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D574-0246

Alias: iOXCT1
D574-0246 is a dual-activity inhibitor of oxCT1, which can simultaneously inhibit the ketogenic and succinylation activities of oxCT1.
D574-0246
D574-0246 Chemical Structure CAS No.: 1269110-12-4
Product category: Mitochondrial Metabolism
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes
Official Supplier of:
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Product Description
D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both oxCT1 ketogenesis and succinylation activity. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells and decreases OXCT1 ketogenesis activity. D574-0246 inhibits HCC cell survival (IC50: 16.49 μM for PLC cells and 6.656 μM for HepG2 cells). D574-0246 exhibits antitumor efficacy in nude mice carrying HepG2 xenografts overexpressing OXCT1. D574-0246 may be used in hepatocellular carcinoma (HCC) research.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
D574-0246 (4 days) reduced the survival rate of PLC cells with an IC50 of 16.49 μM and reduced the survival rate of HepG2 cells with an IC50 of 6.656 μM[1]. D574-0246 (1-10 μM) significantly reduced substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells in a dose-dependent manner[1]. D574-0246 (1-10 μM) significantly reduced the ketogenic activity of OXCT1 in HepG2 cells[1].
ln Vivo
D574-0246 (55 mg/kg, intraperitoneal injection, once every 3 days for a total of 8 times) significantly inhibited tumor growth in nude mice with xenografts of HepG2 overexpressing OXCT1 [1].
Animal Protocol
Animal/Disease Models: HepG2 cells with OXCT1 overexpression or knockout (2 × 106) were subcutaneously implanted into the flanks of 5-week-old male BALB/c nude mice[1]
Doses: 55 mg/kg
Route of Administration: i.p., once every 3 days for 8 times
Experimental Results: Inhibited tumor growth in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors, while exerting no significant inhibitory effect on tumor growth in nude mice with OXCT1-knockout HepG2 xenograft tumors. Reduced both global protein succinylation levels and LACTB K284-specific succinylation levels in OXCT1-overexpressing tumor tissues. Showed no significant changes in body weight. Caused no significant abnormalities in serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP) in nude mice. Induced no obvious morphological changes in major organs (liver, kidney, and spleen) of nude mice.
References

[1]. https://pubmed.ncbi.nlm.nih.gov/40925224/

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H26N6O3
Molecular Weight
446.50
CAS #
1269110-12-4
Appearance
White to light yellow solid powder
Synonyms
iOXCT1
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~223.96 mM; with sonication)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 5 mg/mL (11.20 mM)(saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 50.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix thoroughly. Then add 50 μL of Tween-80 to the above system and mix thoroughly. Finally, add 450 μL of physiological saline to bring the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in ddH₂O and bring the volume to 100 mL to obtain a clear and transparent physiological saline solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 5 mg/mL (11.20 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clarified DMSO stock solution to 900 μL of corn oil and mix well.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • Enter 10 in the Concentration box and choose the correct unit (mM)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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