Name: (+)-SJ733 (SJ000557733)
Brand: GlpBio
SKU: GC32130
Availability: InStock
Rating: 5 (22 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >99.00%

Protocol

Cell experiment:

10 mL of asynchronous culture suspensions (2% hematocrit), at different parasite densities (104, 105, 106, 107, and 108 parasites), are added to each well of a 6-well plate. (+)-SJ733 is added to each well to make a final compound concentration of 1.8 μM, corresponding to 30×EC50 of the compound. Three wells are used for each parasite density. Plates are incubated at 37° C under an atmosphere of 90% N2, 5% O2, 5% CO2 for 90 days under constant drug pressure. The media of each well is replaced 3 times a week with freshly made media containing a compound concentration of 30×EC50. In addition, each well is split (1:2) once a week. Parasite outgrowth is monitored 3 times a week by transferring quadruplicate 40 μL aliquots from each well into a 384-well assay plate and determining parasitemia by a previously described method[1].

Animal experiment:

The pharmacokinetics of (+)-SJ733 are studied in overnight-fasted male Sprague Dawley rats weighing 267 to 291 g predose. Rats have access to water ad libitum throughout the pre- and post-dose sampling period, and access to food is reinstated 4 h post-dose. (+)-SJ733 is administered intravenously as a 10 min constant rate infusion (1.0 mL per rat, n=3 rats) and orally by gavage (10 mL/kg, n=3 rats). The IV formulation consists of pH 7.4 isotonic phosphate buffered saline containing 1% (w/v) hydroxypropyl-β-cyclodextrin, 10% (v/v) ethanol, 10% (v/v) propylene glycol and 40% (v/v) PEG400 whereas the oral formulation is an aqueous suspension in 0.5% (w/v) hydroxypropyl methylcellulose, 0.5% (v/v) benzyl alcohol and 0.4% (v/v) Tween80. Aliquots of the formulations are retained for analysis of the actual dose administered. Samples of arterial blood and total urine are collected at various time points up to 24 h post-dose[1].

References:

[1]. Jiménez-Díaz 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.

(+)-SJ733 is a clinical candidate for malaria which can also inhibit 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[1].

Treatment of P. falciparum-infected NOD-scid IL2Rγnull 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 3D70087/N9 in vivo when administered as four sequential daily oral doses in the NOD-scid IL2Rγnull mouse model, with a 90% effective dose, (ED90 1.9 mg/kg) and exposure [area under the curve at ED90 (AUCED90), 1.5 μM?h] superior to artesunate (11.1 mg/kg; AUCED90 not determined), chloroquine (4.3 mg/kg; AUCED90 3.1 μM?h), and pyrimethamine (0.9 mg/kg; AUCED90 5. μM?h) in the same model. When treated with the ED90 dose, (+)-SJ733 concentrations in blood remain above the average in vitro EC90 for 6 to 10 h after each dose[1].

[1]. Jiménez-Díaz 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.

Cas No.	1424799-20-1	SDF
Synonyms	SJ000557733
Canonical SMILES	O=C([C@@H](C1=C2C=CC=C1)[C@@H](C3=CC=CN=C3)N(CC(F)(F)F)C2=O)NC4=CC=C(F)C(C#N)=C4
Formula	C₂₄H₁₆F₄N₄O₂	M.Wt	468.4
Solubility	DMSO : 50 mg/mL (106.75 mM)	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	2.1349 mL	10.6746 mL	21.3493 mL
	5 mM	0.427 mL	2.1349 mL	4.2699 mL
	10 mM	0.2135 mL	1.0675 mL	2.1349 mL

Molarity Calculator
Dilution Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal:μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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