DDD01510706 has activity against Cryptosporidium both in vitro and in vivo. Data above from Baragana B, et al. Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proc Natl Acad Sci U S A 116, 7015-7020 (2019).
In vitro: We recommend dissovling in 100% DMSO at 10 mM for a working stock.
In vivo: Mice (IFN-gamma knockous) are treated once daily for 7 days with 20 mg/kg (prepared in 0.5% hydroxypropylmethylcellulose, 0.4% Tween 80 and 0.5% benzyl alcohol (v/v)). Toxicity may be observed at doses higher than this.
Experimentally determined values:
PfKRS1 IC50 0.015 µM
CpKRS1 IC50 0.13 µM
Nluc Cp EC50 2.5 µM
HsKRS IC50 1.8 µM
HepG2 EC50 49 µM
MLM CLi 1ml/min/g
CHI-logD 1.7 (clogP 2.4)
MW = 355.31. g/mol
Terms of providing access to DDD01510706:
You may request 25 mg for in vitro work and 100 mg for in vivo work through the MRC PPU reagents and services every year for the cost of shipping.
At Dundee, we have the ability to scale up synthesis of DDD01510706 and produce a larger amount if requested. We are willing to offer this at a competitive price (compared to commercial suppliers). We suggest you first request smaller amounts of compound and validate that it works for you before enquiring about a larger scale synthesis.
If you are interested in larger scale synthesis, contact Dr. Mattie Pawlowic (firstname.lastname@example.org) to discuss further.