pathological

Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.

Nerolidol (Peruviol) shows sedative effects in animals, oxidative process plays a crucial role on neuronal pathological consequence. Nerolidol is mainly related to ROS and DNA single strand breaks generated by the presence of oxidative lesions.

SIRT5 inhibitor 7 (compound 58), a substrate-competitive and selective SIRT5 inhibitor with IC 50 = 310 nM, significantly attenuated renal dysfunction and pathological damage in lipopolysaccharide (LPS)- and cecum ligation perforation (CLP)-induced septic AKI mice, and modulated proteinsuccinimidylation and proinflammatory cytokine release and pro-inflammatory cytokine release in the kidneys of acute kidney injury (AKI) mice.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Ceapin-A7, with an IC50 of 0.59 μM, selectively inhibits ATF6α signaling in response to ER stress. This compound is instrumental in investigating ATF6α's activation mechanism and its function in pathological conditions.

Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease

CT52923 is a selective, orally active antagonist of platelet-derived growth factor receptor (PDGFR), functioning as an ATP-competitive inhibitor. It has versatile applications for researching pathological diseases such as atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer.

LY88074 analog 1, a benzothiophene compound with nitrogen-containing non-basic side chains, can be utilized either independently or alongside estrogen or progestin. This agent is effective for mitigating post-menopausal symptoms, including osteoporosis, cardiovascular-related pathological conditions, and estrogen-dependent cancer.

1,9-Dimethylxanthine acts as an adenosine receptor antagonist, inhibiting the effects of adenosine on the central nervous system, thereby enhancing neural excitability. Utilized as a pharmacological tool in research, it aids in investigating physiological and pathological processes associated with adenosine.

IIQLPEIVVV TFA serves as a specific inhibitor targeting the Drp1-Mff interaction. This compound discriminates between physiological and pathological fission, hindering physiological fission which leads to mitochondrial dysfunction. IIQLPEIVVV TFA is also utilized in research related to Huntington's disease.

FXR agonist9 (compound 26) is a selective, orally active partial agonist of FXR with an EC50 of 0.09 µM (maximum efficacy of 75.13%). It ameliorates the pathological features of fatty liver disease in mice induced by HFD and CCl4-related metabolic dysfunction.

Phosphorylcolamine sodium is primarily used for the prevention and treatment of pathological syndromes caused by calcium and magnesium.

Simufilamum (also known as PTI-125) is an oral small-molecule compound candidate that targets altered conformations of filamin A. It binds and reverts the misfolded filamin A in the brains of Alzheimer's disease patients, thereby slowing the disease's pathological progression. Additionally, PTI-125 reduces tau protein hyperphosphorylation, decreases Aβ42 aggregation and deposition, neurofibrillary tangles, and neuroinflammation. The compound demonstrates concentration-dependent efficacy in vitro, starting at 1 picomolar (pM), in both control groups and post-mortem hippocampal slices from Alzheimer's disease (AD) patients. PTI-125 is the first therapeutic candidate to preferentially bind and reverse pathogenic protein conformations.

α-L-fucopyranose, an endogenous metabolite and six-carbon deoxyhexose, is present at the terminal or anterior position of many cell surface oligosaccharide ligands, mediates cell recognition and adhesion signaling pathways, and is a potentially critical molecule in pathological processes, including tumors.

AS2690168 freebase is an orally active inhibitor of RANKL signaling, capable of suppressing RANKL-induced osteoclastogenesis in RAW264 cells. AS2690168 is applicable in research related to pathological bone resorption.

β-1,4-GALT1-IN-1 (Compound 6) is a β-1,4-GALT1 inhibitor with an IC50 value of 6.2 μM. It is applicable in studying various pathological conditions, including cancer, autoimmune diseases, and viral infections.

AS2690168 hydrochloride is an orally active inhibitor of RANKL signaling that can suppress RANKL-induced osteoclastogenesis in RAW264 cells. AS2690168 is applicable in research related to pathological bone resorption.

ARN23765 is an F508del-CFTR corrector with an EC50 of 38 pM in human bronchial epithelial cells. It enhances the maturation and function of F508del-CFTR at the cell membrane, influencing ion transport and secretion, thereby addressing the pathological mechanisms of cystic fibrosis (CF).

SRSF1-IN-1 (STP2) is an inhibitor of SRSF1 that modulates the splicing of Bcl-x precursor mRNA by downregulating SRSF1 expression. It exhibits antitumor activity in vitro and in vivo, with IC50 values ranging from 0.33 to 6.93 μM against cancer cells such as HepG2 and MCF7. In mice, SRSF1-IN-1 demonstrates a high safety profile, as intraperitoneal administration of 1 g kg does not lead to mortality or pathological damage. SRSF1-IN-1 holds potential for research in the field of antitumor therapy [1].

HDAC11-IN-2 (compound B6) is a highly selective inhibitor of Histone Deacetylase 11 (HDAC11). It demonstrates IC50 values of 51.1 ×10^-3 μM for HDAC11 and 5 μM for HDAC8. HDAC11-IN-2 reduces de novo lipogenesis (DNL) and enhances fatty acid oxidation, which alleviates hepatic lipid accumulation and pathological symptoms in MASLD mice. By inhibiting HDAC11, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at the Thr172 site, thereby modulating de novo lipogenesis and fatty acid oxidation in the liver.

Xestospongin C ((-)-Xestospongin C) is a selective inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor and also inhibits sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA). It has neuroprotective effects in APP PS1 AD mice, improving cognitive and pathological deficits associated with Alzheimer's disease.

Diacetylsplenopentin HCl is used as a synthetic immunomodulator that affects the proliferation and differentiation of bone marrow stem cells without stimulating pathological immune responses beyond the balance of the immune system. This effect is specific

rac-1,2-bis-Palmitoyl-3-chloropropanediol is a 3-monochloropropane-1,2-diol (3-MCPD) ester.1It has been found as a contaminant in edible olive oils, with the lowest and highest concentrations in extra virgin and olive pomace oils, respectively.rac-1,2-bis-Palmitoyl-3-chloropropanediol has also been found in cottonseed and palm oils, as well as in shortening.2It induces renal tubular necrosis and a decrease in spermatids, but no gross pathological changes, in mice.3 1.Hung, W.-C., Peng, G.-J., Tsai, W.-J., et al.Identification of 3-MCPD esters to verify the adulteration of extra virgin olive oilFood Addit. Contam. Part B Surveill.10(3)233-239(2017) 2.MacMahon, S., Begley, T.H., and Diachenko, G.W.Occurrence of 3-MCPD and glycidyl esters in edible oils in the United StatesFood Addit. Contam. Part A. Chem. Anal. Control Expo. Risk Assess.30(12)2081-2092(2013) 3.Liu, M., Gao, B.-Y., Qin, F., et al.Acute oral toxicity of 3-MCPD mono- and di-palmitic esters in Swiss mice and their cytotoxicity in NRK-52E rat kidney cellsFood Chem. Toxicol.50(10)3785-3791(2012)

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