sepsis

Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4). Cl-amidine hydrochloride induces apoptosis in cancer cells and it also induces microRNA (miR)-16 in vitro causing cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation. It improves survival in a murine sepsis model.

Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.

DL-Syringaresinol ( (±)-Syringaresinol) is a lignan from ginseng berries with anti-inflammatory, antioxidant, analgesic and weak anti-mycobacterial activities.DL-Syringaresinol can delay oxidative stress-induced skin aging through autophagy, alleviate oxaliplatin-induced neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses. neuropathic pain and sepsis-induced cardiac dysfunction by inhibiting inflammatory responses.

Ceftriaxone Sodium is a broad-spectrum β-lactam tertiary cephalosporin antibiotic with anti-inflammatory, antitumor, antibacterial, and antioxidant activities.Ceftriaxone Sodium is a covalent GSK3β and Aurora B inhibitor used in the study of sepsis and infective endocarditis.

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb-/-) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb-/- macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb-/- mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

STC314 is an anti-infective agent that reverses organ damage caused by excessive immune response by neutralizing extracellular histones and neutrophil trapping networks, and can be used in the study of sepsis and acute respiratory distress syndrome (ARDS).STC314 protects the stability of lipid bilayers, and inhibits platelet activation and erythrocyte damage.STC314 is also used in the study of prostate cancer.Nardeterol HCl is a selective kappa agonist with analgesic activity.

Paeonoside, found in P. suffruticosa, is biologically active and can promote wound healing and migration during osteoblast differentiation. Paeonoside has certain antidiabetic activity and may prevent sepsis and death from sepsis. Paeonoside has no cytotoxic effect on preosteoblasts of MC3T3-E1 cells, significantly restores the wound area and promotes cell migration and alkaline phosphatase (ALP) staining and its activity in a dose-dependent manner.

Ac-Pro-Gly-Pro-OH is an acetyl-modified tripeptide compound that acts as a CXCR2 agonist.Ac-Pro-Gly-Pro-OH exhibits bactericidal and anti-inflammatory activity, inhibits apoptosis of immune cells, and suppresses the production of pro-inflammatory cytokines.Ac-Pro-Gly-Pro-OH has been used in the study of sepsis and inflammation in the lungs.

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

Tamarixetin (4'-O-Methyl Quercetin) (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin, with anti-inflammatory and anti-oxidative effects. Tamarixetin protects against cardiac hypertrophy.

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride (Pilofrin) mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict.

Norvancomycin hydrochloride (Desmethyl-vancomycin hydrochloride) is used as a treatment for endocarditis, osteomyelitis, pneumonia, sepsis, or soft tissue infections caused by Staphylococcus.

Edobacomab (E5), a monoclonal IgM antibody targeting endotoxin, is utilized in the study of sepsis stemming from Gram-negative bacterial infections [1].

Alpha-Chaconine has anti-inflammatory effect, associated with the suppression of AP-1, and supports its possible therapeutic role for the treatment of sepsis. Alpha-Chaconine also has cytotoxic effects.

Afelimomab (MAK 195F), a F(ab')2 fragment of an anti-tumor necrosis factor monoclonal antibody, is utilized in sepsis research [1].

Senkyunolide G and senkyunolide I could serve as pharmacokinetic markers for sepsis care.

Drotrecogin alfa (activated) (DrotAA), a recombinant human activated protein C (APC), mitigates smoke-induced elevations in pulmonary microvascular permeability and proinflammatory cytokine IL-1β levels in rats. It also inhibits coagulation and inflammation while enhancing fibrinolysis. Drotrecogin alfa (activated) is applicable in severe sepsis research [1] [2].

RIPK1-IN-16 is an orally active, potent RIPK1 inhibitor that mitigates excessive inflammation via inhibition of RIPK1-mediated necroptosis in vivo. It shields mice from TNF-induced systemic inflammatory response syndrome and sepsis [1].

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].

1-Heptadecanoyl-2-hydroxy-sn-glycero-3-phosphocholine, an endogenous metabolite found in blood, is utilized in the study of pregnancy and sepsis [1] [2] [3].

