Back to the Top
Dear all
I would like to know the Ketoconazole inhibition potential and Ki values of CYP 2C9 and 1A enzymes .
It will be grateful,if you can send me the reference for the same.
Thank you in advance. I look forward your reply soon.
Best wishes
A.Karthik
Research scholar
MCOPS
Manipal
Back to the Top
Dear Karthik,
Below table may be useful to you.
CYP Substrate Inhibitor Source: yeast Source : Baculovirus
IC50 (uM) IC50 (uM)
1A2 EOMCC Furafylline 2.06 2.01
CEC Furafylline 3.3 3.7
BFC Furafylline 7.2 7.4
3A4 BFC Ketoconazole 0.15 0.15
BOMCC Ketoconazole 0.2584 0.22
DBF Ketoconazole 0.028 0.032
2C9 BOMCC Sulfaphenazole 0.7164 0.6
MFC Sulfaphenazole 0.67 0.41
DBF Sulfaphenazole 0.29 0.3
Thanks and Regards,
K.N.Purna chandra rao
Research Associate
PREMAS Biotech Pvt. Ltd.
Plot No. 77, Sector 4,
IMT Manesar.
Gurgaon-122050Haryana,
[Table best viewed as courier - db]
Back to the Top
The following message was posted to: PharmPK
Do you have corresponding data with rat liver microsomes. In the past we have had significant mismatches with inhibition determined in recombinant vs microsomes origins.
Norman Huebert, Ph.D. Team Leader, ADME J&J PRD 41-2020 P.O. Box 776 Welsh and McKean Rds Spring House, PA 19477
Back to the Top
Dear All
There are lots of variability in the reported Ki values for ketoconazole in the literature, please see the following recent review paper:
Greenblatt DJ, Venkatakrishnan K, Harmatz JS, Parent SJ and von Moltke LL (2010) Sources of variability in ketoconazole inhibition of human cytochrome P450 3A in vitro. Xenobiotica.
Regards
Masoud
Want to post a follow-up message on this topic?
If this link does not work with your browser send a follow-up message to PharmPK@boomer.org with "Ketoconazole inhibition potential" as the subject | Support PharmPK by using the |
Copyright 1995-2011 David W. A. Bourne (david@boomer.org)