5.38001

T-00127-HEV1

• Synonym(e): T-00127-HEV1, 3-(3,4-Dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholinoethyl)pyrazolo[1,5-a]pyrimidin-7-amine, PI4KIIIβ Inhibitor II
• Empirische Formel (Hill-System): C₂₂H₂₉N₅O₃
• CAS-Nummer: 900874-91-1
• Molekulargewicht: 411.50
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥95% (HPLC)
• Qualitätsniveau: 200
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
PI4KIIIβ

Reversible: yes

Target IC₅₀: 150 nM for PI4KIII&beta

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable