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Lipofermata

Cat. No. M25468
Lipofermata Structure
Synonym:

SIT-4; 5-bromo-5'-phenyl-3'H-spiro[indole-3,2'-[1,3,4]thiadiazol]-2(1H)-one

Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 290  USD290 In stock
25mg USD 430  USD430 In stock
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Quality Control & Documentation
Biological Activity

Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM. Lipofermata inhibits C1-BODIPY-C12 transport into C2C12, INS-1E, Caco-2 and HepG2 cells at comparable levels yielding sigmoidal dose-response curves with IC50s in the low micromolar range (IC50=2.74-39.34 μM).

Chemical Information
Molecular Weight 360.23
Formula C15H10BrN3OS
CAS Number 297180-15-5
Form Solid
Solubility (25°C) DMSO 90 mg/mL
Storage Powder -20°C
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] Jiyoon L Kim, et al. J Biol Chem. Fatty acid transport protein 2 interacts with ceramide synthase 2 to promote ceramide synthesis

[2] Fernando Santos-Beneit, et al. Sci Rep. A metabolic modeling approach reveals promising therapeutic targets and antiviral drυgs to combat COVID-19

[3] Adeleye Oluwatosin Adeshakin, et al. Data Brief. Lipidomics data showing the effect of lipofermata on myeloid-derived suppressor cells in the spleens of tumor-bearing mice

[4] Maomao Zhang, et al. Cancer Discov. Adipocyte-Derived Lipids Mediate Melanoma Progression via FATP Proteins

[5] Constance Ahowesso, et al. Biochem Pharmacol. Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death

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Keywords: Lipofermata, SIT-4; 5-bromo-5'-phenyl-3'H-spiro[indole-3,2'-[1,3,4]thiadiazol]-2(1H)-one supplier, Antibiotic, inhibitors, activators


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