Cabamiquine


CAS No. : 1469439-69-7

(Synonyms: DDD107498; DDD-498; M5717)

1469439-69-7
Price and Availability of CAS No. : 1469439-69-7
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Cat. No. : HY-117684
M.Wt: 462.56
Formula: C27H31FN4O2
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic)
Introduction of 1469439-69-7 :

Cabamiquine (DDD107498) 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 inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2[1]. In Vitro:Cabamiquine (24-48 h) leads to abnormal trophozoites, and inhibits the development of trophozoites and schizonts in parasites, and inhibits protein synthesis[1].
Cabamiquine shows excellent activity against 3D7 parasites: EC50 =1.0 nM, EC90 = 2.4 nM, EC99 = 5.9 nM[1].
Cabamiquine shows good metabolic stability when incubated with hepatic microsomes or hepatocyte[1].
In Vivo:Cabamiquine (p.o., a single dose) shows an ED90 (90% reduction in parasitaemia) of 0.57 mg/kg in mice infected with the rodent parasite P. berghei[1].
Cabamiquine (p.o., 3 mg/kg) shows Cmax of 80 ng/mL, Tmax of 4 h, AUC of 200542 ng·min/mL, F (%) of 84%[2].

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