| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In P. falciparum-infected erythrocytes, (+)-SJ733 binds to a single receptor site with an affinity equivalent to its growth inhibitory potency (kd=50 nM). In extensive in vitro assays, as well as in single or repeated dose studies at any tested dose in any preclinical species safety or tolerability (no adverse effect levels observed and maximum tolerated dose >240 mg/kg in a 7-day repeated-dose study in rats), (+)-SJ733 did not demonstrate significant safety at any dose. Consequently, it is anticipated that (+)-SJ733 will have a safety margin of at least 43 times [1].
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| ln Vivo |
After administering (+)-SJ733 to P. falciparum-infected NOD-scid IL2R·null mice, the parasites were rapidly cleared, becoming undetectable within 48 hours and 80% eliminated in the first 24. In a NOD-scid IL2Rγnull mouse model, (+)-SJ733 was highly potent and effective against Plasmodium falciparum 3D70087/N9 in vivo, with an effective dose of 90% (ED90 1.9 mg) when given orally four times a day. When compared to artesunate (11.1 mg/kg; AUCED90 undetermined), chloroquine (4.3 mg/kg; AUCED90 3.1 μM·h), and pyrimethamine (0.9 mg/kg; AUCED90 5. μM⋅h) in the same model, (+)-SJ733 was superior. Blood concentrations of (+)-SJ733 treated with ED90 dosages stayed above the mean in vitro EC90 for 6 to 10 hours following each dose [1].
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| References |
[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
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| Molecular Formula |
C24H16F4N4O2
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|---|---|
| Molecular Weight |
468.403059005737
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| CAS # |
1424799-20-1
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| SMILES |
FC(CN1C(C2C=CC=CC=2[C@H](C(NC2C=CC(=C(C#N)C=2)F)=O)[C@H]1C1C=NC=CC=1)=O)(F)F
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~106.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1349 mL | 10.6746 mL | 21.3493 mL | |
| 5 mM | 0.4270 mL | 2.1349 mL | 4.2699 mL | |
| 10 mM | 0.2135 mL | 1.0675 mL | 2.1349 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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