COVID-19 Related Products
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HIV protease 抑制剂
Darunavir Ethanolate (Prezista)是一种HIV蛋白酶抑制剂。
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GSK-3 抑制剂
Tideglusib是一种不可逆的，非ATP竞争性的GSK-3β抑制剂，无细胞试验中IC50为60 nM。用于治疗阿尔茨海默氏病和进行性核上性麻痹。
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viral RNA polymerase 抑制剂
T-705 (Favipiravir)是一种有效的选择性RNA-dependent RNA polymerase抑制剂，在体外和体内均表现出有效的抗流感病毒活性。
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- Satoko Yamaoka, .et al. Development of accelerated high-throughput antiviral screening systems for emerging orthomyxoviruses, Antiviral Res, 2022, Apr;200:105291 PMID: 35296419
- Crystal A Mendoza, .et al. The NF- κB inhibitor, SC75741, is a novel antiviral against emerging tick-borne bandaviruses, Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
- Liva Checkmahomed, .et al. In Vitro Combinations of Baloxavir Acid and Other Inhibitors against Seasonal Influenza A Viruses, Viruses, 2020, Oct; 12(10): 1139 PMID: 33049959
- JE Comer, .et al. Filovirus Virulence in Interferon α,β and γ Double Knockout Mice, and Treatment with Favipiravir, Viruses, 2019, Feb 3;11(2). pii: E137 PMID: 30717492
- Ma J, .et al. Enhancing the antiviral potency of ER α-glucosidase inhibitor IHVR-19029 against hemorrhagic fever viruses in vitro and in vivo, Antiviral Res, 2018, Feb;150:112-122 PMID: 29253498
- Ji-Ae Kim, .et al. Favipiravir and Ribavirin Inhibit Replication of Asian and African Strains of Zika Virus in Different Cell Models, Viruses, 2018, Feb; 10(2): 72 PMID: 29425176
- Haejin Chun, .et al. Efficient antiviral co-delivery using polymersomes by controlling the surface density of cell-targeting groups for influenza A virus treatment, Polym Chem, 2018, 9: 2116-2123
- Baz M, .et al. Combination Therapy with Oseltamivir and Favipiravir Delays Mortality but Does Not Prevent Oseltamivir Resistance in Immunodeficient Mice Infected with Pandemic A(H1N1) Influenza Virus, Viruses, 2018, Nov 3;10(11) PMID: 30400276
- Sehee Park, .et al. Combination Effects of Peramivir and Favipiravir against Oseltamivir-Resistant 2009 Pandemic Influenza A(H1N1) Infection in Mice, PLoS One., 2014, 9(7): e101325 PMID: 24992479
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Bepotastine是组胺1（H1）受体的非镇静性选择性拮抗剂。
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Lamivudine是一种有效的核苷类似物逆转录酶抑制剂(nRTI)。
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- Masaaki Toyama, .et al. Novel Neplanocin A Derivatives as Selective Inhibitors of Hepatitis B Virus with a Unique Mechanism of Action, Antimicrob Agents Chemother, 2022, Jun 21;66(6) PMID: 35604213
- Toyama M, .et al. Pyrimidotriazine derivatives as selective inhibitors of HBV capsid assembly, Virus Res, 2019, Oct 2;271:197677 PMID: 31376401
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NS5A 抑制剂
Ledipasvir (GS 5885)是丙型肝炎病毒HCV NS5A蛋白的抑制剂。
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- Sayuri Nitta, .et al. Impact of novel NS5A resistance-associated substitutions of hepatitis C virus detected in treatment-experienced patients, Scientific Reports, 2019, 9: 5722 PMID: 30952914
- Miyayama Y, .et al. Comparative study on the replication of HCV1b genome between wild type and cell culture adaptive mutant in regard to sensitivities against anti-HCV drugs, Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Sayuri Nitta, .et al. Effects of Resistance-Associated NS5A Mutations in Hepatitis C Virus on Viral Production and Susceptibility to Antiviral Reagents, Sci Rep, 2016, 6: 34652 PMID: 27703205
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Trx-1 抑制剂
PX 12抑制缺氧诱导的HIF-1a转录活性（IC50 11 nM）和HT29和MCF-7肿瘤细胞的增殖（IC50分别为1.9和0.9 uM）。
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PTEN 抑制剂
Shikonin一种中草药成分，抑制趋化因子受体功能，抑制人类免疫缺陷病毒1型。
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- Yang J, .et al. Shikonin ameliorates isoproterenol (ISO)-induced myocardial damage through suppressing fibrosis, inflammation, apoptosis and ER stress, Biomed Pharmacother, 2017, Sep;93:1343-1357 PMID: 28753907
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Atovaquone是一种抗原生动物线粒体电子传递抑制剂。
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Hydroxychloroquine Sulfate是一种抗疟疾药，用于治疗系统性红斑狼疮，类风湿性关节炎和其他自身免疫性，炎性和皮肤病性疾病。还可以作为自噬和通行费样受体（TLR）7/9的抑制剂。
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HIV protease 抑制剂
Nelfinavir Mesylate是一种有效的HIV蛋白酶抑制剂，Ki为2 nM。
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HMG-CoA reductase 抑制剂
Pitavastatin Lactone是HMG-CoA还原酶抑制剂。
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HIV-1 protease 抑制剂
Nelfinavir是一种有效的口服生物可利用的人类免疫缺陷病毒HIV-1蛋白酶抑制剂(Ki=2 nM ),广泛用于与HIV逆转录酶抑制剂联合治疗HIV感染。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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Ciclesonide是一种糖皮质激素，用于治疗阻塞性气道疾病。
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Azithromycin Dihydrate是一种酸稳定的口服大环内酯类抗菌药物，在结构上与红霉素有关。
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Chloroquine Phosphate是一种4-氨基喹啉抗疟和抗类风湿药，也可作为ATM活化剂。
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- Egawa Y, .et al. Therapeutic potential of CPI-613 for targeting tumorous mitochondrial energy metabolism and inhibiting autophagy in clear cell sarcoma, PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
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HIV-1 integrase 抑制剂
Bictegravir，也称为GS-9883，是一种有效的，未经增强的，每日一次的HIV-1整合酶链转移抑制剂（INSTI）（IC50-1.6 nM），具有改善的药代动力学和体外耐药性。
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- Michal S Barski, .et al. Structural basis for the inhibition of HTLV-1 integration inferred from cryo-EM deltaretroviral intasome structures, Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
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antiviral
Remdesivir也称为GS-5734，在治疗24小时后，其EC50为30 nM抑制鼠肝炎病毒（MHV），并在HAE细胞中以两个74 nM的EC50阻断HAS细胞中的SARS-CoV和MERS-CoV。
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- Haidar Saify Nabiabad, .et al. Specific delivering of RNAi using Spike's aptamer-functionalized lipid nanoparticles for targeting SARS-CoV-2: A strong anti-Covid drug in a clinical case study, Chem Biol Drug Des, 2022, Feb;99(2):233-246 PMID: 34714580
- Kuoyuan Cheng, .et al. Genome-scale metabolic modeling reveals SARS-CoV-2-induced host metabolic reprogramming and identifies metabolic antiviral targets, bioRxiv, 2021, Jan 28 PMID: 33532779
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HCV NS5A inhibitor
Velpatasvir, also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor.
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HCV NS5A inhibitor
Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
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HIV-1 capsid CTD dimerization inhibitor
Ebselen (SPI-1005) is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen can permeate the blood-brain barrier and inhibit inositol monophosphatase (IMPase). Ebselen is a non-toxic seleno-organic drug with anti-inflammatory and antioxidant properties. Ebselen inhibits QSOX1 enzymatic activity and has anticancer activity .
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HIV protease inhibitor
Darunavir is an HIV protease inhibitor
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serine protease inhibitor
Nafamostat hydrochloride is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma.
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serine protease inhibitor
Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma.
