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[1].
Product Specifications
CAS Number
255049-08-2
UNSPSC
12352005
Target
Neurokinin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Field of Research
Endocrinology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/zd6021.html
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
Molecular Formula
C35H35Cl2N3O2S
Molecular Weight
632.64
References & Citations
[1]Bernstein PR, et al. Discovery of novel, orally active dual NK1/NK2 antagonists. Bioorg Med Chem Lett. 2001 Oct 22;11 (20) :2769-73.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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