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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
21 Results for "
channels isoforms
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "channels isoforms" in MCE Product Catalog:
11
11 Publications Verification
Cat. No.: HY-N6778
CAS No.: 57186-25-1
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2 Cited Publications
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OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation .
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1 Cited Publications
Synonyms: NBI-921352; XEN901
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Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .
Synonyms: 5,6-EET; (±)5,6-EpETrE
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5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
Cat. No.: HY-P5174
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Cat. No.: HY-W074537
CAS No.: 460346-02-5
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P7-2104 is a blood-brain barrier-permeable, selective PDE7A inhibitor with an IC50 of 31 nM. P7-2104 shows selectivity for hERG channels and most CYP450 subtypes. P7-2104 can be used for PDE7-targeted PET neuroimaging studies and research related to neurodegenerative diseases, when labeled with 11C or 18F .
Cat. No.: HY-120078
CAS No.: 1845753-81-2
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AZD2716 is an orally active secretory phospholipase A2 (sPLA2) inhibitor. AZD2716 inhibits human GIIA sPLA2 (IC50=10 nM), human GV sPLA2 (IC50=40 nM), human GX sPLA2 (IC50=400 nM), snake venom sPLA2 (IC50=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (Kd=110 μM). AZD2716 inhibits sPLA2 isoforms IIa, V, X, snake venom sPLA2s, and snake venom Lys49-PLA2-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming .
Cat. No.: HY-123825
CAS No.: 1432913-36-4
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GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 of 0.1 nM at -40 mV .
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BI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
Cat. No.: HY-P1219
CAS No.: 925463-91-8
Synonyms: β-TRTX-Cj1α
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Cat. No.: HY-108043
CAS No.: 875647-81-7
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AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki of 0.49 and 0.75 nM and EC50 of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .
Cat. No.: HY-12946A
CAS No.: 1198784-97-2
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BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
Cat. No.: HY-P5771
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Cat. No.: HY-124906
CAS No.: 1001019-46-0
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JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .
Cat. No.: HY-130309
CAS No.: 851378-93-3
Synonyms: (±)8,9-EEQ; (±)8,9-epoxy Eicosatetraenoic acid
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Eicosapentaenoic acid (EPA) is converted to epoxyeicosatetraenoic acids (EpETEs) by several cytochrome P450 isoforms. The major product of this epoxygenase pathway, (±)17(18)-EpETE, relaxes vascular and airway smooth muscle by activating large conductance Ca 2+-activated K + (BKCa) channels by directly interacting with BKα channel subunits. (±)8(9)-EpETE is an epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo.
Cat. No.: HY-118030
CAS No.: 1257116-00-9
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RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
Cat. No.: HY-169367
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ERD-1233 is an orally active ERα PROTAC degrader with a DC50 of 0.9 nM. ERD-1233 exhibits plasma stability and microsomal stability across multiple species, and shows no significant inhibitory effect on major cytochrome P450 subtypes and hERG channels. ERD-1233 inhibits tumor growth and degrades ERα protein levels in xenograft tumor models, with favorable biosafety. ERD-1233 can be used in breast cancer-related research .
Cat. No.: HY-L099
2,297 compounds
MCE Targeted Diversity Library contains 2,297 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.
Cat. No.: HY-135746S
Cat. No.: HY-183606
Mycobacterium tuberculosis-IN-9 is an orally active Mycobacterium tuberculosis BioA inhibitor with a Ki value of 0.2 nM. Mycobacterium tuberculosis-IN-9 targets the biotin biosynthesis pathway. Mycobacterium tuberculosis-IN-9 inhibits the growth of Mycobacterium tuberculosis in mouse models and is effective against both drug-sensitive and drug-resistant strains. Mycobacterium tuberculosis-IN-9 can be used for the research of tuberculosis .
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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
