sars-cov, in vero cells

SARS-CoV-IN-1 is an effective SARS-CoV replication inhibitor with an EC50 of 4.9 μM in Vero cells.

SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication.

SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity that inhibits the replication of severe acute respiratory syndrome coronavirus [SARS-CoV] in Vero 76 cells, Middle East respiratory syndrome coronavirus [MERS-CoV] in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s = 0.1, 0.15, and 0.3 μM, respectively).

SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is a conformational inhibitor of SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. It demonstrates good cellular permeability, being able to effectively cross the cell membrane following co-incubation with Vero-E6 cells.

SARS-CoV-2 Mpro-IN-34 (Compound 26) acts as an inhibitor of SARS-CoV-2 Mpro with an IC50 of 6 nM. It also inhibits OC43 Mpro, demonstrating an IC50 of 33 nM. Furthermore, this compound exhibits antiviral activity in Vero E6 cells infected with SARS-CoV-2, with an EC50 of 0.103 μM.

SARS-CoV-2 Mpro-IN-29 (Compound 7) is an inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 of 310 nM for Mpro and an EC50 of 0.5 μM in Vero cells. By binding to the active site of Mpro, it prevents the cleavage of viral polyproteins, exhibiting significant antiviral activity and enhanced metabolic properties. SARS-CoV-2 Mpro-IN-29 holds potential for research in SARS-CoV-2 antiviral drug development.

CKP-25 is an inhibitor that disrupts the interaction between Spike RBD and ACE2, preventing virus entry into host cells, thus reducing viral replication and infection. It inhibits SARS-CoV-2 with an IC50 of 3.5 μM in Vero E6 cells.

SARS-CoV-2 PLpro-IN-1 (Compound 85) is a non-covalent competitive inhibitor of SARS-CoV-2 PLpro with an IC50 value of 15.06 μM and a Ki value of 22.93 μM. It inhibits the proliferation of Vero cells, exhibiting an IC50 of 7.47 μM.

SARS-CoV-2 Mpro-IN-39 (Compound 9d) is an inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 value of 5.94 µM. It inhibits the replication of SARS-CoV-2 in Vero cells with an EC50 value of 9.33 µM, and has a cytotoxicity CC50 value of 289.63 µM. This compound is applicable in COVID-19 related research.

SARS-CoV-2-IN-111 (compound 77) is a highly effective inhibitor of SARS-CoV-2, exhibiting an IC50 of 0.67 μM. It markedly decreases the presence of SARS-CoV-2 within Vero cells.

3-Deazaguanosine (C3Guo) exhibits potent antiviral activity against SARS-CoV-2 with an EC50 of 1.14 μM and a CC50 greater than 200 μM in Vero E6 cells. It has the potential to prevent COVID-19.

RH12 is a dual inhibitor of SARS-CoV-2-related RNA-dependent RNA polymerase (RdRp, IC50 of 4.42 nM) and human transmembrane serine protease 2 (TMPRSS2, IC50 of 4.2 nM). It demonstrates antiviral activity by inhibiting viral replication and absorption, showing 90.5% virucidal effect in Vero-E6 cells. Additionally, RH12 inhibits Calu-3 cell viability with an IC50 of 17.5 nM.

Peptide originally derived from SARS-CoV Spike (S) protein; corresponds to amino acid residues 668 to 679. Highly potent inhibitor of SARS-CoV S protein and ACE2 interaction (IC50 = 1.88 nM in biochemical assay). Inhibits interaction of SARS-CoV S protein and Vero E6 cells in vitro. Please note, this peptide displays 80% sequence identity to homologous site on SARS-CoV-2 S-protein (residues 689-697).

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

SARS-CoV-2-IN-7 demonstrates potent inhibition of viral replication in SARS-CoV-2-infected Vero E6 cells with an IC50 value of 844 nM.

SARS-CoV-2-IN-36 is a potent inhibitor of SARS-CoV-2 Mpro (SARS-CoV), demonstrating an IC50 of 2.37 μM and a Kd of 1.19 μM in enzymatic assays, and exhibits antiviral activity against SARS-CoV-2 variants UC-1074, RG2674, and NVDBB-2220 in Vero cells.

SARS-CoV-2-IN-54 (Compound 2), a SARS-CoV-2 inhibitor, exhibits antiviral activity in Vero E6 cells with an inhibitory concentration (IC50) of 21.4 μM [1].

SARS-CoV-2-IN-56 (Compound 63) is a SARS-CoV-2 inhibitor exhibiting antiviral activity, with an IC50 of 0.7 μM in Vero E6 cells [1].

SARS-CoV-2 3CLpro-IN-14 (compound 11j) is an orally active inhibitor of SARS-CoV-2 3CLpro, demonstrating potent anti-SARS-CoV-2 properties with an EC50 of 0.18 μM and exhibits minimal cytotoxicity, having a CC50 greater than 50 μM, in Vero E6 cells [1].

SARS-CoV-2 3CLpro-IN-18 (Compound 3C) is a covalent inhibitor of SARS-CoV-2 3CLpro with an IC50 of 0.478 μM. It inhibits SARS-CoV-2 in Vero E6 cells with an EC50 of 2.499 μM and exhibits low cytotoxicity (CC50 > 200 μM) [1].

SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication, exhibiting low cytotoxicity and effectively suppressing viral replication in Vero E6 and Calu-3 cells, with half-maximal effective concentration (EC50) values of 1.99 μM and 1.92 μM, respectively [1].