5.38001

T-00127-HEV1

• Sinonimo/i: T-00127-HEV1, 3-(3,4-Dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholinoethyl)pyrazolo[1,5-a]pyrimidin-7-amine, PI4KIIIβ Inhibitor II
• Formula empirica (notazione di Hill): C₂₂H₂₉N₅O₃
• Numero CAS: 900874-91-1
• Peso molecolare: 411.50
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥95% (HPLC)
• Livello qualitativo: 200
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

A cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC₅₀ = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC₅₀ = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC₅₀ = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC₅₀ >50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.

A cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC₅₀ = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC₅₀ = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC₅₀ = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC₅₀ >50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
PI4KIIIβ

Reversible: yes

Target IC₅₀: 150 nM for PI4KIII&beta

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20&degC). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Mejdrova, I., et al. 2015. J. Med. Chem.58, In press.

Spickler, C., et al. 2013. Antimicrob. Agents Chemother.57, 3358.
Sasaki, J., et al. 2012. EMBO J.31, 754.
Arita, M., et al. 2011. J. Virol.85, 2364.

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 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable