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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 150881-27-9
- Formule: C40H36N6O4
- Masse moléculaire:664.77
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform Endogenous Metabolite
MoreVoir tous les produits spécifiques à Isoform Calcium Channel
More
Activité biologique
|
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
-
CAS No. 150881-27-9
-
Masse moléculaire 664.77
-
Formule C40H36N6O4
-
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]
-
Structure Classification
-
Initial Source
Aspergillus Species
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WIN-64821 Related Classifications
HY-N9554 Related Classifications
Powered by Bioz