Plasmodium Inhibitor

Quinine dihydrochloride (Standard) is the analytical standard of Quinine dihydrochloride (HY-D0143A). This product is intended for research and analytical applications. Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark, possessing various biological activities including antimalarial, antidengue virus (DENV), and anticancer properties. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (K_Ca5.1) channel currents evoked by voltage pulses to +100 mV with an IC₅₀ of 169 μM.

Chloroquine-d₅ (diphosphate) is the deuterium labeled Chloroquine (phosphate). Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

Cletoquine-d₄ is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment.

19,20-Epoxycytochalasin C, a cytochalasin, is a fungal metabolite from Nemania sp. 19,20-Epoxycytochalasin C shows potent in vitro antiplasmodial activity and phytotoxicity.

Nitidanin ((±)-Nitidanin) is an antimalarial and antiviral compound that can be isolated from the wood of Xanthoxylum nitidun D. C. Nitidanin is shows IC₅₀ values of 21.2 and 18.4 μM for D6 and W2 clones of Plasmodium falciparum, respectively. Nitidanin can be used for the research of malaria and virus infection.

Asperaculane B is a fungal metabolite against P. falciparum transmission with an IC₅₀ of 7.89 µM. Asperaculane B also inhibits the development of asexual P. falciparum with IC₅₀ of 3 µM, and it is nontoxic to human cells.

Shinjulactone M is a quassinoid isolated from various parts of Ailanthus species. Ailanthus, an important genus of the Simaroubaceae family, can be used as an febrifuge (antimalarial) and anthelmintic, and is given for the research of chronic bronchitis, epilepsy and asthma.

Sulfadiazine-¹³C₆ is a labeled Sulfadiazine (HY-B0273). Sulfadiazine is an orally active sulfonamide antibiotic. Sulfadiazine competitively inhibits p-aminobenzoic acid in the folic-acid-metabolism cycle, inhibiting multiplication of most Gram-positive and many Gram-negative bacteria. Sulfadiazine persists in soil long-term, and exerts selective pressure for sulfonamide-resistant microbial populations. Sulfadiazine targets Toxoplasma gondii DHPS enzyme. Sulfadiazine can be used for the research of congenital toxoplasmosis and bacterial infection.

Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC₅₀=155 nM), 3D7 strain (EC₅₀=136 nM). Antimalarial agent 12 has CC₅₀ values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli.

P-orlandin, a fungal metabolite, prevents FREP1 from binding to gametocytes or ookinetes. P-orlandin effectively inhibits P. falciparum infection in mosquitoes.

Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma.

Sulfadoxine-d₄ is the deuterium labeled Sulfadoxine. Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.

Polyketomycin is a tetracyclic quinone glycoside antibiotic isolated from Streptomyces sp. or Streptomyces diastatochromogenes. Polyketomycin inhibits growth of Gram-positive bacteria, and its MIC values is less than 0.2 µg/mL. Polyketomycin has antibacterial, anticancer, antimalarial activities.

7-Methoxy-β-carboline-1-propionic acid (compound 46) is a cytotoxic and antimalarial compound. 7-Methoxy-β-carboline-1-propionic acid can be extracted from the roots of Eurycoma longifolia.

6-O-Methacrylate, a trilobolide, is isolated from the leaves of Wedelia trilobata. 6-O-Methacrylate displays marked antimalarial activity, with IC₅₀ of 8.9 μg/mL against P. falciparum parasite. 6-O-Methacrylate also has anti-tobacco mosaic virus (TMV) activity.

Antimalarial agent 18 is an potent antimalarial agent, based on electronic, highly lipophilic and siderophoric properties. Antimalarial agent 18 belongs to acyloxymethyl series, as a fosmidomycin surrogate, which is potent IspC inhibitor against the non-mevalonate isoprenoid biosynthesis pathway. Antimalarial agent 18 inhibits P. falciparum (IC₅₀=50 nM) and A. baumanii (IC₅₀=390 nM).

Lettowienolide, a geranylbenzoquinonoid, exhibits mild in vitro activity against the Plasmodium falciparum malaria parasite (IC₅₀~20 μg/mL).

Purine phosphoribosyltransferase-IN-1 (Compound (S,R)-48) is a potent inhibitor of the Plasmodium falciparum (Pf), P. vivax (Pv) and Trypanosoma brucei (Tbr) 6-oxopurine purine phosphoribosyltransferases (PRTs), with K_i values of 50, 20, and 2 nM, respectively.

Sulfalene-¹³C₆ is the ¹³C₆ labeled Sulfalene. Sulfalene (Sulfametopyrazine) is an antimalarial agent. Sulfalene is also a long-acting sulfonamide antibacterial.

Antimalarial agent 3 shows nanomolar antiplasmodial activity (IC₅₀ = 0.035 μM) and has a very high selectivity index with respect to mammalian cells.