5-tert-butoxyquinazoline-2,4-diaMine Property

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

insoluble in H2O; ≥11.6 mg/mL in DMSO; ≥8.82 mg/mL in EtOH

form 

solid

color 

White to light yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H332Harmful if inhaled

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

5-tert-butoxyquinazoline-2,4-diaMine Chemical Properties,Usage,Production

Biological Activity

hz-1157 is a potent hepatitis c virus (hcv) inhibitor toward hcv ns3/4a protease with ic50 value of 1.0 μmol/l [1].the ns3 protease of hcv is a prime target for the development of anti-hcv agents because it cleaves the viral polyprotein and liberates ns3, ns4a, ns4b, ns5a, and ns5b, allowing them to function normally in viral rna replication, and it deactivates many host proteins involved in innate immunity to foster a favorable cellular environment for hcv replication. the ns3 protease is most active when complexed with its cofactor ns4a [1].

in vitro

huh7.5.1 cell line stably transfected with hcv ns3/4a protease reporter was established to investigate the anti-hcv mechanism of hz-1157 (0.001~1 μmol/l). the results showed that hz-1157 exhibited inhibitory effect on the hcv ns3/4a protease with ic50 value of 1.0 μmol/l. hz-1157 was further tested against an infectious hcv virus (j399em) which can infect and replicate in huh7.5.1 cells in vitro. the results showed that hz-1157 effectively inhibited j399em virus replication in huh7.5.1 cells with ic50 value of 0.82 μmol/l [1].

References

[1]. yu y, jing j, tong x, et al. discovering novel anti-hcv compounds with inhibitory activities toward hcv ns3/4a protease[j]. acta pharmacologica sinica, 2014, 35(8): 1074.