WIN-64821
WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The Ki values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca2+ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research.
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- CAS No.: 150881-27-9
- Formule: C40H36N6O4
- Masse moléculaire:664.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
NK1R 0.24 μM (Ki) |
NK2R 0.26 μM (Ki) |
NK3R 15.2 μM (Ki) |
In Vitro
WIN 64821 (1-10 μM; 10 minutes) acts as a competitive functional antagonist against substance P (SP)-induced contraction in guinea pig ileal strips, with a pA2 value of 6.6 and a corresponding EC50 of 0.63 μM[1].
WIN 64821 (0.01-10 μM) inhibits substance P-induced 45Ca2+ efflux in human astrocytoma U-373 MG cells, with a mean IC50 value of 0.6 μM; at concentrations of 0.5 and 10 μM, it does not induce 45Ca2+ efflux on its own[1].
WIN 64821 inhibits the NK2 functional model-induced enhancement of twitch in rat vas deferens (an NK2 functional model), with a mean IC50 of 3.4 μM, and shows minimal effect on basal twitch at concentrations up to 30 μM[1].
WIN-64821 is a competitive antagonist of human NK1 receptors in human astrocytoma cells, with a Ki value of 230 nM[2].
WIN-64821 is a competitive antagonist of the human NK1 receptor in normal human fetal tissues, with a Ki value of 0.74 μM[2].
WIN-64821 is a competitive antagonist of the NK1 receptor in guinea pig submandibular gland membrane preparations, with a Ki value of 0.6 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 150881-27-9
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Masse moléculaire 664.77
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Formule C40H36N6O4
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SMILES
O=C1N2[C@@]3([C@@](C=4C(N3)=CC=CC4)(C[C@]2(C(=O)N[C@H]1CC5=CC=CC=C5)[H])[C@@]67[C@@](N8[C@@](C6)(C(=O)N[C@@H](CC9=CC=CC=C9)C8=O)[H])(NC=%10C7=CC=CC%10)[H])[H]
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Structure Classification
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Initial Source
Aspergillus Species
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WIN-64821 Related Classifications
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