Posted here due to the comparisons.
A question about data: Your scientists developed a cmpd for diabetes Dapagliflozin (Diabetes 2008 57 1723-1729). In this paper data are presented for hSGLT1 and hSGLT2 inhibition. Lexicon has a compound in developement LX4211 and have presented data (J Med Chem 2009 52 6201-6204).
Cmpd .................hSGLT2.............hSGL1...........ratio IC50
........................IC50 (nM) .........IC50 (nM).....hSGLT1/hSGLT2
Dapagliflozin..ref 1..1.1...................1320...............1200
..................ref 2..4.8.....................810................169
LX4211.........ref 2..14....................1900................134
.................. ref 3..18.....................363..................20
ref 1 Diabetes 57 1723 2008
ref 2 J Med Chem 2009 "The published selectivity of dapagliflozin for hSGLT1/hSGLT2 is 1200-fold (PCT Int. Appl. WO2002053573, 2002.). However, in our assays, we observed a 169-fold selectivity for hSGLT2.
ref 3 www.lexicon-genetics.com/images/pdfs/LX4211_ADA_2010_poster.pdf
I can understand not 'exactly duplicating' the absolute numbers but in the direct comparison BMS compound is a 'bit' more potent and a 'bit' more selective. Ref 3 is a poster with seemingly interesting results. The data for their own compound is different and they do not directly compare both - only citing published data for Dapagliflozin. When does Selective become a Non-selective? 1000:1 10:1 2:1 ???
Look at the edit history of the wiki page
http://en.wikipedia.org/w/index.php?title=Lexicon_Pharmaceuticals&diff=prev&oldid=374319798
http://en.wikipedia.org/w/index.php?title=Lexicon_Pharmaceuticals&diff=next&oldid=374319798
The question is- DATA
http://ethicsessays.blogspot.com/2006/01/truth-about-lying.html
A question about data: Your scientists developed a cmpd for diabetes Dapagliflozin (Diabetes 2008 57 1723-1729). In this paper data are presented for hSGLT1 and hSGLT2 inhibition. Lexicon has a compound in developement LX4211 and have presented data (J Med Chem 2009 52 6201-6204).
Cmpd .................hSGLT2.............hSGL1...........ratio IC50
........................IC50 (nM) .........IC50 (nM).....hSGLT1/hSGLT2
Dapagliflozin..ref 1..1.1...................1320...............1200
..................ref 2..4.8.....................810................169
LX4211.........ref 2..14....................1900................134
.................. ref 3..18.....................363..................20
ref 1 Diabetes 57 1723 2008
ref 2 J Med Chem 2009 "The published selectivity of dapagliflozin for hSGLT1/hSGLT2 is 1200-fold (PCT Int. Appl. WO2002053573, 2002.). However, in our assays, we observed a 169-fold selectivity for hSGLT2.
ref 3 www.lexicon-genetics.com/images/pdfs/LX4211_ADA_2010_poster.pdf
I can understand not 'exactly duplicating' the absolute numbers but in the direct comparison BMS compound is a 'bit' more potent and a 'bit' more selective. Ref 3 is a poster with seemingly interesting results. The data for their own compound is different and they do not directly compare both - only citing published data for Dapagliflozin. When does Selective become a Non-selective? 1000:1 10:1 2:1 ???
Look at the edit history of the wiki page
http://en.wikipedia.org/w/index.php?title=Lexicon_Pharmaceuticals&diff=prev&oldid=374319798
http://en.wikipedia.org/w/index.php?title=Lexicon_Pharmaceuticals&diff=next&oldid=374319798
The question is- DATA
http://ethicsessays.blogspot.com/2006/01/truth-about-lying.html