255049-08-2
Chemical Structure
ZD6021
- CAS. Nr.: 255049-08-2
- Formula:C35H35Cl2N3O2S
- Molecular Weight:632.64
IUPAC Name: 3-cyano-N-((S)-2-(3,4-dichlorophenyl)-4-(4-(2-((S)-methylsulfinyl)phenyl)piperidin-1-yl)butyl)-N-methyl-1-naphthamide
InChIKey: SJHZTGDJTIZMSK-KPRDSAADSA-N
SMILES: O=C(N(C)C[C@@H](CCN1CCC(CC1)C2=CC=CC=C2[S@](C)=O)C3=CC=C(C(Cl)=C3)Cl)C4=C5C=CC=CC5=CC(C#N)=C4
Biological Activity: ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg[1].
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ZD6021 | ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg. | |||||||||||||||||||||
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