5.38001

T-00127-HEV1

• Synonym(s): T-00127-HEV1, 3-(3,4-Dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholinoethyl)pyrazolo[1,5-a]pyrimidin-7-amine, PI4KIIIβ Inhibitor II
• Empirical Formula (Hill Notation): C₂₂H₂₉N₅O₃
• CAS Number: 900874-91-1
• Molecular Weight: 411.50
• UNSPSC Code: 12352200

Properties

• assay: ≥95% (HPLC)
• Quality Level: 200
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

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 Actions

Cell permeable: yes

Primary Target
PI4KIIIβ

Reversible: yes

Target IC₅₀: 150 nM for PI4KIII&beta

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable