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31st July 2012 @ 03:11
Frozen plasma samples collected from in vivo plasmodium berghei were assayed for quantity of PMY 10-6 at 1, 4 and 24 hours.


Time, hconcentration, ng/mL
1583
444.9
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)
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Comments
Re: Pharmacokinetics of OSM-S-5/TCMDC-123812/PMY 10-6 by Matthew Todd
12th May 2013 @ 04:18
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!