1009734-33-1 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1009734-33-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,9,7,3 and 4 respectively; the second part has 2 digits, 3 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1009734-33:
(9*1)+(8*0)+(7*0)+(6*9)+(5*7)+(4*3)+(3*4)+(2*3)+(1*3)=131
131 % 10 = 1
So 1009734-33-1 is a valid CAS Registry Number.
1009734-33-1Relevant articles and documents
USE OF A QUINAZOLINE COMPOUND IN PREPARING A MEDICAMENT AGAINST FLAVIVIRIDAE VIRUS
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Paragraph 0039-0040, (2013/10/08)
Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
Discovery and optimization of 2,4-diaminoquinazoline derivatives as a new class of potent dengue virus inhibitors
Chao, Bo,Tong, Xian-Kun,Tang, Wei,Li, De-Wen,He, Pei-Lan,Garcia, Jean-Michel,Zeng, Li-Min,Gao, An-Hui,Yang, Li,Li, Jia,Nan, Fa-Jun,Jacobs, Michael,Altmeyer, Ralf,Zuo, Jian-Ping,Hu, You-Hong
, p. 3135 - 3143 (2012/06/01)
The results of a high-throughput screening assay using the DENV-2 replicon showed that the 2,4-diaminoquinazoline derivative 4a has a high dengue virus inhibitory activity (EC50 = 0.15 μM). A series of 2,4-diaminoquinazoline derivatives based on 4a as a lead compound were synthesized and subjected to structure-antidengue activity relationship studies. Among the series of 2,4-diaminoquinazoline derivative probed, 4o was observed to display both the highest antiviral potency (EC50 = 2.8 nM, SI > 1000) and an excellent pharmacokinetic profile.