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HCV NS3/4A protease 抑制剂
Danoprevir (RG7227)是HCV NS3/4A丝氨酸蛋白酶的有效抑制剂。
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- Mahim Khan, .et al. Hesperidin identified from Citrus extracts potently inhibits HCV genotype 3a NS3 protease, BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Inês GARCEZ PALHA, .et al. An in vivo translation-reporter system for the study of protein synthesis in zebrafish embryos, Biol Open, 2018, Nov 7 PMID: 30404898
- Hui Shen, .et al. Inhibitory Effects of Caffeic Acid Phenethyl Ester Derivatives on Replication of Hepatitis C Virus, PLoS One., 2013, 8(12): e82299 PMID: 24358168
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HCV NS3-4A protease 抑制剂
Telaprevir (VX-950)被称为蛋白酶抑制剂，可抑制丙型肝炎病毒NS3.4A丝氨酸蛋白酶。
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- Mahim Khan, .et al. Hesperidin identified from Citrus extracts potently inhibits HCV genotype 3a NS3 protease, BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Adita Ayu Permanasari, .et al. An in vitro study of an Artocarpus heterophyllus substance as a hepatitis C antiviral and its combination with current anti-HCV drugs, BMC Complement Med Ther, 2021, Oct 12;21(1):260 PMID: 34641875
- Che C Colpitts, .et al. Hepatitis C virus exploits cyclophilin A to evade PKR, eLife, 2020, 9: e52237 PMID: 32539931
- TS Wahyuni, .et al. Enhancement of Anti-Hepatitis C Virus Activity by the Combination of Chalepin From Ruta Angustifolia and Current Antiviral Drugs, Southeast Asian J Trop Med public health, 2020, 51(1)
- Stefan Bittmann, .et al. TMPRSS2-Inhibitors Play a role in Cell Entry Mechanism of COVID-19: An Insight into Camostat and Nafamostat, J Regen Biol Med, 2020, 2(2):1-3
- Wahyuni TS, .et al. Synergistic anti-hepatitis C virus activity of Ruta angustifolia extract with NS3 protein inhibitor, J Basic Clin Physiol Pharmacol, 2019, Dec 14 PMID: 31837259
- Jacobs CL, .et al. StaPLs: versatile genetically encoded modules for engineering drug-inducible proteins, Nat Methods, 2018, Jul;15(7):523-526 PMID: 29967496
- Apriyanto DR, .et al. Anti-Hepatitis C Virus Activity of a Crude Extract from Longan (Dimocarpus longan Lour.) Leaves, Jpn J Infect Dis, 2016, May 20;69(3):213-20 PMID: 26255732
- Mizuki Yamamoto, .et al. Identification of Nafamostat as a Potent Inhibitor of Middle East Respiratory Syndrome Coronavirus S Protein-Mediated Membrane Fusion Using the Split-Protein-Based Cell-Cell Fusion Assay, Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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serine protease 抑制剂
Nafamostat mesylate是一种抗凝剂。广谱丝氨酸蛋白酶抑制剂。在哮喘小鼠模型中减少嗜酸性粒细胞浸润，肥大细胞活化和气道反应性。
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HIV Protease 抑制剂
Ritonavir是一种蛋白酶抑制剂，具有抗人类免疫缺陷病毒1型(hiv-1)的活性。蛋白酶抑制剂阻断hiv中被称为蛋白酶的部分，利托那韦抑制hiv病毒蛋白酶，这种蛋白酶防止gag-pol多蛋白的裂解，从而产生非感染性的未成熟病毒颗粒。
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HMG-CoA reductase 抑制剂
Rosuvastatin calcium (Crestor)是他汀类药物中的一员，用于治疗高胆固醇及相关疾病，并预防心血管疾病。罗苏伐他汀是一种竞争性HMG-CoA reductase抑制剂，无细胞试验中IC50为11 nM。
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HIV reverse transcriptase 抑制剂
Tenofovir (Viread)属于一类称为核苷逆转录酶抑制剂（NRTIs）的药物。它通过减少血液中的HIV含量起作用。
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HMG-CoA reductase 抑制剂
Rosuvastatin是用于治疗高胆固醇和相关疾病的抑制剂。
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nucleotide reverse transcriptase 抑制剂
Tenofovir Disoproxil Fumarate属于一类抗逆转录病毒药物，其通过与天然底物脱氧腺苷5’-三磷酸盐竞争以及整合到DNA后终止DNA链抑制HIV reverse transcriptase活性。
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- Kazumoto Murata, .et al. Induction of IFN-λ3 as an additional effect of nucleotide, not nucleoside, analogues: a new potential target for HBV infection, Gut, 2018, Feb; 67(2): 362-371 PMID: 27789659
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HIV Protease 抑制剂
Lopinavir (ABT-378)是HIV蛋白酶的抑制剂。
