SML1743

ETaKG

≥95% (HPLC)

• 別名: 2-Oxo-pentanedioic acid 5-ethyl ester 1-(3-trifluoromethyl-benzyl) ester, 5-Ethyl 1-(3-(trifluoromethyl)benzyl) 2-oxopentanedioate
• 実験式（ヒル表記法）: C₁₅H₁₅F₃O₅
• CAS番号: 2122289-21-6
• 分子量: 332.27
• UNSPSCコード: 12352200
• PubChem Substance ID: 329826049
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: oil
• 色: colorless to light yellow
• 保管温度: 2-8°C
• SMILES記法: O=C(C(CCC(OCC)=O)=O)OCC1=CC=CC(C(F)(F)F)=C1
• InChI: 1S/C15H15F3O5/c1-2-22-13(20)7-6-12(19)14(21)23-9-10-4-3-5-11(8-10)15(16,17)18/h3-5,8H,2,6-7,9H2,1H3
• InChI Key: OKDCLZOKKGLMIX-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

A cell-permeable, bioavailable & aqueous stable α-ketoglutarate prodrug that selectively induces PHD-dependent cell death in hypoxic cells

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.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable