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DNDI-6174

Chemical Structure : DNDI-6174

CAS No.: 2868298-43-3

DNDI-6174 (DNDI-0003366174, DNDI 6174)

Catalog No.: PC-21550Not For Human Use, Lab Use Only.

DNDI-6174 is a highly potent inhibitor of Leishmania cytochrome bc1 complex activity, shows broad activity against a panel of representative visceral leishmaniasis clinical isolates from various sources (EC50=10-360 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    DNDI-6174 is a highly potent inhibitor of Leishmania cytochrome bc1 complex activity, shows broad activity against a panel of representative visceral leishmaniasis clinical isolates from various sources (EC50=10-360 nM).
    DNDI-6174 is active against clones resistant to currently used therapeutics, such as paromomycin (PM) and miltefosine (MIL).
    DNDI-6174 shows high potency against T. cruzi (Tulahuen strain, EC50 value of <5 nM), the causative agent of Chagas disease, considerably less active against T. brucei brucei and T. brucei rhodesiense (bloodstream form) associated with human African trypanosomiasis, with EC50 values ranging from 5 to 20 μM.
    DNDI-6174 targets the Qi site of L donovani cytochrome b.
    DNDI-6174 is a potent inhibitor of complex III in lysates prepared from both promastigote and axenic amastigote stages of L. donovani with IC50 of 8 nM and 2 nM respectively.
    DNDI-6174 shows potent in vitro antileishmanial activity against a range of Leishmania species responsible for causing VL or CL and current drug-resistant species and clinical isolates.
    DNDI-6174 (12.5 mg/kg twice daily or 25 mg/kg once daily) decreased the liver parasite burden of infected BALB/c mice.

    Physicochemical Properties

    M.Wt 307.31
    Formula C16H13N5O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    7-(2-amino-4,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzo[d][1,3]dioxole-4-carbonitrile

    References

    1. Stéphanie Braillard, et al. Sci Transl Med. 2023 Dec 13;15(726):eadh9902.

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