clearance

CRT0273750 regulates plasma LPA levels and is suitable for in vivo studies. CRT0273750 is an autotaxin (ATX) inhibitor with IC50 of 0.014 μM.

Mebrofenin (SQ 26962) is available as a ready to use the kit for radio-labeling with Tc-99m.Technetium Tc 99m Mebrofenin is a diagnostic radiopharmaceutical composed of diisopropyl-iminodiacetic acid (DISIDA) attached to a technetium-99m ion.

PF-06291874 (Glucagon receptor antagonists-4) (Glucagon receptor antagonists-4) is a highly effective and orally active antagonist of the glucagon receptor.

Ambroxol (NA-872) is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosolvan, Lasolvan or Mucoangin. The substance is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract which play an important role in the body's natural defense mechanisms. It stimulates synthesis and release of surfactant by type II pneumocytes. Surfactants act as an anti-glue factor by reducing the adhesion of mucus to the bronchial wall, in improving its transport and in providing protection against infection and irritating agents.

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

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

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

2-Iodohippuric Acid can be used to measure renal clearance for renal function studies, and for the diagnosis of certain diseases, such as liver and kidney disease. In addition, it is used in the synthesis of certain drugs.

BPN-15606, an orally active γ-secretase modulator (GSM), significantly reduces Aβ42 and Aβ40 production in SHSY5Y neuroblastoma cells, demonstrating IC50 values of 7 nM and 17 nM, respectively. This compound exhibits favorable pharmacokinetic pharmacodynamic (PK PD) properties, such as bioavailability, half-life, and clearance. Importantly, BPN-15606 markedly decreases Aβ42 and Aβ40 levels in the central nervous system of both rats and mice[1].

Arimoclomol (BRX-220 free base), a co-inducer of heat shock proteins (HSP), is utilized in studies on the treatment of amyotrophic lateral sclerosis (ALS).

Arimoclomol maleate (BRX-220) (BRX-220) is a heat shock protein (HSP) co-inducer.

Dusquetide TFA is a kind of innate defense regulator (IDR).Dusquetide TFA has been shown to be active in reducing inflammation and increasing clearance of bacterial infections.Dusquetide TFA regulates innate immune responses to PAMPs and DAMPs in combinat

Dusquetide is a first-in-class innate defense regulator. Dusquetide displays activity in both reducing inflammation and increasing the clearance of bacterial infection.

Leukotriene B4 (LTB4) is a compound derived from arachidonic acid via the 5-lipoxygenase pathway that mediates certain inflammatory and immune responses. Leukotriene B4 induces neutrophil extracellular traps that impede the clearance of Pneumocystis japonicus.

Concanamycin A (Folimycin), a polycyclic lactone antibiotic, is a selective inhibitor of vacuolar H+-ATPase (V-ATPase) and lysosomal acidification, and can be used to study inflammation.Concanamycin A enhances the immune clearance of infected progenitor cells by cytotoxic T lymphocytes, and inhibits Nef et al. from different branches of HIV and simian immunodeficiency virus. Concanamycin A enhances immune clearance of cytotoxic T lymphocytes from infected progenitor cells, inhibits the Nef allele from different branches of HIV and simian immunodeficiency virus, and can be used to study HIV infection.

ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.

p38 MAPK-IN-1 is a novel selective p38 MAPK inhibitor with high potency, long duration, and low clearance, which reduces inflammatory responses by inhibiting LPS-induced TNF-α production.

Resolvin E1 (RvE1) is an endogenous lipid mediator derived from the omega-3 fatty acid eicosapentaenoic acid (EPA). It exhibits anti-inflammatory properties, activates inflammation resolution, and promotes phagocytic clearance. It prevents 2,4,6-trinitrobenzenesulfonic acid-induced colitis and improves erythrocytosis and severe aplastic anaemia (SAA).

SIRT3 activator2 (compound 2a) acts as an activator of SIRT3. It is presumed to bind directly with SIRT3 in SH-SY5Y cells, as inferred through thermal stability, facilitating the SIRT3-dependent clearance of α-Syn. Furthermore, SIRT3 activator2 enhances motor functions in Parkinsonian mice and dose-dependently prevents the loss of dopaminergic (DA) neurons in the substantia nigra.

HIV-1inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor with an EC50 range of 0.0039-0.338 μM. Its target is the reverse transcriptase, exhibiting an IC50 value of 0.055 μM. Additionally, HIV-1inhibitor-75 demonstrates good metabolic stability in vitro, presenting moderate clearance rates and an extended half-life in human plasma and liver microsomes.

Pyrocatechol sulfate, a phenolic metabolite found in human plasma, is associated with the intake of specific foods such as berries and the state of the gut microbiome. It serves as a potential urinary biomarker for kidney function, dialysis clearance rates, whole grain consumption, and regular coffee intake. Additionally, in conjunction with other phenolic sulfates, pyrocatechol sulfate plays a role in regulating various biological functions, including those related to brain health and the rhythmic beating of cardiac cells.

Antimalarial agent 44 (Compound 3) is an antiparasitic agent effective against malaria. It exhibits good permeability in MDCK-MDR1 cell monolayers and has a high clearance rate in mouse liver microsomes.

68Ga-DOTA-NT-20.3 is an analogue of neurotensin (NTS) and acts as a ligand for 68Ga ions. In PET imaging, it demonstrates rapid tumor uptake and high contrast between tumor and background, along with fast clearance from the blood and moderate accumulation in the kidneys. Its pharmacokinetic and biodistribution properties are advantageous, producing high-quality PET images in mice with subcutaneous or orthotopic human pancreatic cancer xenografts. 68Ga-DOTA-NT-20.3 specifically binds to NTSR1 on pancreatic cancer cells and outperforms 18F-FDG in PET detection of adenocarcinoma.

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.