Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution[1][2].
Isobellidifolin, a xanthone, is a free radical scavenger and antioxidant compound. Isobellidifolin has potent antifungal effect[1].
Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated, immunoglobulin G1 (IgG1) anti-OX40 monoclonal antibody. Rocatinlimab can be used for the research of atopic dermatitis (AD)[1].
Biapenem is a parenteral carbapenem antibacterial agent with a broad spectrum.Target: AntibacterialBiapenem is a carbapenem antibiotic of in vitro antibacterial activity encompassing many Gramnegative and Gram-positive aerobic and anaerobic bacteria, including species producing β-lactamases. Biapenem is more stable than imipenem, mero-penem and panipenem to hydrolysis by human renal dihydropeptidase-I (DHP-I), and therefore does not require the coadministration of a DHP-I inhibitor. In randomised, nonblind or double-blind clinical trials, biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/ cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections.
2,3-Butanediol-d8 is the deuterium labeled 2,3-Butanediol[1]. 2,3-Butanediol is a butanediol derived from the bioconversion of natural resources[2].
4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity.
Anti-infective agent 2 (compound 3k) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL[1].
Friulimicin D, a lipopeptide antibiotic, like Friulimicin B, is isolated from the actinomycete Actinoplanes friuliensis[1].
2-Hydroxy-1-methoxyanthraquinone could be isolated from the stem bark of Morinda lucida Benth. (Rubiaceae) and possesses antibacterial activity[1].
Albendazole sulfone is a metabolite of Albendazole, and exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes[1][2].
Cap-dependent endonuclease-IN-1 is an orally active cap-dependent endonuclease inhibitor with high potency. Cap-dependent endonuclease-IN-1 can be used for the research of influenza[1][2].
(E)-3,4-Dimethoxycinnamyl alcohol is an antimutagenic. (E)-3,4-Dimethoxycinnamyl alcohol has antimutagenic activity against furylfuramide, Trp-P-1, and activated Trp-P-1[1].
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis[1].
Garenoxacin-d4 (BMS284756-d4) is the deuterium labeled Garenoxacin. Garenoxacin (BMS284756) is a quinolone antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections[1][2].
Varioxepine A is a 3H-oxepine-containing alkaloid with a new oxa-cage found in the marine algal-derived endophytic fungus Paecilomyces variotii. Varioxepine A inhibits plant pathogenic fungus Fusarium graminearum[1].
Duramycin (Moli1901;Lancovutide) is a cyclic peptide lantibiotic derived from Streptomyces cinnamoneuma. Duramycin stimulates chloride secretion in airway epithelium and has the potential for cystic fibrosis treatment. Duramycin interacts with phosphatidylethanolamine (PE) and has antibacterial, antiviral effects[1][2].
Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Efrotomycin is an orally active antibiotic. Efrotomycin can be isolated from the Streptomyces Lactamdurans. Efrotomycin has insignificant effect on Salmonella typhimurium quantity, duration, shedding rate, and antimicrobial susceptibility in infected pigs[1][2].
Norstictic acid is a potent and selective allossteric transcriptional regulator. Norstictic acid shows anticancer activity. Norstictic acid shows antioxidant activity and antimicrobial activity[1][2][3][4].
8CN, a 2-amino-thiophene derivative, has anti-leishmanial activity. 8CN can be used in research of Leishmaniasis[1].
Omadacycline is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.IC50 Value:Target: Antibacterialin vitro: in vivo: Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
Cecropin A (1-7)-Melittin A (2-9) is an antimicrobial peptide with antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative aerobic bacteria, as well as antimalarial activity, without the adverse hemolytic properties of bee venom peptides[1].
Valacyclovir hydrochloride hydrate is a potent antiviral agent. Valacyclovir hydrochloride hydrate can be used in the management of herpes simplex, herpes zoster and herpes B. Valacyclovir hydrochloride hydrate can be formulate ocular inserts for the treatment of ocular herpes. Valacyclovir hydrochloride hydrate is a prodrug and can be rapidly converted into acyclovir in vivo[1][2].
Metaldehyde-d16 is a deuterium labeled Metaldehyde (HY-B1870).
Urtoxazumab (TMA-15) is a humanized monoclonal antibody against Shiga toxin (Stx) 2[1].
Vincetoxicoside B, isolated from Polygonum paleaceum Wall, shows antifungal activity[1].
7-O-Demethyl rapamycin, a derivative rapamycin (HY-10219), has antifungal activity and also immunosuppressant properties. 7-O-Demethyl rapamycin has useful tumor cell growth-inhibiting activity[1].
L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
Antibacterial agent 96 (compound 4k) is a potent antibacterial agent. Antibacterial agent 96 shows antitubercular activity against drug-susceptible and multidrug-resistantMycobacterium tuberculosis (M. tuberculosis) strains. Antibacterial agent 96 shows toxicity to HepG2 and Vero cells[1].