| Identification | Back Directory | [Name]
Butanedioic acid, compd. with 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]-4-quinolinecarboxamide (1:1) | [CAS]
2444781-71-7 | [Synonyms]
Butanedioic acid, compd. with 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]-4-quinolinecarboxamide (1:1) | [Molecular Formula]
C31H37FN4O6 | [MOL File]
2444781-71-7.mol | [Molecular Weight]
580.66 |
| Hazard Information | Back Directory | [Description]
DDD107498 succinate (DDD-498 succinate) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2[1].
EC50: 1 nM (3D7 parasites), 2 nM (WT-PfeEF2)[1] DDD107498 exhibits an ED90 of 0.57 mg/kg after a single oral dose in mice infected with the rodent parasite P. berghei[1]. | [Uses]
Cabamiquine (DDD107498) succinate is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2[1]. | [in vivo]
Cabamiquine (p.o., a single dose) succinate shows an ED90 (90% reduction in parasitaemia) of 0.57 mg/kg in mice infected with the rodent parasiteP. berghei[1].
Cabamiquine (p.o., 3 mg/kg) succinate shows Cmax of 80 ng/mL, Tmax of 4 h, AUC of 200542 ng·min/mL, F (%) of 84%[2].
| [IC 50]
CaMK III; Plasmodium | [References]
[1]. BaragaÑa B, et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20. |
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