x
This LabTrove instance has just been upgraded to 2.3, to see what new check out the documentation, http://www.labtrove.org/documentation/
This Post
PermalinkURI
URI Label
Revisions
Export:
XML
Archives
- May 2013 (1)
- April 2013 (1)
- February 2013 (2)
- January 2013 (1)
- December 2012 (2)
- November 2012 (1)
- October 2012 (2)
- July 2012 (2)
- May 2012 (4)
- April 2012 (2)
- March 2012 (2)
- January 2012 (3)
Authors
Sections
- 3D7 IC50 Avery Lab (3)
- Biology (19)
- GSH-EE - Chapman Lab (1)
Tools
Show/Hide QR CodeShow/Hide Keys
Frozen plasma samples collected from in vivo plasmodium berghei were assayed for quantity of PMY 10-6 at 1, 4 and 24 hours.
PMY 10-6 has a 3D7 IC50 of 0.4-0.8 μM, therefore ineffective plasma concentrations are reached in under 4 hours.
Data:
See also:
In vivo Plasmodium Berghei mouse trial of initial leads
Human and Mouse Plasma Stability of OSM-S-5/PMY 10-6
Synthesis of TCMDC-123812 via acid chloride (PMY 10-6)
InChi:
InChI=1S/C15H15FN2O3/c1-9-7-13(15(20)21-8-14(17)19)10(2)18(9)12-5-3-11(16)4-6-12/h3-7H,8H2,1-2H3,(H2,17,19)
| Time, h | concentration, ng/mL |
| 1 | 583 |
| 4 | 44.9 |
| 24 | <5.00 |
PMY 10-6 has a 3D7 IC50 of 0.4-0.8 μM, therefore ineffective plasma concentrations are reached in under 4 hours.
Data:
data
See also:
In vivo Plasmodium Berghei mouse trial of initial leads
Human and Mouse Plasma Stability of OSM-S-5/PMY 10-6
Synthesis of TCMDC-123812 via acid chloride (PMY 10-6)
InChi:
InChI=1S/C15H15FN2O3/c1-9-7-13(15(20)21-8-14(17)19)10(2)18(9)12-5-3-11(16)4-6-12/h3-7H,8H2,1-2H3,(H2,17,19)
Linked Posts
This post is linked by:
Attached Files
data
Original data provided by Paul Willis. Numbers in black are the data provided by the analysis. The number in blue is Paul Willis' calculation of the plasma levels (uM). The compounds profile maintains plasma levels above the EC50 for short periods of time (<4 hrs) so this is a likely cause of the lack of in vivo efficacy.
Paul Ylioja email comments: This ties in well with the observed metabolism in mouse plasma (http://malaria.ourexperiment.org/uri/115). 0.2 uM after 4 hours is on the limit of any effect for this compound anyway (3D7 IC50 375-818 nM). Still interesting to see the compound in the blood!
Paul Ylioja email comments: This ties in well with the observed metabolism in mouse plasma (http://malaria.ourexperiment.org/uri/115). 0.2 uM after 4 hours is on the limit of any effect for this compound anyway (3D7 IC50 375-818 nM). Still interesting to see the compound in the blood!