PDE4-IN-9 (Compound 5j) is a potent PDE4 inhibitor. In vitro enzyme assay, the IC 50 value of PDE4-IN-9 against PDE4 is 1.4 μM which is lower than 2.0 μM of parent rolipram. PDE4-IN-9 also shows good in vivo activity in LPS-induced animal models of asthma/COPD and sepsis [1].

AMPR-22, an antimicrobial peptide, binds to bacterial membranes to induce permeabilization and has demonstrated efficacy in a murine sepsis model induced by multidrug-resistant (MDR) strains [1].

HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/NLRP3 signaling pathway. This compound demonstrates promising anti-inflammatory and anti-sepsis properties, particularly in the context of renal injury [1].

ALPK1-IN-3,serves as an ALPK1 inhibitor that dampens proinflammatory gene expression in the kidney and enhances survival in animal models of sepsis-induced acute kidney injury [1].

Pagibaximab, a chimeric IgG1 antibody, targets the lipoteichoic acid on the surfaces of S. aureus and S. epidermidis, and is utilized for the prevention of staphylococcal sepsis [1].

Nebacumab (HA-1A), a monoclonal antibody, targets the lipid A component of endotoxin and has potential applications in sepsis research [1] [2].

CAP18 (rabbit) is a 37 amino acid antimicrobial peptide derived from rabbit granulocytes. It exhibits extensive antimicrobial activity against both Gram-positive (IC50, 130-200 nM) and Gram-negative (IC50, 20-100 nM) bacteria. Thus, CAP18 (rabbit) holds promise for the study and advancement of bacterial sepsis research.

Dicloxacillin Sodium hydrate is a narrow-spectrum β-Lactam antibiotic of the penicillin class, used to treat infections caused by susceptible Gram-positive bacteria.

An antibiotic produced by Streptomyces fradiae.

Fosfomycin calcium (Phosphomycin calcium salt) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis.

SIRT5 inhibitor 7 (compound 58), a selective and substrate-competitive SIRT5 inhibitor, exhibits anti-inflammatory properties by modulating protein succinylation and attenuating pro-inflammatory cytokine release. It demonstrates renal protective effects and is active in vivo, showing efficacy in AKI mouse models subjected to lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury [1].

Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when administered orally. It has been shown to be effective in vivo using a mouse model of staphylococcal sepsis [1].

Vipoglanstat is a prostaglandin E synthase inhibitor and an anti-inflammatory. Vipoglanstat ameliorates leukocyte infiltration and lung injury resulting from both endotoxin-induced and sepsis-induced lung injury.

Enrofloxacin-d5 is intended for use as an internal standard for the quantification of enrofloxacin by GC- or LC-MS. Enrofloxacin is a fluoroquinolone antibiotic. It is active against panels of Campylobacter, E. coli, and Salmonella isolates (mean MIC50s = 0.06, 0.5, and 0.03 µg/ml, respectively). It is also active against equine isolates of L. intracellularis (MICs = 0.125-0.5 µg/ml). Enrofloxacin inhibits bacterial DNA gyrase. In vivo, enrofloxacin (10 mg/kg) increases survival in a mouse model of enteropathogenic E. coli-induced sepsis. Formulations containing enrofloxacin have been used in the treatment of veterinary bacterial infections.

Tauro-ω-muricholic acid sodium (TωMCA sodium) is an analogue of tauro-α-muricholic acid, a bile acid of hepatic origin. Tauro-ω-muricholic acid sodium can be used as a serum marker for early onset neonatal sepsis (EOS) and biliary stasis.

CTCE-0214, a chemokine CXC receptor 4 (CXCR4) agonist and SDF-1α (stromal cell-derived factor-1α) peptide analog, exhibits anti-inflammatory properties. It is applicable in the research of inflammation, sepsis, and systemic inflammatory syndromes [1] [2] [3].

BET-IN-7 (Compound 1) is a highly effective BET inhibitor, possessing a K i of 12.27 μM and a K d of 89.3 μM. It exhibits promising properties for sepsis-related research [1].

