elimination

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation.

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.

Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis.

Meproscillarin is a glycoside with high bioavailability (about 70%) and an elimination independent of renal function.

BNTA is a potent extracellular matrix (ECM) modulator. In a rat model of arthritis, BNTA modulates arthritis by promoting the synthesis of cartilage structural molecules on chondrocytes through the induction of superoxide dismutase 3 (SOD3) and regulating chondrogenesis through superoxide anion elimination.

TP-16 is a novel potent and selective EP4 antagonist that blocks the function of IMCs and enhances cytotoxic T cell-mediated tumor elimination in vivo.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Secnidazole (PM-185184) is a second-generation 5-nitroimidazole antimicrobial that is structurally related to other 5-nitroimidazoles including [DB00916] and [DB00911], but displays improved oral absorption and longer terminal elimination half-life than antimicrobial agents in this class [A27210]. Secnidazole is selective against many anaerobic Gram-positive and Gram-negative bacteria and protozoa.

D-Glucuronic acid sodium salt monohydrate (Sodium D-glucuronate) is a carboxylic acid that is highly soluble in water. In humans, glucuronic acid often binds to toxic substances to facilitate elimination and to hormones to aid in their transport.

Hexaflumuron is a chitin synthesis inhibitor used to bait and eliminate termite colonies. Termites are unable to metabolize hexaflumuron and clearance is slow, resulting in up to 100% elimination. Hexaflumuron has also been tested for use with the raisin

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

2-Quinolinecarboxaldehyde (Quinoline-2-carbaldehyde) is a small rigid molecule that is a compound in the Henry reaction and subsequent elimination. 2-Quinolinecarboxaldehyde inhibits AChE with an IC50 of 13.48 μM.

Disodium succinate (Sodium succinate) is the sodium salt form of succinate, which is an important metabolite at the cross-road of several metabolic pathways and involved in the formation and elimination of reactive oxygen species.

UR-7247 is a novel orally active angiotensin II subtype I (AT1) antagonist, demonstrating very long pharmacological effects. in vivo studies indicate no significant difference between 10 mg UR-7247 and 100 mg losartan four hours post-administration, while in vitro blockade with 100 mg losartan exceeds that observed with UR-7247, confirming UR-7247’s extended plasma half-life potentially due to high-affinity protein binding, highlighting its long-lasting, well-tolerated AT1 receptor antagonism in healthy subjects.

Etebenecid (Urelim) is uricosuric agents, which lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys. It also inhibits penicillin tubular secretion.

PLX5622 hemifumarate is a highly selective, blood-brain barrier-permeable, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and a Ki of 5.9 nM. It can be used to eliminate proliferating and specific microglia before and during disease progression and is applicable for inducing Alzheimer's disease models.

D-Phenothrin ((-)-trans-Phenothrin) is a type II synthetic pyrethroid extensively employed in veterinary medicine for pest control on animals, crop protection, and the elimination of insects, mosquitoes, and human lice.

BMS-962212, a direct, reversible, and selective factor XIa (FXIa) inhibitor, demonstrates fast pharmacodynamic (PD) response onset and rapid elimination with a well-tolerated profile. It dependently increases activated partial thromboplastin time and decreases FXI clotting activity exposure [1].

IU1-47 is an effective and specific USP14 inhibitor (IC50: 0.6 μM). IU1-47 causes tau elimination in cultured neurons. IU1-47 inhibits IsoT/USP5 (IC50: 20 μM).

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized E3 ligase ligand-linker conjugate, incorporating the cereblon ligand from Pomalidomide and a linker used in PROTAC technology. It facilitates targeted protein degradation by modulating E3 ligase activity, thereby enabling the selective elimination of specific proteins of interest.

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination compared to BRD3. It effectively suppresses solid tumors with minimal cytotoxic effects and comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN)/cullin 4A[1].

PF-07265028 is an HPK1 inhibitor with an IC50 of 17 nM. Pharmacokinetic studies in mice and monkeys indicate that PF-07265028 exhibits moderate clearance, terminal half-life, volume of distribution, and oral bioavailability. It targets, binds, and inhibits Hpk1 activity, blocking Hpk1-mediated signaling pathways to prevent immune suppression mediated by Hpk1, including the inhibition of T-cell receptor (TCR) signaling, effector T-cell suppression, aberrant cytokine expression, and the elimination of the immunosuppressive tumor microenvironment (TME). This action can activate a cytotoxic T lymphocyte (CTL)-mediated immune response against tumor cells. Hpk1 is primarily expressed in hematopoietic cells and acts as a negative regulator of TCR signaling and T and B cell activation.

Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant with no acute toxicity when administered. In rats, the systemic elimination half-life of Octachlorodibenzo-p-dioxin (50 μg/kg intravenously or 50-5000 μg/kg orally) is 3-5 months. It can accumulate and concentrate in the liver and adipose tissue after low-dose, repeated exposure. Repeated dosing of Octachlorodibenzo-p-dioxin leads to increased activity of 7-ethoxyresorufin-O-deethylase (7-EROD) and elevated total cytochrome P-450 levels.