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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
2944 Results for "
Sodium Channel
" in MedChemExpress (MCE) Product Catalog:
Products (2944)
2944 Results for "Sodium Channel" in MCE Product Catalog:
Cat. No.: HY-183335
Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma .
Cat. No.: HY-189235
CAS No.: 3078735-55-1
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IHCH-8110 is a peripherally restricted, non-brain-penetrant 5-HT2AR and 5-HT2CR agonist (Ki=47.86 nM) that antagonizes 5-HT2BR. IHCH-8110 induces CXCL10 and IL-18 expression by activating 5-HT2AR on enteric glial cells, thereby promoting CD8 + T cell recruitment and effector polarization, and avoids the risk of cardiac valvulopathy associated with 5-HT2BR activation. IHCH-8110 exhibits a low risk of hERG channel inhibition (IC50=5.96 μM) and is well tolerated, sensitizing immunologically cold colorectal cancer to PD-1 blockade therapy, making it suitable for research related to colorectal cancer .
Cat. No.: HY-N0168A
CAS No.: 69097-99-0
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Cat. No.: HY-P1636
CAS No.: 113274-56-9
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Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
Cat. No.: HY-W027553S1
Synonyms: NIK-247-d9 free base
Cat. No.: HY-L211
86 compounds
Hormones are a class of biologically active substances secreted by endocrine gland cells, which are transported through the circulatory system to various parts of the body, and precisely act on specific target organs or cells, playing a crucial role in regulating the growth, development, metabolism, and reproduction of organisms. The mechanisms of hormone action are diverse and complex. Some hormones (such as corticosteroids, vitamin D, and thyroid hormones) can enter the cell interior and interact with receptors in the nucleus, thereby regulating gene expression and affecting cell function. Other hormones (such as growth hormone and thyrotropin-releasing hormone) bind directly to receptors on the cell surface, exerting their effects by regulating enzyme activity or influencing the state of ion channels. Additionally, hormones play a key role in the study of endocrine and metabolic diseases, and are closely related to the development of diseases such as diabetes and thyroid diseases.
MCE has included 86 human hormone compounds, which is of great significance for the study of human metabolic pathways, and can also be used to build a metabonomics database.
Cat. No.: HY-128866
CAS No.: 2332841-25-3
TBAJ-876 is an orally active diarylquinoline anti-Mycobacterium agent. TBAJ-876 regulates energy metabolism by targeting the c and ε subunits of Mycobacterium tuberculosis F-ATP synthase, exerts bactericidal activity against replicating Mycobacterium tuberculosis, and retains activity against strains carrying the Rv0678 mutation. TBAJ-876 undergoes N-demethylation in vivo to form its major active metabolite TBAJ-876-M3, which has lower lipophilicity and hERG potassium channel binding affinity. TBAJ-876 is well tolerated in BALB/c mice and significantly reduces the colony-forming units of Mycobacterium tuberculosis in the lungs. In addition, TBAJ-876 exhibits inhibitory activity against Mycobacterium abscessus, reduces bacterial loads in the lungs and spleens of infected mice, and shows no antagonistic effect when used in combination with common antibiotics. TBAJ-876 can be used in studies related to tuberculosis and Mycobacterium abscessus pulmonary diseases .
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-145491
CAS No.: 578008-43-2
Cat. No.: HY-D3127
CAS No.: 455251-97-5
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DCA-Mln is a Fluorescent probe for ferric iron (Fe³⁺) detection. The probe works via an internal charge transfer (ICT) process from its diethylamino group to its dicyano group, which produces bright pink fluorescence in its unbound state; when Fe³⁺ is present, two molecules of DCA-Mln chelate with one Fe³⁺ ion, with one cyano group of each DCA-Mln participating in the complexation, and this binding triggers a photoinduced electron transfer (PET) process that provides a nonradiative deactivation pathway, resulting in fluorescence quenching; additionally, the probe exhibits a visible color change from purple to peach pink upon Fe³⁺ binding, enabling dual-channel detection. The probe has an excitation wavelength of 570 nm and an emission wavelength of 670 nm, and it shows a rapid response, with fluorescence stabilizing within 15 seconds of Fe³⁺ addition. DCA-Mln is cell-membrane-permeable, nontoxic at the imaging concentration of 10 μM, and can be used for Fe³⁺ detection in actual water samples, Fe³⁺ imaging in living cells, and as an anti-counterfeiting ink[1].
Cat. No.: HY-N0168AR
CAS No.: 69097-99-0
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Cat. No.: HY-N0168AS
CAS No.: 1346605-26-2
Cat. No.: HY-N4267
CAS No.: 13060-14-5
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-182517
CAS No.: 2225980-49-2
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AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus .
Cat. No.: HY-188044
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DC-98-LC74 is a selective modulator of adult skeletal muscle-type nicotinic acetylcholine receptor (α1β1δε), with an EC50 value of 6.5 µM for the human receptor and an IC50 of 13.45 µM for the human α3β4 nicotinic acetylcholine receptor. DC-98-LC74 increases the ligand-free opening probability of the receptor via the ε subunit M2-M3 loop, and prolongs the burst duration and opening probability of wild-type and fast-channel mutant AChR. DC-98-LC74 exerts weak effects on neuronal AChR subtypes and has no agonist activity. DC-98-LC74 prolongs the mouse diaphragm endplate current and improves muscle contractility in isolated neuromuscular preparations from sarcopenic mice. DC-98-LC74 can be used for studies on neuromuscular junction function and myasthenia-related diseases .
Cat. No.: HY-N0168AS1
CAS No.: 2750534-85-9
Cat. No.: HY-L220
91 compounds
Biotoxins, also referred to as natural toxins, are chemical substances produced by plants, animals, or microorganisms that exert toxic effects on other living organisms. Due to unique biological activities, biotoxins have been widely applied in molecular biology, physiology, pharmacology, and the clinical diagnosis and treatment of various human diseases, becoming an important source of natural drug development. Biotoxins can specifically bind to and interfere with intracellular signaling molecules or receptors, thereby altering cellular signaling processes. Leveraging this characteristic, biotoxins can be used to study the regulatory mechanisms of cellular signaling pathways. For example, neurotoxins such as snake venom peptides can be used to investigate the functional regulation of neurotransmitter receptors and ion channels. Additionally, biotoxins have demonstrated significant potential in drug development across various fields, including neurological diseases, cardiovascular diseases, anticoagulation, and anti-cancer therapies. With advancements in high throughput screening, structural optimization, and antibody-toxin conjugation technologies, numerous biotoxins or their structural analogs have been successfully brought to market, such as Ziconotide, Captopril, Bivalirudin, and Eptifibatide.
MCE offers 91 types of biotoxins, including neurotoxins, cardiotoxins, mycotoxins, and more.
Cat. No.: HY-30234B
CAS No.: 17162-20-8
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Infection Neurological Disease Inflammation/Immunology Endocrinology
Clemizole sulfate is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole sulfate 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 sulfate 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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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
