420640

Ketohexokinase Inhibitor

• Sinonimo/i: Ketohexokinase Inhibitor, N⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
• Formula empirica (notazione di Hill): C₂₁H₂₆N₈S · 2HCl
• Peso molecolare: 495.47
• Codice UNSPSC: 12352200
• NACRES: NA.28

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow
• Solubilità: DMSO: 16.6 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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.

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable