rsv in 2

RSV-IN-2 is a powerful compound that acts as a dual inhibitor of both wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. It efficiently inhibits the activity of these proteins, with an EC50 value of 0.27 nM for the wild-type and 0.70 nM for the D486N-mutant protein.

RSV IAV-IN-2 (compound 14c) 是一种有效的 RSV IAV 双重抑制剂。RSV IAV-IN-2 的细胞毒性低于临床药物利巴韦林。RSV IAV-IN-2 具有研究 RSV 和 或 IAV 感染的潜力。

RSVL-protein-IN-2 (Compound A)为一种RSV聚合酶的非竞争性抑制剂，其IC50值为4.5 μM。此化合物对长RSV株表现出抗病毒活性，EC50值达1.3 μM。

GS-441524tris-isobutyryl ester is a prodrug form of the antiviral nucleoside analog and remdesivir metabolite GS-441524 .1It reduces the cytopathic effect of respiratory syncytial virus (RSV) in infected HEp-2 cells with an EC50value of 0.26 μM. 1.Mackman, R.L., Hui, H.C., Perron, M., et al.Prodrugs of a 1’-CN-4-aza-7,9-dideazaadenosine C-nucleoside leading to the discovery of remdesivir (GS-5734) as a potent inhibitor of respiratory syncytial virus with efficacy in the african green monkey model of RSVJ. Med. Chem.64(8)5001-5017(2021)

RSVL-protein-IN-3为一野生型RSV聚合酶抑制剂，具IC50值10.4 μM及EC50值2.1 μM(RSV)。相较之下，RSV IAV-IN-2之细胞毒性显著低于临床活性分子Ribavirin。

RSVL-protein-IN-5（compound E）是一种高效针对呼吸道合胞病毒（RSV）的抑制剂，拥有EC50值为0.1 μM。该化合物在IC50为0.66 μM的条件下能够抑制聚合酶（Polymerase），并通过阻断病毒转录物的鸟苷酸化过程来抑止RSVmRNA的合成。RSVL-protein-IN-5具有中等细胞毒性（CC50为10.7 μM，HEp-2细胞），同时，在每日4.1 mg kg剂量下，能减少RSV感染小鼠模型中的病毒滴度。

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

PC786是一种有效和选择性的的非核苷类RSV L蛋白聚合酶抑制剂，用于吸入治疗RSV感染，对RSV-A（IC50=0.09~0.71 nM）和RSV-B （IC 50=1.3~50.6 nM）具有抗病毒活性, 在HEp-2细胞能够抑制RSV RNA依赖性RNA聚合酶（RdRp）。

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)

RSV-IN-4 (Compound 2) 具有抗 RSV 活性，EC50值为11.76 μM。RSV-IN-4 是呼吸道合胞病毒 (RSV) 和甲流病毒 A (IAV) 的双重抑制剂。