400093

HIF-PHD Inhibitor II, JNJ-42041935

The HIF-PHD Inhibitor II, JNJ-42041935 controls the biological activity of HIF-PHD. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Sinónimos: HIF-PHD Inhibitor II, JNJ-42041935, 1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II
• Fórmula empírica (notación de Hill): C₁₂H₆ClF₃N₄O₃
• Número de CAS: 1193383-09-3
• Peso molecular: 346.65
• Número MDL: MFCD28900740
• Código UNSPSC: 12352200
• NACRES: NA.28

Propiedades

• Nivel de calidad: 100
• Análisis: ≥99% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 100 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: ClC1=CC2=C(NC(N3C=C(C=N3)C(O)=O)=N2)C=C1OC(F)(F)F

Descripción

Descripción general

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pK_i = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC₅₀ ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg).

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pK_i = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC₅₀ ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

Lee, K., et al., 2013. Angew. Chem. Int. Ed.52, In press.
Barrett, T.D., et al. 2011. Mol. Pharmacol.79, 910.
Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable