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420640 Ketohexokinase Inhibitor - Calbiochem

Ketohexokinase Inhibitor - Calbiochem: Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

Sinónimos: N⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor

420640
Purchase on Sigma-Aldrich

Descripción

Replacement Information

Tabla espec. clave

Empirical Formula
C₂₁H₂₆N₈S•2HCl

Products

Número de referenciaEmbalaje Cant./Env.
420640-10MG Frasco de vidrio 10 mg
Description
OverviewAn 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.
Catalogue Number420640
Brand Family Calbiochem®
SynonymsN⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
References
ReferencesMaryanoff, B.E., et al. 2011. ACS Med. Chem. Lett. 2, 538.
Product Information
FormYellow solid
Hill FormulaC₂₁H₂₆N₈S•2HCl
Chemical formulaC₂₁H₂₆N₈S•2HCl
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Número de referencia GTIN
420640-10MG 04055977187625

Documentation

Ketohexokinase Inhibitor - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Ketohexokinase Inhibitor - Calbiochem Certificados de análisis

CargoNúmero de lote
420640

Referencias bibliográficas

Visión general referencias
Maryanoff, B.E., et al. 2011. ACS Med. Chem. Lett. 2, 538.
Ficha técnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision22-February-2013 JSW
SynonymsN⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
DescriptionAn 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.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₁H₂₆N₈S•2HCl
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (16.6 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesMaryanoff, B.E., et al. 2011. ACS Med. Chem. Lett. 2, 538.