Valacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. IC50 Value: 2.9 microg/ml (for HSV-1 W)[4]. Target: HSV infectionin vitro: VACV uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 +/- 0.06 mM and 23.34 +/- 0.36 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro [5]. in vivo: For treatment of a first episode of genital herpes, a large comparative trial has shown that valacyclovir (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day[1]. The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1,000 mg of valacyclovir three times a day [2]. EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b.i.d., 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA [3].Clinical trial: Evaluation of Valaciclovir in Patients with Chickenpox. Phage3
Vilobelimab (CaCP-29, IFX-1) is a monoclonal anti-C5a antibody to the allergen C5a, a pro-inflammatory complement division product that plays a central role in mediating organ dysfunction. Vilobelimab acts as a C5a inhibitor, inhibiting neutrophil activation, chemotaxis, and reducing inflammatory signalling, and may be used in studies related to sepsis, COVID-19, etc[1].
Antibacterial agent 158 (compound 6c), a Micrococcin analogue, and is effective against impetigo and C. difficile infection (CDI)[1].
β-Lactamase-IN-5 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 720. β-Lactamase-IN-5 can be used for the research of bacterial infections[1].
Influenza virus-IN-7 (Example 16) is an orally active cap-dependent endonuclease inhibitor that can be used for the research of influenza viral infectious diseases[1].
IDO-IN-18 (Compound 00815) is an IDO inhibitor. IDO-IN-18 can be used for research of immunosuppression associated infectious or cancer diseases[1].
Fascaplysin is an antimicrobial and cytotoxic red pigment, that can come from the marine sponge (Fascaplysinopsis sp.). Fascaplysin has been synthesized in seven steps from indole (65% yield). Fascaplysin can induces apoptosis and autophagy in human leukemia HL-60 cells. Fascaplysin shows anti-tumor activity[1][2].
(E)-Coniferyl alcohol is the isomer of Coniferyl alcohol. Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbenoids and coumarin. Coniferyl alcohol specifically inhibits fungal growth[1][2].
Furomollugin is a natural product with antioxidant and antibacterial activities, can be isolated from Rubia cordifolia. Furomollugin lacks potent anti-tyrosinase activity, but also exhibits significant anticancer property[1].
11-Keto fusidic acid shows strong antibacterial activity toward Staphylococcus aureus with an MIC value of 0.078 μg/mL.
Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
2-Phenylethanol-d5 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
2-Phenylethyl isothiocyanate is a potent antifungal agent. 2-Phenylethyl isothiocyanate significantly inhibited spore germination and mycelial growth of Alternaria alternata, with a MIC (minimum inhibitory concentration) of 1.22 mM. The antifungal effect of 2-Phenylethyl isothiocyanate against Alternaria alternata might be via reduction in toxin content and breakdown of cell membrane integrity[1][2].
2,6-Dihydroxy-4-methoxyacetophenone is a phytoalexin, that can be isolated from the root tissue of Sanguisorba minor. 2,6-Dihydroxy-4-methoxyacetophenone exhibits antifungal activity. 2,6-Dihydroxy-4-methoxyacetophenone is a strong germination inhibitor on B. cinerea[1].
Squalamine(MSI-1256) is an aminosterol compound with potent broad spectrum antiviral activity.IC50 value: Target: in vitro: squalamine can strongly displace membrane-bound cationic proteins such as Rac1, a ρ-GTPase recruited to the inner leaflet of the eukaryotic cytoplasmic membrane for the actin remodeling necessary for endocytosis. At concentrations between 20 and 60 μg/mL, squalamine has been shown to inhibit a broad array of growth factor-induced, actin-dependent responses in endothelial cells, including cell migration, cell division, and vascular tube formation in a 3D matrix [1]. Squalamine effectively inhibited HBV replication in human primary hepatocytes when added either during the initial exposure of virus to the cells or at 24 h after infection. A similar study was performed to evaluate the effect of squalamine on the replication of HDV. Squalamine was introduced at 20 μg/mL during HDV exposure, and the effects were measured at day 7 when total RNA was extracted and assayed for HDV RNA sequences [1]. in vivo: one time daily treatment with squalamine (15 or 30 mg/kg per d s.c.) was started beginning on day 1 or 2 after viral administration and continuing until day 8 or 9, respectively. Survival was monitored, and animals that remained alive by day 21 were considered cured [1].
Amphotericin B methyl ester is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester disrupts HIV-1 particle production and potently inhibits HIV-1 replication[1][2].
Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells[1][2].
Carbocisteine, a mucolytic agent, can be used for the research of chronic obstructive pulmonary disease (COPD)[1].
Thalifoline is an alkaloid isolated from the New Caledonian plant Cryptocarya longifolia[1] and displays antifungal activity[2].
Zika virus-IN-2 (Compd 3) is a Zika virus inhibitor, with an EC50 of 7.4 μM [1].
SDZ 224-015 is an orally active inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1. SDZ 224-015 possesses anti-COVID-19 activity, targeting Mpro (IC50 of 30 nM)[1][2].
4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research[1][2][3].
Monooctyl phthalate-d4 (Mono-n-octyl phthalate-d4) is a deuterium labeled Monooctyl phthalate (HY-133671). Monooctyl phthalate (Mono-n-octyl phthalate) exhibits antimycobacterial activity with a MIC of 20 μg/mL[1][2].
Actinomycin D inhibits DNA repair with an IC50 of 0.42 μM.
Pymetrozine is a feeding inhibitor of Homoptera, in preventing transmission of cauliflower mosaic caulimovirus by the aphid species Myzus persicae (Sulzer).
Paecilaminol (FKI-0550) is potent NADH-fumarate reductase inhibitor. Paecilaminol exhibits an IC50 value of 5.1 μM against Ascaris suum NADH-fumarate reductase[1].
Temporin L is a potent antimicrobial peptide and is active against Gram-negative bacteria and yeast strains. Temporin L also has antiendotoxin properties[1][2].
NS1-IN-1 (compound 3) is a potent NS1 inhibitor. NS1 is a major influenza A virus virulence factor that inhibits host gene expression. NS1-IN-1 decreases viral protein levels, contributing to the reduction of virus replication. NS1-IN-1 shows antiviral activity by repressing the activity of mTORC1 in a TSC1-TSC2-dependent manner[1].
Toltrazuril sulfone is an antiprotozoal agent that acts upon Coccidia parasites.IC50 Value:Target: AntiparasiticPonazuril (INN, Toltrazuril sulfone), sold by the Bayer Corporation under the trade name Marquis, is a drug currently approved for the treatment of equine protozoal myeloencephalitis in horses, caused by Sarcocystis neurona. More recently, veterinarians have been preparing a formulary version of the medication for use in small animals such as cats and dogs against coccidia, an intestinal parasite. Coccidia treatment is far shorter than treatment for EPM. Ponazuril (INN, Toltrazuril sulfone) is useful for Antiprotozoal.