(+)-SJ733 是一种抗疟疾剂，也是一个 Na⁺-ATPase PfATP4 抑制剂。

(+)-SJ733 is an anti-malaria agent which can also inhibit Na-ATPase PfATP4.

Solid

Parasite, Na-ATPase PfATP4

(+)-SJ733 binds to a single receptor site in P. falciparum -infected erythrocytes with equivalent affinity to its growth-inhibitory potency (kd=50 nM). (+)-SJ733 has not exhibited either significant safety liabilities at any dose in extensive profiling in vitro or significant safety or tolerability liabilities in either single- or repeat-dose studies at any dose tested in any preclinical species (no observed adverse effect level and maximum tolerated dose >240 mg/kg from 7-d repeat dosing study in rat). Therefore, (+)-SJ733 is expected to have a safety margin of at least 43-fold. has not independently confirmed the accuracy of these methods. They are for reference only.

Treatment of P. falciparum-infected NOD-scid IL2Rγ mice with (+)-SJ733 causes rapid clearance of parasites, which are 80% depleted within the first 24 h and undetectable by 48 h. (+)-SJ733 is highly potent and efficacious against P. falciparum 3D7 in vivo when administered as four sequential daily oral doses in the NOD-scid IL2Rγ mouse model, with a 90% effective dose, (ED 90 1.9 mg/kg) and exposure [area under the curve at ED 90 (AUC ED90 ), 1.5 μM?h] superior to artesunate (11.1 mg/kg; AUC ED90 not determined), chloroquine (4.3 mg/kg; AUC ED90 3.1 μM?h), and pyrimethamine (0.9 mg/kg; AUC ED90 5. μM?h) in the same model. When treated with the ED 90 dose, (+)-SJ733 concentrations in blood remain above the average in vitro EC 90 for 6 to 10 h after each dose.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Jimenez-Diaz MB, et al. (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium. Proc Natl Acad Sci U S A. 2014 Dec 16;111(50):E5455-62.

In Vitro: DMSO : 50 mg/mL (106.75 mM; Need ultrasonic)配制储备液