2944 Results for "

Channel

" in MedChemExpress (MCE) Product Catalog:
Products (2944)

2944 Results for "Channel" in MCE Product Catalog:

Cat. No.: HY-30234S
CAS No.: 1251554-64-9
Clemizole-d4 is the deuterated-labeled Clemizole (HY-30234). Clemizole is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C .
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Cat. No.: HY-L109
826 compounds

Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs.

However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.

With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 826 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

Cat. No.: HY-L950
2,787 compounds

Seven-membered rings are privileged medium-sized scaffolds with distinct twist-chair conformations and greater 3D diversity than five- and six-membered rings. Their flexible conformations allow induced-fit protein binding and precise pharmacophore positioning. They also modulate Fsp³, pKa and logP to enhance solubility and permeability. Azepanes, oxepanes and benzodiazepines serve as bioisosteres for hit discovery against GPCRs, ion channels and kinases.

Widely found in plant and microbial alkaloids, seven-membered heterocycles show excellent biocompatibility and target affinity. They underpin many approved drugs for CNS, cancer and infectious diseases, including diazepam, imipramine and carbamazepine. Clinical candidates further highlight their unique value. However, high transannular strain and synthetic difficulty limit their availability, leaving them rare in standard screening libraries.

MCE 7 Membered Scaffold Library contains 2,792 structurally diverse, lead-like molecules covering azepanes, oxepanes, benzodiazepines and dibenzazepines. With varied substitutions, chiral centers and synthetic accessibility, it fills the shortage of medium-ring scaffolds. Ideal for HTS, virtual screening and SAR studies, these novel, patent-clear compounds offer a distinctive starting point for drug discovery in CNS disorders, oncology, antivirals and challenging targets such as PPIs.

Cat. No.: HY-D3133
CAS No.: 2410296-16-9
Target:  

Fluorescent Dye

Research Areas:  

Others

HS-CyBz is a Fluorescent probe for H₂S detection, enabling ratiometric optical/photoacoustic dual-modality in/ex vivo imaging. Its detection mechanism relies on nucleophilic substitution of its benzoic ester group by HS⁻, which releases an enolic meso-hydroxyltricarboheptamethine cyanine that then undergoes keto-enol tautomerization to form Cy-ketone; this tautomerization causes distinct shifts in absorption and emission spectra, producing a ratiometric response that reduces interferences from tissue scattering, autofluorescence, and probe concentration. In its initial state, HS-CyBz has an excitation wavelength of 595 nm, with emission bands centered at 805 nm (main) and 630 nm (minor); upon reaction with H₂S, the 805 nm emission band decreases while the 630 nm band drastically increases, and its absorption spectrum shows a sharp band at 775 nm and a shoulder band at 708 nm, which decrease upon H₂S reaction with a minor increase at 850 nm and an isosbestic point at 825 nm. For in vivo optical imaging, excitation at 560 nm is used with emission channels at 620 nm and 790 nm, while in vivo photoacoustic imaging uses excitation at 775 nm and 825 nm. The detection limit of HS-CyBz for H₂S is 0.5 μM, and it shows high selectivity, with only H₂S inducing a distinct enhancement of the emission ratio F₆₃₀/F₈₀₅ and PA ratio PA₈₂₅/PA₇₇₅, while other biochemical species including cations, anions, reactive oxygen species, biothiols, and carboxylesterase trigger only minor changes and do not interfere with H₂S sensing. Tail intravenous injection of HS-CyBz leads to accumulation in the liver of mice, and it can be used to verify endogenous H₂S upregulation triggered by S-adenosyl-L-methionine via ratiometric optical/photoacoustic imaging .
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