227088-94-0 Usage
Uses
A selective P2X7 receptor antagonist.
Biological Activity
Potent and selective human P2X 7 antagonist (K B values are 5 - 7 and > 10,000 nM at hP2X 7 and rP2X 7 respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1 β release in vitro (K B values are 15 and 92 nM respectively).
references
1. stokes l, jiang lh, alcaraz l, et al. characterization of a selective and potent antagonist of human p2x(7) receptors, az11645373. british journal of pharmacology. 2006;149(7):880-887.
Check Digit Verification of cas no
The CAS Registry Mumber 227088-94-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,2,7,0,8 and 8 respectively; the second part has 2 digits, 9 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 227088-94:
(8*2)+(7*2)+(6*7)+(5*0)+(4*8)+(3*8)+(2*9)+(1*4)=150
150 % 10 = 0
So 227088-94-0 is a valid CAS Registry Number.
227088-94-0Relevant articles and documents
Novel P2X7 receptor antagonists.
Alcaraz,Baxter,Bent,Bowers,Braddock,Cladingboel,Donald,Fagura,Furber,Laurent,Lawson,Mortimore,McCormick,Roberts,Robertson
, p. 4043 - 4046 (2007/10/03)
The synthesis and pharmacological evaluation of a new series of potent P2X(7) receptor antagonists is disclosed. The compounds inhibit BzATP-mediated pore formation in THP-1 cells. The distribution of the P2X(7) receptor in inflammatory cells, most notabl