c-16

PAF (C16) is a potent MAPK and MEK ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.

Lyso-PAF C-16 is a biologically inactive precursor of platelet-activating factor (PAF).

Methylcarbamyl PAF C-16 (Carbamyl-PAF) is a platelet-activating factor analogue with PAF agonist properties, activating inflammation in pregnancy tissues and promoting preterm birth.

PAF C-16 is a naturally occurring phospholipid produced upon stimulation through two distinct pathways known as the remodeling and 'de novo' pathways. It is a potent mediator of neutrophil migration and the production of reactive oxygen species and IL-6. Pathological processes involving PAF include necrotizing enterocolitis

2-O-methyl PAF C-16 is a synthetic analog of platelet-activating factor (PAF) featuring a methyl group attached via an ether linkage at the sn-2 position. While the specific biological activities of 2-O-methyl PAF C-16 remain undercharacterized, studies with its C-18 counterpart have demonstrated its ability to modulate various biological processes. These processes include reducing plasma membrane fluidity and hindering the invasiveness of tumor cells in embryonic chick hearts. Furthermore, in rat astrocytes, the C-18 analog prompts the release of significant amounts of nitric oxide (NO) through a mechanism that involves the activation of nitric oxide synthase (NOS).

2-O-Ethyl PAF C-16, a homolog of Platelet-activating Factor (PAF) and competitive ligand for the Platelet-activating Factor Receptor (PAFR), inhibits the binding of PAF antagonist WEB 2086 to PAFR with an IC50 of 21 nM [1].

Dihomo-γ-Linolenoyl PAF C-16 is a PAF analogue that incorporates dihomo-γ-linolenoate at the sn-2 position instead of the acetate moiety found in PAF C-16.

c-Met-IN-16, a c-Met inhibitor, is utilized in cancer research.

16-O-Acetylpolyporenic acid C is a natural product and can be used as a standard reference.

23-Aldehyde-16-O-angeloybarringtogenol C (compound 7) is an acid hydrolysis product obtained through oxidative alkaline degradation of camellia seed saponins, which exhibit potential quinone oxidoreductase inducing activity.

LHC-165 is an agonist of TLR7. It also has the potential to treat solid tumors.

HNC-1664 is an orally active inhibitor of RNA-dependent RNA polymerase (RdRP). It exhibits broad-spectrum antiviral activity against coronaviruses, including SARS-CoV-2 wild type and its variants (XBB.1.18, HK.3.1, BF.7.14, BA.1, HCoV-229E, HCoV-OC43), as well as arenaviruses. HNC-1664 also demonstrates anti-infective efficacy in a mouse model infected with the SARS-CoV-2 Delta variant.

AC-165024 is a biochemical.

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

TC-1698 dihydrochloride is a selective nicotinic α7 receptor agonist that also displays weak partial agonist antagonist activity at β-subunit-containing receptors. This product is a neuroprotectant.

VPC-16606 is a potent and selective inhibitor of ERα-dependent cell growth and gene expression. VPC-16606 prevents the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner.

NPC-16731 is a Bradykinin antagonist.

OPC-163493 is an orally active, liver-targeted mitochondrial uncoupling agent that diminishes Δψ (delta psi) and mitochondrial ROS (reactive oxygen species) production. This compound demonstrates antidiabetic properties and cardiovascular benefits, including lowering blood pressure, prolonging survival, and enhancing renal function in a rat model of stroke hypertension [1].

RC-160 [Lys(Boc)], an 8-amino acid peptide, functions as a somatostatin analog [1].

NRC-16 is a biologically active peptide with characteristics similar to pleurocidin, a cationic antimicrobial peptide (cationic AMP).

ETC-168 is a selective, orally active MNK inhibitor with IC50 values of 23 nM for MNK1 and 43 nM for MNK2. It demonstrates antiproliferative efficacy both in vivo and in vitro [1].

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

Cytarabine hydrochloride (Ara-C hydrochloride) is a nucleoside analog that causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC 50 of 16 nM. Cytarabine hydrochloride has antiviral effects against HSV.

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.