SML1743

ETaKG

≥95% (HPLC)

• Synonym(e): 2-Oxo-pentanedioic acid 5-ethyl ester 1-(3-trifluoromethyl-benzyl) ester, 5-Ethyl 1-(3-(trifluoromethyl)benzyl) 2-oxopentanedioate
• Empirische Formel (Hill-System): C₁₅H₁₅F₃O₅
• Molekulargewicht: 332.27
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 329826049
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: oil
• Farbe: colorless to light yellow
• Lagertemp.: 2-8°C
• SMILES String: O=C(C(CCC(OCC)=O)=O)OCC1=CC=CC(C(F)(F)F)=C1

Beschreibung

Biochem./physiol. Wirkung

ETaKG is a cell-permeable, aqueous stable, bioavailable, non-toxic α-ketoglutarate/2-oxoglutarate (α-KG/2-OG) diester derivative that readily undergoes hydrolysis by cytosolic esterases to α-KG. The monoester analog, TaKG is also membrane permeant. ETaKG elevates intracellular [α-KG] by ~15-fold in a prologned fashion, destabilizes HIF-1α/2α and reactivates prolyl hydroxylases (PHDs) in hypoxic HCT116, A431 and RPE cells at 2 mM. Further, shown to selectively trigger PHD-dependent cell death in hypoxic cells and decreases cellular [ATP] and glucose uptake. ETaKG has shown to reduce glucose metabolism, elevate [α-KG] levels and suppress A375 xenograft tumor growth (750 mg/kg of mice, p.o., q.d., 14 days). Also, induces mTORC1 lysosomal translocation and stimulates mTORC1 activity in the absence of glutaminolysis in U2OS cells.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable