420640

Ketohexokinase Inhibitor

• Sinônimo(s): Ketohexokinase Inhibitor, N⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
• Fórmula empírica (Notação de Hill): C₂₁H₂₆N₈S · 2HCl
• Peso molecular: 495.47
• Código UNSPSC: 12352200
• NACRES: NA.28

Propriedades

• Ensaio: ≥97% (HPLC)
• Nível de qualidade: 100
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 16.6 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

An orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC₅₀ = 12 nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC₅₀ ≤ 400 nM in HepG2 cells). Displays ~50-fold lower potency towards metabolic kinases, namely, ribokinase, hexokinase and adenosine kinase, and minimal binding affinities to diverse receptors and ion-channels, and excellent selectivity among a panel of 31-kinases including Akt1, AMPK, CaMKI/II, InsR, IRAK4, PKA and PKCθ (IC₅₀ >>10 µM). Shown to minimally affect the activities of human cytochrome p450 isozymes (1A2, 2C19, 2D6, 2C9 and 3A4), and exhibit high volume of distribution and high rate of clearance in rats.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Maryanoff, B.E., et al. 2011. ACS Med. Chem. Lett.2, 538.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable