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. Nr.: 150881-27-9
- Formel: C40H36N6O4
- Molecular Weight:664.77
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
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NK1R 0.24 μM (Ki) |
NK2R 0.26 μM (Ki) |
NK3R 15.2 μM (Ki) |
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.
Chemical Information
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CAS. Nr. 150881-27-9
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Molecular Weight 664.77
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
WIN-64821 Related Classifications
HY-N9554 Related Classifications
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