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Mitoxantrone是一种合成的抗肿瘤药蒽二酮（IC50 = 0.42 mM）。
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Ivermectin是一种广谱抗寄生虫阿维菌素药物。
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Prulifloxacin (Pruvel)是氟喹诺酮类药物的一种较旧的合成化学治疗抗生素。与其他氟喹诺酮类药物一样，Prulifloxacin 通过抑制细菌DNA促旋酶来防止细菌DNA复制，转录，修复和重组。
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HCV Protease 抑制剂
Boceprevir (SCH-503034)是一种蛋白酶抑制剂，可用于治疗C型肝炎基因型1。
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- Ueda Y, .et al. Evaluation of preclinical antimalarial drugs, which can overcome direct-acting antivirals-resistant hepatitis C viruses, using the viral reporter assay systems, Virus Res, 2017, May 2;235:37-48 PMID: 28322919
- Shirasaki T, .et al. Impaired interferon signaling in chronic hepatitis C patients with advanced fibrosis via the transforming growth factor beta signaling pathway., Hepatology., 2014, 60(5):1519-30 PMID: 24962339
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Proteasome 抑制剂
PR-171 (Carfilzomib)是四肽环氧酮和选择性蛋白酶体抑制剂。它是环氧霉素的类似物。
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- Ori Kalid, .et al. PTX80, A Novel Compound Targeting the Autophagy Receptor p62/SQSTM1 for Treatment of Cancer, Chem Biol Drug Des, 2022, Mar 24 PMID: 35322538
- Abbas Rahdar, .et al. Pluronic F127/carfilzomib-based nanomicelles as promising nanocarriers: synthesis, characterization, biological, and in silico evaluations, Journal of Molecular Liquids, 2022, 346: 118271
- Sadegh Zarei, .et al. Carfilzomib Induces Drug Resistance in A2780 Ovarian Cancer Cells Through p53-Dependent and Caspase-3 Independent Pathways, J Appl Biotechnol Rep, 2019, June;6(2):45-49
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Moexipril hydrochloride是一种有效的口服活性非巯基血管紧张素转换酶抑制剂(ACE),可作用于高血压和充血性心力衰竭。
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GSK-3 抑制剂
TDZD-8是一种非ATP竞争性GSK-3β抑制剂，IC50为2 μM；对CDK1， casein kinase II， PKA和PKC具有最低限度的抑制效果。
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Carmofur是用作抗肿瘤药的嘧啶类似物。 它是氟尿嘧啶的衍生物。
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Disulfiram是通过抑制乙醛脱氢酶来阻止体内酒精的加工，从而在消耗酒精时引起令人不快的反应。
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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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Histamine Receptor 拮抗剂
Bepotastine Besilate是组胺H1受体激动剂。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Camostat mesylate是胰蛋白酶样的蛋白酶抑制剂，抑制胰蛋白酶和各种炎症性蛋白酶，包括纤溶酶，激肽释放酶和凝血酶。
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Mitoxantrone Dihydrochloride是一种抗病毒，抗菌，抗原生动物，免疫调节和抗肿瘤细胞抑制性蒽醌衍生物。
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HMG-CoA reductase 抑制剂
Pitavastatin calcium (Livalo)是HMGCR（HMG-CoA还原酶）酶的竞争性抑制剂，可降低LDL胆固醇的合成。
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- Weizhen Chen, .et al. An improved osseointegration of metal implants by pitavastatin loaded multilayer films with osteogenic and angiogenic properties, Biomaterials, 2021, 280:121260 PMID: 34823885
- Karis Tutuska, .et al. Statin as anti-cancer therapy in autochthonous T-lymphomas expressing stabilized gain-of-function mutant p53 proteins, Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
- D Jarmuzek, .et al. Phototransformations of pitavastatin - The inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, J Photochem Photobiol A Chem, 2019, November
- Marwan Ibrahim Abdullah, .et al. Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells, Sci Rep, 2017, 7: 8090 PMID: 28808351
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Praziquantel (Biltricide)是针对所有血吸虫物种的高效驱虫药。
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Azithromycin (Zithromax)是一种氮杂内酯类抗生素，可抑制革兰氏阴性细菌（如流感嗜血杆菌）的生长。
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Indinavir sulfate是HIV-1蛋白酶抑制剂。
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