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Chemical Structure| 101623-68-1 Chemical Structure| 101623-68-1

Structure of 101623-68-1

Chemical Structure| 101623-68-1

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Ganga Reddy Velma ; Zhengnan Shen ; Cameron Holberg ; Jiqiang Fu ; Farinaz Soleymani ; Laura Cooper , et al.

Abstract: The SARS-CoV-2 papain-like (PLpro), essential for viral processing and immune response disruption, is a promising target for treating acute infection of SARS-CoV-2. To date, there have been no reports of PLpro inhibitors with both submicromolar potency and animal model efficacy. To address the challenge of PLpro’s featureless active site, a noncovalent inhibitor library with over 50 new analogs was developed, targeting the PLpro active site by modulating the BL2-loop and engaging the BL2-groove. Notably, compounds 42 and 10 exhibited strong effects and were further analyzed pharmacokinetically. 10, in particular, showed a significant lung accumulation, up to 12.9-fold greater than plasma exposure, and was effective in a mouse model of SARS-CoV-2 infection, as well as against several SARS-CoV-2 variants. These findings highlight the potential of 10 as an in vivo chemical for studying PLpro inhibition in SARS-CoV-2 infection.

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Product Details of [ 101623-68-1 ]

CAS No. :101623-68-1
Formula : C11H11NO7
M.W : 269.21
SMILES Code : O=C(OC1=CC=C([N+]([O-])=O)C=C1)OC(OC(C)=O)C
MDL No. :MFCD27940873

Safety of [ 101623-68-1 ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330
 

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