MedChemExpress (MCE) Product Catalog:
Products (99)
99 Results for "spatial" in MCE Product Catalog:
Cat. No.: HY-116488
CAS No.: 1778682-59-9
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IND8 is a α7 nAChR activator and cognitive enhancer. IND8 mediates cognitive enhancement by activating α7 nAChR . IND8 improves spatial working memory, episodic short-term memory and spatial long-term memory in amnesic mice induced by Scopolamine (HY-N0296). IND8 improves memory function in mice with delayed natural memory decline. IND8 can be used in research related to Alzheimer's disease .
Cat. No.: HY-100406R
CAS No.: 150145-89-4
Synonyms: (+)-MCPG (Standard)
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(S)-MCPG (Standard) is the analytical standard of (S)-MCPG (HY-100406). This product is intended for research and analytical applications. (S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371) . (S)-MCPG can be used for the study of the function of mGluRs in spatial learning .
Cat. No.: HY-14314
CAS No.: 147402-53-7
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ABT-418 is a selective neuronal nicotinic acetylcholine receptor ligand with activity in improving spatial memory. ABT-418 administered before training can significantly reduce the spatial discrimination deficit caused by ventricular damage. ABT-418 is considered to be a potential treatment for attention deficit disorder .
Cat. No.: HY-189013
CAS No.: 832082-44-7
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THRX160209 is a dual-site antagonist of the M2 muscarinic acetylcholine receptor with M2 receptor subtype selectivity. THRX160209 binds simultaneously to the orthosteric site and a spatially distinct allosteric site, competitively inhibiting receptor activation at the acetylcholine binding pocket. THRX160209 exhibits affinity for all five muscarinic receptor subtypes. THRX160209 can be used in research related to neurological disorders .
Cat. No.: HY-P11629
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Neurological Disease Metabolic Disease Inflammation/Immunology
Cat. No.: HY-168731
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AChE/BChE-IN-25 (Compound 6e) is the orally active inhibitor for hAChE and eqBChE with IC50 of 7.9 nM and 0.79 nM. AChE/BChE-IN-25 exhibits antioxidant activity, that scavenges free radical with IC50 of 22.91 μM. AChE/BChE-IN-25 exhibits neuroprotective effects by reducing mitochondrial and cellular oxidative stress in the Drosophila Alzheimer's disease model. AChE/BChE-IN-25 ameliorates Scopolamine (HY-N0296)-induced spatial and cognitive memory impairment in mouse model .
Cat. No.: HY-186284
CAS No.: 2245952-60-5
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EGX358 is a selective, orally active estrogen receptor β (ERβ) agonist with an EC50 of 27.4 nM for ERβ. EGX358 enhances object recognition ability, spatial memory and memory consolidation, and attenuates drug-induced vasomotor responses. EGX358 alleviates partial uterine atrophy without inducing uterine hypertrophy, while it does not alter anxiety-like behavior, depression-like behavior or body weight. EGX358 can be used in research related to Alzheimer's disease and menopause .
Cat. No.: HY-182786
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MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC50 values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease .
Cat. No.: HY-187155
CAS No.: 158778-21-3
Cat. No.: HY-124329AS
CAS No.: 910292-87-4
Cat. No.: HY-183325
CAS No.: 1434867-98-7
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FTO-IN-17 is an orally active and brain-penetrant FTO (m6A RNA demethylase) inhibitor with an IC50 of 1.1 μM. FTO-IN-17 stably binds the FTO catalytic pocket. FTO-IN-17 protects against Aβ1-42-induced toxicity while increasing global m6A levels and dampening pro-inflammatory gene (CXCL10, TNF-α) expression. FTO-IN-17 ameliorates anxiety-like behavior and rescues hippocampal-dependent spatial, recognition memory and neuroinflammation in Alzheimer's disease mice models .
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Cat. No.: HY-184761
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Keap1-Nrf2-IN-30 is an orally active, blood-brain barrier-permeable Keap1-Nrf2 protein-protein interaction inhibitor with a Keap1 Kd value of 157 nM. Keap1-Nrf2-IN-30 selectively inhibits the Keap1-Nrf2 protein-protein interaction, promotes Nrf2 nuclear translocation, suppresses induced ferroptosis, reduces the expression of Aβ and p-Tau, and upregulates the expression of GPX4 and SLC7A11. Keap1-Nrf2-IN-30 upregulates the expression of HO-1 and NQO1, alleviates neuronal damage, and improves cognitive and spatial memory deficits. Keap1-Nrf2-IN-30 can be used in the research of Alzheimer's disease .
Cat. No.: HY-L041
468 compounds
Macrocycles, molecules containing 12-membered or larger rings, are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, showing favorable ADME- and PK-properties. Macrocycles have demonstrated repeated success when addressing targets that have proved to be highly challenging for standard small-molecule drug discovery, especially in modulating macromolecular processes such as protein–protein interactions (PPI). Otherwise, the size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity.
MCE offers a unique collection of 468 macrocyclic compounds which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE Macrocyclic Compound Library is a useful tool for discovering new drugs, especially for “undruggable” targets and protein–protein interactions.
Cat. No.: HY-103430B
CAS No.: 164265-49-0
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SKF-83566 hydrochloride is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 hydrochloride modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 hydrochloride acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 hydrochloride competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 hydrochloride is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-176036A
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MS1262 TFA is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC50 of 19 nM and a Kd of 74 nM against G9a, and an IC50 of 6 nM and a Kd of 19 nM against GLP. MS1262 TFA reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 TFA restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 TFA reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 TFA reduces the risk of thrombus rupture. MS1262 TFA can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer .
Cat. No.: HY-103430AR
CAS No.: 99295-33-7
SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-L170
258 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 258 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
Cat. No.: HY-L944
11028 compounds
MCE 18 stands for Medicinal Chemistry Evolution 2018. This metric was established based on structural data of 28,161 patented lead molecules, 1,370 marketed innovative drugs, and nearly 30,000 investigational candidates from preclinical to Phase III stages across 23 major global pharmaceutical companies from 1950 to 2018. After scaffold clustering analysis, a scoring model was constructed by integrating five three dimensional scaffold characteristics, including aromatic rings (AR), non aromatic heterocycles (NAR), chiral centers (CHIRAL), spirocycles (SPIRO), and the sp³ carbon ratio in cyclic and acyclic moieties, enabling quantitative assessment of molecular scaffold novelty and three dimensional complexity.
According to the score distribution of patented molecules, the top 25% of the original patent dataset was defined as the high novelty region. MCE 18 high scoring compounds selected based on this criterion can effectively avoid scaffold patent conflicts and intellectual property risks from the source. Molecules in this range typically feature a high sp³ carbon ratio, abundant chiral centers, spirocycles, and fused heterocycles with prominent three dimensional conformations. Their spatial properties allow precise matching to complex non traditional undruggable target pockets such as PPI interfaces and allosteric sites, making them ideal structural types for early stage screening of First in class drugs.
MCE‑18 Novelty Focused drug‑Like library strictly selects molecules from the aforementioned high scoring range, containing more than 10,000 premium drug like molecules with highly diverse scaffolds and rich 3D diversity. It can be used for high throughput screening of well established targets such as kinases, GPCRs, and proteases, and is especially suitable for hit identification in allosteric modulation, protein–protein interactions, and various undruggable orphan targets, fully supporting early stage drug discovery for cutting edge innovat
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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
