SARS-CoV Inhibitor

Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.

Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC₅₀ of 24.70 μM and a K_i of 15.29 μM against PTP1B, an IC₅₀ of 41.46 μg/mL against BChE, a K_i of 0.61 mM against mushroom tyrosinase, and an IC₅₀ of 2.50 μM against SARS-CoV-2 3CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury.

Bepridil hydrochloride hydrate (CERM 1978 hydrate; Org 5730 hydrochloride hydrate) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride hydrate modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride hydrate acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride hydrate alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride hydrate also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride hydrate is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Diosmetin-7-O-β-D-glucopyranoside is a natural product that can be isolated from the flowers of Chrysanthemum morifolium. Diosmetin-7-O-β-D-glucopyranoside has potent antiviral and anti-inflammatory activities against SARS-CoV-2 both in vitro (IC₅₀ = 0.74 μM) and in vivo. Diosmetin-7-O-β-D-glucopyranoside has significant anti-thrombotic activity when combined with Pae and 5-HMF at a ratio of 3:4:3 in a zebrafish model.

Bemnifosbuvir hemisulfate (AT-527), a hemisulfate salt of AT-511, a guanosine nucleotide proagent, is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir hemisulfate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₉₀=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity.

NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

(±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (M_pro).

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

Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC₅₀=13 nM).

Cilgavimab (AZD-1061; COV2-2130) is a human SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection.

Imdevimab (REGN10987) is a human monoclonal antibody that targets SARS-CoV-2 virus. Imdevimab can be used in combination with Casirivimab (HY-P99341) to reduce viral load and transiently increases anti-receptor-binding domain IgG titers. Imdevimab maintains most of its neutralization activity against viruses with B.1.1.7, B.1.351 and mink cluster 5 spike proteins.

Arteannuin B, No. 2000 can be jointly submitted with the blue material. Arteannuin B had anti-SARS-CoV-2 activity, EC₅₀=10.28 μM.

Tubeimoside II is an orally active triterpenoid saponin and antiviral agent that binds to PACT/PRKRA with K_d values of 5.37 μM and 133.1 μM, respectively. Tubeimoside II inhibits oxidase-dependent EGFR activation and reduces TGF-β1-induced oxidative stress. Tubeimoside II activates the RIG-I signaling pathway and increases IFN-β secretion. Tubeimoside II suppresses TPA-induced ear edema, mouse sarcoma 180 growth, and TPA-induced skin tumor formation. Tubeimoside II exerts broad-spectrum antiviral activity against SARS-CoV-2, HCoV-OC43, and IAV-H1N1/FM1. Tubeimoside II can be used in research related to retinoblastoma, respiratory viral infections, skin tumors, and sarcoma 180.

Hydroxychloroquine (sulfate) (Standard) is the analytical standard of Hydroxychloroquine (sulfate). This product is intended for research and analytical applications. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

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.

Bebtelovimab a human IgG1-λ2 antibody targeting to SARS-CoV-2, especially COVID-19 ((the IC₅₀ value for SARS-CoV-2/MT020880.1 virus is 9-22.1 ng/mL)). Bebtelovimab potently neutralizes SARS-CoV-2 variants, and inhibits COVID-19 with mild-to-moderate efficacy.

SARS-CoV-2-IN-41 (compound 2) is a potent SARS-CoV-2 3CL^pro inhibitor with an IC₅₀ value of 0.022 µM. SARS-CoV-2-IN-41 shows antiviral effect.

Secutrelvir is an oral SARS-CoV-2 3C-like protease (3CLpro) inhibitor and antiviral agent, with IC₅₀ values of 0.655 nM and 0.697 nM against SARS-CoV-2 3CLpro, respectively. Secutrelvir forms a reversible covalent bond with the catalytic cysteine C145 of SARS-CoV-2 3CLpro, thereby inhibiting viral replication. Secutrelvir exhibits activity against multiple SARS-CoV-2 variants and can be used in research related to coronavirus disease 2019 (COVID-19).

Walrycin B, an analogue of toxoflavin, is a potent SARS-CoV-2 3CL^pro inhibitor with an IC₅₀ of 0.26 μM. Walrycin B is a WalR response regulator inhibitor. Walrycin B has potent activity of inhibiting bacteria growth.

MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity.