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(+)-SJ733

Cat. No. M28397
(+)-SJ733 Structure
Synonym:

SJ000557733

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Biological Activity

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

Chemical Information
Molecular Weight 468.4
Formula C24H16F4N4O2
CAS Number 1424799-20-1
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Aditya H Gaur, et al. EBioMedicine. Combining SJ733, an oral ATP4 inhibitor of Plasmodium falciparum, with the pharmacokinetic enhancer cobicistat: An innovative approach in antimalarial drug development

[2] Arya SheelaNair, et al. Malar J. Similarly efficacious anti-malarial drugs SJ733 and pyronaridine differ in their ability to remove circulating parasites in mice

[3] Yizhe Chen, et al. Malar J. Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

[4] Aditya H Gaur, et al. Lancet Infect Dis. Safety, tolerability, pharmacokinetics, and antimalarial efficacy of a novel Plasmodium falciparum ATP4 inhibitor SJ733: a first-in-human and induced blood-stage malaria phase 1a/b trial

[5] María Belén Jiménez-Díaz, et al. Proc Natl Acad Sci U S A. (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium

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Keywords: (+)-SJ733, SJ000557733 supplier, Sodium Channel, inhibitors, activators


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