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17th February 2014 @ 05:20

Posted on behalf of Paul Willis

 

One member of the triazolopyrazines (Series 4) (MMV639565) had previously been evaluated in vivo and shown rapid parasite clearance. Data shown here.

Another member of the series (MMV669844) has now been tested in a snapshot (one dose level of 4 x 50 mg/Kg) efficacy SCID study at Swiss TPH. The compound had excellent efficacy as shown in the attached report (>99.9% inhibition of parasitimia) showing this appears a general property of the series.

MMV669844 and MMV639565

MMV669844_SCID.pdf
Attached Files
3rd February 2014 @ 10:59

Data obtained at the outset of Series 4 included potency and PK data, but no formal record of how the data were obtained - i.e. details of assays. Paul Willis wrote on 3rd Feb 2014 by email to provide the following methods:

 

1. Parasite assay - In Vitro EC50 (uM) (Erythrocyte assay - NF54 with 3H-Hypoxanthine at 72hr time point)

 

2. Rat and human liver microsomes - Test compound is incubated with pooled human (or rat) liver microsomes in 100 mM phosphate buffer (pH 7.4) at 37°C in the presence of NADP cofactor. The incubation volume is 0.1 mL. Test compounds are tested at 1 mM.

 

These assays will need to be linked with the data upon upload to ChEMBL following assignment of OSM numbers.

 

Inherited Data on Series 4 Amides

Collected Amides in the TP Series (Triazolopyrazines, Series 4)

A New Triazolopyrazine Series for OSM - Series 4

MMV triazolopyrazine data

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