85-2073-97　Ketohexokinase Inhibitor (N8-(Cyclopropylmethyl)-N4-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor) 10mg　217490

特徴

• An orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC50 = 12nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400nM 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 PKCtheta (IC50 >> 10uM). 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.
• Molecular Formula:C₂₁H₂₆N₈S•2HCl
• Solubility:DMSO
• Molar Mass:495.5
• Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.