Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity[1][2][3].
Sancycline (Bonomycin; 6-Demethyl-6-deoxytetracycline) hydrochloride is a semi-synthetic tetracycline antibiotic[1].
Apigravin is a potent antibacterial agent. Apigravin shows antibacterial activity against Bacillus subtilis with a MIC value of 61 μM[1].
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability[1].
Anti-MRSA agent 1 (Compound 13d) is a wonderful MRSA (MIC = 0.5 μg/mL) inhibitor. Anti-MRSA agent 1 (Compound 13d) could effectually relieve the development of MRSA resistance[1].
HBV-IN-7 is a potent HBV inhibitor with an EC50 of 7 nM (WO2021213445A1, compound 5)[1].
Isatin-β-thiosemicarbazone is a potent anti-poxvirus agent (including monkeypox virus, orthopoxvirus, vaccinia virus, etc). Isatin-β-thiosemicarbazone also is a potent herpes simplex virus (HSV) inhibitor. Isatin-β-thiosemicarbazone exhibits
MGB-BP-3 is an antibiotic that has been shown to be active against a broad range of important multi-resistant Gram-positive pathogens.
Mycophenolic acid sodium is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid sodium is an immunosuppressive agent. Antiangiogenic and antitumor effects[1][2].
Acyclovir, a molecule tailored to inactivate the thymidine kinase of the herpesvirus, is a guanosine analogue antiviral drug. It is a drug for HSV infection by GlaxoSmithKline.IC50 Value: 0.53-0.75 uM [3]Target: HSVin vitro: Acyclovir sensitivity was determined in a plaque-reduction assay in Vero cells. IC50 Values were consistently 2-3 fold lower in B2 compared with the H strain of Vero cells. HSV Type 2 strains were 2-10-fold less sensitive than Type 1 strains [2]. in vivo: two patients experienced a recurrence during treatment with oral acyclovir (200 mg 4 times daily) for up to 12 weeks, compared with nine during placebo treatment (P = 0.016). There was no difference between acyclovir and placebo in the time to the next recurrence following completion of treatment [3]. low-dose oral acyclovirmay be effective in the prevention of HSV infection during OKT3 treatment of seropositive patients. Continuation of acyclovir prophylaxis for two to four weeks following the conclusion of OKT3 therapy may prevent occurrence of delayed infections [4].Clinical trial: Acyclovir to Treat Patients Co-infected With HIV and Herpes Viruses in Uganda. Phage2
Emtricitabine triphosphate tetrasodium salt is the tetrasodium salt form of Emtricitabine triphosphate (HY-131596). However，Emtricitabine triphosphate ((-)-Emtricitabine triphosphate) is the phosphorylated anabolite of Emtricitabine (HY-17427)，a nucleoside reverse transcriptase inhibitor，targeting to HIV and HBV[1].
Fosravuconazole is a prodrug of ravuconazole, with antifungal activity.
Influenza NP (147-155) is a Kd restricted epitope from influenza nucleoprotein[1].
Enzaplatovir (BTA-585, BTA-C585) is an orally bioavailable RSV fusion protein inhibitor for the treatment of respiratory syncytial virus infections. RSV Infection Phase 2 Discontinued
Gallinamide A is a potent inhibitor of cathepsin L with an IC50 value of 17.6 pM.
Boscalid is an anti-fungal agent. Boscalid is a succinate dehydrogenase (SDH) inhibitor[1].
18BIOder is a neuroprotective inhibitor of GSK-3β, highly selectively inhibiting HIV-1. It is the second generation derivative of 6BIO.
Djalonensone, isolated from the roots of Anthocleista djalonensis (Loganiaceae), is an important taxonomic marker of the plant species[1].
1,4-Epidioxybisabola-2,10-dien-9-one is a 1,4-epidioxy-bisabola-2,12-diene derivate, which can be isolated from Curcuma longa L. 1,4-Epidioxybisabola-2,10-dien-9-one exhibits antiviral activity against influenza virus A/PR/8/34 (H1N1) in the MDCK cell line with an IC50 of 16.79 ± 4.03 μg/mL[1].
Itraconazole-d9 is the deuterium labeled Itraconazole[1]. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[2][3][4][5].
ATV006 is a potent, orally active antiviral agent and ester prodrugs of GS-441524. ATV006 inhibits the replication of SARS-CoV-2 and its variants. ATV006 can be used for SARS-CoV-2 research[1].
Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5].
Tetramycin B (4-Hydroxytetramycin A) is a polyene macrolide antibiotic, an antifungal active compound isolated from Streptomyces hygrospinosus var. Beijingensis. The antifungal activity of Tetramycin B is higher than that of Tetramycin A, and the C-4 hydroxyl of Tetramycin B plays an important role in its biological activity[1].
Ronidazole is an antiprotozoal agent.Target: AntiparasiticRonidazole is an antiprotozoal agent used in veterinary medicine. It may also have use for the treatment of Tritrichomonas foetus infection in cats. Ronidazole kills T foetus at concentrations > 0.1 μg/mL in vitro. Ronidazole (30 or 50 mg/kg) cures T foetus infection for follow-up durations of 21 to 30 weeks after treatment in 10/10 cats [1].
Yimitasvir (Emitasvir) is an orally active hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor. Yimitasvir can be used for research of chronic HCV infection[1].
Usnic acid, a lichen-derived secondary metabolite, has a unique dibenzofuran skeleton. Usnic acid has excellent anticancer and antimicrobial properties. Usnic acid significantly inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1[1].
Cap-dependent endonuclease-IN-19 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-19 is a spirocyclic pyridone derivative. Cap-dependent endonuclease-IN-19 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN111410661A, compound 1)[1].
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
Sulfamonomethoxine-13C6 is the 13C6 labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.