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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
731 Results for "
current
" in MedChemExpress (MCE) Product Catalog:
Products (731)
731 Results for "current" in MCE Product Catalog:
Cat. No.: HY-137325A
CAS No.: 301334-89-4
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2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
Cat. No.: HY-14977
CAS No.: 840523-39-9
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CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
Cat. No.: HY-176036
CAS No.: 3070323-06-4
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MS1262 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 reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 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 reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 reduces the risk of thrombus rupture. MS1262 can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer .
Cat. No.: HY-189470
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Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy .
Cat. No.: HY-46286
CAS No.: 352560-76-0
Synonyms: N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide
Research Areas:
TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn 2+- and H +-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
Cat. No.: HY-P1837
CAS No.: 186302-15-8
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Cat. No.: HY-W100287R
CAS No.: 4532-33-6
Cat. No.: HY-L127
39 compounds
Orthopoxvirus is a genus of viruses in the family Poxviridae and subfamily Chordopoxvirinae. The orthopoxvirus genus consists of 12 viruses including variola virus, vaccinia virus (VV), cowpox viruses (CV), monkeypox virus, and camelpox virus. Smallpox has been eradicated worldwide in 1980, but some other orthopoxvirus, such as monkeypox virus, are still threats to human health.
There are not many drugs available for orthopoxvirus treatment. The only product currently available for treatment of complications of Orthopoxvirus infection is vaccinia immunoglobulin (VIG). In 2021, brincidofovir was approved by FDA for the treatment of smallpox and tecovirimat was approved by EMA for the treatment of monkeypox in 2022. A few active compounds including interferon and interferon inducers, and a variety of nucleosides or nucleotides have been reported to have activity against orthopoxvirus.
MCE carefully prepared a unique collection of 39 compounds reported with the anti- orthopoxvirus activity which can be used for drug screening and other research about orthopoxvirus.
Cat. No.: HY-L153
5,267 compounds
Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.
To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 5,267 compounds with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc.
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PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
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-N2125R
CAS No.: 174972-80-6
Category:
Cat. No.: HY-L925
9,363 compounds
Cysteine proteases (CPs), a key enzyme family regulating physiological metabolism and mediating pathological processes (such as abnormal bone resorption, tumour invasion, and pathogen infection), represent a core therapeutic target for developing specific inhibitors in disease intervention. Currently reported CP inhibitors primarily achieve their inhibitory function by precisely binding to CP active pockets (e.g., S1-S4 non-primed regions or S1'-S2' primed regions) and forming covalent/non-covalent interactions with the active site cysteine residues, providing clear structural references for the development of novel inhibitors.
This compound library, designed based on the core strategy of "similarity-based known active structures", contains over 200 cysteine protease inhibitors. Leveraging AI-driven molecular screening technology, it retains the critical pharmacological and shape features of reported CP inhibitors, serving as a specialized tool for efficiently discovering novel cysteine protease inhibitors.
Cat. No.: HY-L048
585 compounds
The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins, overexpression and changes in drug targets and biofilm formation, emphasizing the importance of discovering new antifungal drugs and therapies. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, such as the combination of antifungal drugs, development of new formulations for antifungal agents and modifications to the chemical structures of traditional antifungals, etc.
MCE offers a unique collection of 585 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
Cat. No.: HY-L102
1,900 compounds
Rare diseases are an important public-health issue and a challenge for the medical community. Most rare diseases are genetic disorders, which are often severely disabling, substantially affect life expectancy, and impair physical and mental abilities. Currently, there are about 7,000 identified rare diseases, together affecting 10% of the population. However, fewer than 6% of all rare diseases have an approved treatment option, highlighting their tremendous unmet needs in drug development. The process of repurposing drugs for new indications, compared with the development of novel orphan drugs, is a time-saving and cost-efficient method resulting in higher success rates, which can therefore drastically reduce the risk of drug development for rare diseases.
MCE carefully collects a unique of 1,900 compounds studied in preclinical, clinical trials or approved used in rare diseases treatment. MCE rare diseases drug library is a useful tool for the research of rare diseases. All compounds can provide corresponding indications for rare diseases.
Cat. No.: HY-L070
1,851 compounds
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases.
MCE offers a unique collection of 1,851 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.
Cat. No.: HY-L156
1,040 compounds
Autoimmune disease is a pathological disease characterized by inflammatory disorders targeting autoantigens. The routine treatment of autoimmune diseases suppresses general immune function to regulate uncontrolled inflammation. The current targeted immunotherapy suppresses the main pro-inflammatory signaling pathways by blocking inflammatory cytokines, cell surface molecules, and intracellular kinases. As key participants in innate immunity, macrophages and dendritic cells (DCs) are crucial for Ag presentation and pro-inflammatory cytokine production, such as TNF and IL-1 β、 IL-6, IL-23, B cell activating factor (BAFF), and the proliferation-inducing ligand (APRIL, also known as TNFSF13A).
MCE designs a unique collection of 1,040 autoimmune disease-related compounds, covering multiple targets and subtypes, such as TNF Receptor, IFNAR, JAK, Btk, TLR, IL-6, IL-17, IL-23, etc. It is a useful tool for screening autoimmune disease drugs.
Cat. No.: HY-184044
CAS No.: 13112-05-5
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P2X2R antagonist-1 (compound 66) is a P2X2 receptor antagonist derived from Reactive Blue 4 (HY-125815). P2X2R antagonist-1 shows high selectivity for P2X4, P2X7, P2Y2, P2Y4, P2Y6 and P2Y12 receptors, moderate selectivity for P2X1 and P2X3 receptors, and exhibits higher potency toward homomeric P2X2 receptors than heteromeric P2X2/3 receptors. P2X2R antagonist-1 competitively inhibits ATP-mediated currents. P2X2R antagonist-1 can be used in research related to pain and urinary incontinence .
Cat. No.: HY-188056
CAS No.: 121714-70-3
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Biotin-11-UTP is a biotinylated uridine triphosphate that can be incorporated into short RNA strands via co-transcription with T7 RNA polymerase, and is used for synthesizing labeling reagents and detection markers. After binding to streptavidin, Biotin-11-UTP generates characteristic downward ionic current peaks during nanopore translocation, which allows the differentiation between modified and unmodified RNA. Biotin-11-UTP enables site-specific labeling of short RNA, and is suitable for single-molecule solid-state nanopore sensing detection. Biotin-11-UTP can serve as a raw material for synthesizing biotinylated single-stranded RNA probes, which is applied to rotavirus nucleic acid detection; it can also label single-stranded RNA probes targeting and immobilizing 28S ribosomal RNA in leukemia cells. Biotin-11-UTP can alter the electrophoretic mobility of transcribed RNA in agarose gels, and can be used to monitor the biotinylation degree of RNA probes .
Cat. No.: HY-L154
3,728 compounds
Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.
To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 3,728 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.
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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
