Virus Protease Inhibitor

ZIKV-IN-3 (compound 5a), an andrographolide derivatives, is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC₅₀ value of 18.34 μM. ZIKV-IN-3 inhibits ZIKV replication and infection. ZIKV-IN-3 can be used in research of Zika virus (ZIKV).

UAWJ-247 is a potent and reversible SARS-CoV-2 main protease (Mpro) inhibitor with an IC₅₀ of 0.042 μM and a K_i of 0.035 μM. UAWJ-247 can be used for the research of covid-19.

AVI8122 is a covalent coronavirus main protease (M^pro) inhibitor, with IC₅₀ values of 0.0047 μM, 0.065 μM, 0.04 μM, 0.004 μM, 0.027 μM and 0.020 μM against SARS-CoV-2, MERS-CoV, HKU8, PEDV, IBV and HKU15, respectively; it exhibits K_i values of 0.14 nM, 1.8 nM, 0.9 nM, 0.2 nM and 5.2 nM against SARS-CoV-2, HKU8, PEDV, IBV and HKU15, respectively. AVI8122 forms a covalent hemithioacetal bond with the catalytic cysteine of M^pro, blocks its proteolytic activity, and acts on the four coronavirus genera α, β, γ and δ. AVI8122 is applicable to research related to SARS-CoV-2 infection.\n

Tirilazad (U 74006F free base) Standard is the analytical standard of Tirilazad (HY-132280). This product is intended for research and analytical applications. Tirilazad (U 74006F free base) is a neuroprotective agent. Tirilazad can also bind tightly to the main protease of the COVID-19 virus and exert anti-SARS-CoV-2 activity. Tirilazad scavenges hydroxyl and lipid peroxyl free radicals and maintains the levels of endogenous antioxidants. Tirilazad reduces cerebral infarct volume and improves neurobehavioral scores in animal models of focal ischemia. Tirilazad can be used in research related to ischemic stroke and subarachnoid hemorrhage.

SB-140 is a selective, covalent PLpro inhibitor with an IC₅₀ of ≤2.5 nM against SARS-CoV-2 PLpro. SB-140 has antiviral activity against SARS-CoV-2, MERS-CoV and SARS-CoV-1.

SARS 3CLpro-IN-2 (Example 9) is a severe acute respiratory syndrome 3C-like protease (SARS 3CL^pro) inhibitor with an IC₅₀ of 0.02 mM. It exhibits antiviral activity against SARS with an EC₅₀ of 42 mM. SARS 3CLpro-IN-2 can be used in research related to severe acute respiratory syndrome.

Crepidiaside B is a plant-derived active component that can be found in Cichorium intybus. Crepidiaside B acts as a SARS-CoV-2 spike glycoprotein inhibitor and is used in research related to coronavirus disease 2019 (COVID-19).

Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells.

DENV-IN-8 (Compound 5e) is a DENV2 inhibitor with an EC₅₀ of 0.068 μM.

SARS-CoV-2 Mpro-IN-25 (Compound 3a) is a SARS-CoV-2 protease inhibitor with an IC₅₀ value of 0.26 μM. SARS-CoV-2 Mpro-IN-25 exhibits antiviral activity and can be used in pneumonia-related research.

Mer-NF5003F (Stachybotrydial; F 1839M), a sesquiterpene isolated from Stachybotrys, inhibits avian medulloblastoma virus (AMV) protease (IC₅₀=7.8 μM). Mer-NF5003F inhibits sialyltransferase 6N (ST6N), ST3O, and ST3N (IC₅₀=0.61, 6.7, and 10 μg/mL, respectively), and fucosyltransferase (IC₅₀=11.3 μg/mL). Mer-NF5003F has in vitro activity against herpes simplex virus HSV-1 (IC₅₀=4.32 μg/mL) and multidrug-resistant Plasmodium falciparum K1 strain (IC₅₀=0.85 μg/mL).

VMPWDEWLTKRKPELP is a chikungunya virus (CHIKV) nsP2 protease inhibitor with a IC₅₀ of 4.6 μM and a K_d of 1.39 μM. VMPWDEWLTKRKPELP can be used for the research of chikungunya fever.

SP-393D is an amidoxime-based prodrug inhibitor targeting dengue virus NS2B/NS3. The EC₅₀ values of SP-393D in Huh7 cells infected with DENV-1, DENV-2, DENV-3 and DENV-4 are 1.41, 0.066, 0.66 and 0.071 μM, respectively, while its CC₅₀ against Huh7 cells is >100 μM. SP-393D exhibits pan-serotypic activity against dengue virus serotypes 1, 2, 3 and 4. SP-393D binds to the allosteric pocket of dengue virus NS2B/NS3 protease and generates additional hydrogen bonding interactions. SP-393D can be used in studies related to dengue virus infection.

SARS-CoV-2 3CLpro-IN-39 (compound 7c) is a broad-spectrum antiviral agent and 3CLpro inhibitor that inhibits SARS-CoV-2, HCoV-OC43, HCoV-HKU1 and HCoV-NL63 3CL^pro with IC₅₀ values of 20, 710, 22 and 470 nM, respectively. SARS-CoV-2 3CLpro-IN-39 functionally inhibits the 3CLpro enzymatic activity of different coronaviruses. SARS-CoV-2 3CLpro-IN-39 exhibits anti-SARS-CoV-2 and anti-HCoV-NL63 activities. SARS-CoV-2 3CLpro-IN-39 can be used in the research of coronavirus infections.

Artecanin is a SARS-CoV-2 main protease (M^pro) inhibitor with predicted high gastrointestinal absorption and oral bioavailability, and no predicted hepatotoxicity, carcinogenicity, mutagenicity or cytotoxicity. Artecanin interacts with His41 and Cys145, the key amino acid residues in the active site of M^pro, blocks the cleavage and maturation of viral precursor proteins, and forms a stable complex with M^pro. Artecanin blocks the invasion of SARS-CoV-2. Artecanin is applicable to the research of COVID-19.

Probucol-¹³C₃ is the ¹³C-labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.

NSC 288387 is a pan-flavivirus MTase inhibitor. NSC 288387 binds to the SAM-binding pocket. NSC 288387 inhibits ZIKV with an IC₅₀ of 0.2 μM. NSC 288387 also inhibits viral replication in cell culture.

MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection.

mCMX110 is an orally active SARS-CoV-2 main protease inhibitor with an IC₅₀ of 35 nM. mCMX110 inhibits SARS-CoV-2 infection. SARS-CoV-2 mCMX110 can be used for the research of SARS-CoV-2 infection.

N-Desmethylclozapine (Standard) is the analytical standard of N-Desmethylclozapine. This product is intended for research and analytical applications. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.