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). α7 nAchR-JAK2-STAT3 agonist 1 has been shown to have a positive effect on iNOS, IL-1β and IL-1β in murine macrophages RAW264.7. α7 nAchR-JAK2-STAT3 agonist 1 was effective in inhibiting the expression of iNOS, IL-1β and IL-6 in mouse macrophages. α7 nAchR-JAK2-STAT3 agonist 1 inhibited LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 agonist 1 was able to be used to study sepsis.

BBS-4 is a selective and potent inducible nitric oxide synthase (NOS2) dimerization inhibitor (IC50: 0.49 nM), and BBS-4 protects mice from the cardiovascular dysfunction of sepsis.

BET-IN-8 (Compound 27) is a potent inhibitor of BET (Ki: 0.83 μM, Kd: 0.571 μM), which ameliorates LPS-induced sepsis in vivo.BET-IN-8 has shown potential in sepsis.

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

M62812 (free base), a Toll-like receptor 4 (TLR4) signal transduction inhibitor, suppresses activation of endothelial cells and leukocytes and prevents lethal septic shock in mice. It is utilized in sepsis research [1].

Mitogen-activated protein kinase 1 (MAPK1) activates the p38/NF-κB pathway and regulates cellular processes in sepsis-associated diseases. Its catalytic action phosphorylates substrate proteins, serving as a regulatory switch for their activity [1].

F1, an anti-inflammatory peptide, incorporates the HIV-1 Tat protein transduction domain linked with a 15-amino acid sequence from residues 46-60 of the inhibitor of NF-κB kinase-interacting peptide (IKIP). It effectively blocks LPS-induced phosphorylation of IκB kinase α (IKKα) and IKKβ, along with the nuclear translocation of NF-κB (p65) in mouse peritoneal macrophages at 5 µM concentration. F1, administered at 5 mg/kg in vivo, significantly reduces IL-6, TNF-α, and IL-1β serum levels and enhances survival in a mouse sepsis model induced by LPS.

5-Androstenetriol, a steroid and active metabolite of dehydroepiandrosterone (DHEA), demonstrates significant therapeutic effects. Administered at 0.75 mg/25 g body weight, it mitigates radiation-induced mortality and facilitates hematopoietic recovery from surviving stem cells in mice. Moreover, a dosage of 40 mg/kg enhances survival rates in rats subjected to surgical trauma-induced sepsis. Additionally, elevated urinary levels of 5-androstenetriol are observed in women suffering from androgenic alopecia.

Aldose reductase-IN-3 (Compound 5) is an effective and moderately selective aldose reductase (AR) inhibitor (IC50=3.99 μ M). Aldose reductase is a molecular target involved in various inflammatory diseases (including sepsis). Aldose reductase-IN-3 has research potential in sepsis.

STING-IN-5, a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, significantly suppresses lipopolysaccharide (LPS)-induced nitric oxide (NO) synthesis in macrophages, exhibiting an IC50 of 1.15 μM. This compound dampens the inflammatory response and offers potential for research into anti-inflammatory diseases and sepsis [1].

Vilobelimab (CaCP-29, IFX-1), a monoclonal antibody targeting C5a, inhibits this pro-inflammatory complement component which is pivotal in causing organ dysfunction. By preventing the activation and chemotaxis of neutrophils and reducing inflammatory signaling, Vilobelimab could be beneficial in researching conditions such as sepsis and COVID-19 [1].

FPL-65447 hydrochloride is a selective D1 receptor agonist that has potential for the acute treatment of renal and cardiac failure and of sepsis and septic shock.

PNU-282987 free base is a selective and potent α7 nicotinic acetylcholine receptor (nAChR) agonist and 5-HT3 receptor antagonist with anti-inflammatory activity.PNU-282987 free base protects against sepsis-induced acute lung injury in mice, attenuates activation of ILC2s and Streptozotocin-induced airway inflammation.PNU-282987 free base is used in the study of neurological diseases.

Enrofloxacin (BAY-Vp2674) is a veterinary antibacterial agent, used in poultry.

Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) serves as a potent antibiotic, exhibiting a minimum inhibitory concentration (MIC 90) of 0.312 μg/mL against Mycoplasma bovis and demonstrating inhibitory activity towards the vaccinia virus (VV).

Enrofloxacin hydrochloride is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.