5.00670

FATP2 Inhibitor, CB-2

• Synonym(s): FATP2 Inhibitor, CB-2, (5E)-5-((3-bromo-4-hydroxy-5-methoxyphenyl)methylene)-3-(3-chlorophenyl)-2-thioxothiazolidin-4-one, CB2, Fatty Acid Transport Protein 2 Inhibitor
• Empirical Formula (Hill Notation): C₁₇H₁₁BrClNO₃S₂
• Molecular Weight: 456.76
• UNSPSC Code: 41106300
• NACRES: NA.77

Properties

• Assay: ≥99% (HPLC)
• Quality Level: 100
• form: solid
• potency: 8 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell permeable thioxothiazolindine compound that reversibly inhibits FATP2- (fatty acid transport protein 2) mediated long chain fatty acid uptake in Caco-2 and HepG2, but not non-FATP2-expressing 3T3-L1 adipocytes, cultures (IC₅₀ against C₁-BODIPY-C₁₂ = 3.99, 7.55, and 231.1 µM, respectively), exhibiting much reduced potency toward cellular Acsl (acyl-CoA synthetase) activity (IC₅₀ = 50 µM using lysates from 1h inhibitor-treated Caco-2 cells). Shown not to affect Caco-2 viability (50 µM in MTT assay), membrane permeability (by trans-epithelial electrical resistance measurement; 50 µM), glucose transport (20 µM in 2-NBDG uptake assay).

A cell permeable thioxothiazolindine compound that reversibly inhibits FATP2-mediated long chain fatty acid uptake in Caco-2 and HepG2, but not non-FATP2-expressing 3T3-L1 adipocytes, cultures (IC₅₀ = 3.99, 7.55, and 231.1 µM, respectively), while exhibiting much reduced potency toward cellular Acsl (acyl-CoA synthetase) activity (IC₅₀ = 50 µM). Shown not to affect Caco-2 viability, membrane permeability, or glucose transport.

Biochem/physiol Actions

Cell permeable: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sandoval, A., et al. 2010. Biochem. Pharmacol.79, 99.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable