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PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouseplasma.
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouseplasma. Enpp-1-IN-11 can be used for researching anticancer .
AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC50s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouseplasma stability, and no obvious cytotoxicity .
BH-Vis is a two-photon fluorescent probe that inhibits cell plasma membrane (CPM). BH-Vis has great potential to accurately identify pyroptosis at the cellular level during AAA development in the mouse abdominal aortic aneurysm AAA model .
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC500 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC500 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
C20 Sphingomyelin is a naturally occurring sphingolipid. Levels of C20 sphingomyelin are upregulated in the hippocampus of rats with diabetes induced by streptozotocin (HY-13753) and in human plasma where it is positively correlated with insulin resistance in obese humans. C20 sphingomyelin is also upregulated in the liver of a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. The plasma concentration of C20 sphingomyelin is decreased in men with prostate cancer. As this product is derived from a natural source, there may be variations in the sphingoid backbone.
C2 3'-Sulfo galactosylceramide (d18:1/2:0) (C2 Sulfatide) is one of the sulfatide class of glycolipids. C2 3'-Sulfo galactosylceramide (d18:1/2:0) can be used in the quantification of lysosulfatides in mouse brain tissue and plasma .
ML356 (Compound 16) is an inhibitor for fatty acid synthase (FAS), that inhibits the thioesterase domain of FAS (FAS TE) with an IC50 of 0.334 μM, and blocks the de novo palmitate synthesis in PC-3 cell with an IC50 of 20 μM. ML356 exhibits good membrane permeability, and good stability in human and mouseplasma .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouseplasma. PAT-048 reduces dermal fibrosis in vivo .
FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC50 of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models .
σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
DOTA-bis(tert-butyl)ester is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide conjugates (RDCs). DOTA-bis(tert-butyl)ester can be conjugated with different salts to form different metal chelators, such as (HY-B1244) hydrochloride to obtain DOTA-MN2. DOTA-MN2 can be reacted with [67]Ga-citrate to obtain radiolabeling. When (67)Ga-DOTA-MN2 is incubated in phosphate buffer solution or mouseplasma for 24 hours, it does not undergo significant decomposition. In the biodistribution experiment of NFSa tumor mice, it has high tumor uptake and rapid plasma clearance, and is a good material for SPECT and PET studies.
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
GZNL-P36 is an orally active inhibitor for SARS-CoV-2 papain-like protease (PL pro), with an IC50 of 6.45 nM. GZNL-P36 inhibits SARS-CoV and its variants with EC50 range from 58.2 nM to 2.66 μM. GZNL-P36 exhibits a peak plasma concentration Cmax of 549 ng/mL, a half-life T1/2 of 1.45 h and a bioavailability of 74.7% in CD-1 mouse. GZNL-P36 exhibits antiviral activity in SARS-CoV-2 XXB.1 infection in mouse .
Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouseplasma .
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
Garcinia cambogia extract contains several active compounds, including hydroxycitric acid (HCA) (an ECC inhibitor), xanthones, benzophenones, hydroxycitric acid (an ATP-citrate lyase inhibitor). Garcinia cambogia extract lowers the body weight gain, visceral fat accumulation, blood and hepatic lipid concentrations, and plasma insulin and leptin levels in a high-fat diet (HFD)-induced obesity mouse model. Garcinia cambogia extract is promising for research of fatty liver, dyslipidemia, hyperinsulinemia and hyperleptinemia rendered by HFD .
TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
Oleuropein aglycone is a polyphenol and an aglycone form of Oleuropein (HY-N0292) that has been found in extra virgin olive oil and has diverse biological activities. It is formed from oleuropein via enzymatic, acidic, or acetyl hydrolysis. Dietary administration of oleuropein aglycone (50 mg/kg of food) increases the number of neuronal autophagic vesicles and reverses cognitive deficits in a TgCRND8 transgenic mouse model of Alzheimer’s disease. It also decreases cortical and hippocampal levels of histone deacetylase 2 (HDAC2) and restores long-term potentiation in the same model. Oleuropein aglycone increases urinary norepinephrine, as well as interscapular brown adipose tissue epinephrine and UCP1 protein levels, and decreases plasma leptin levels and total abdominal cavity adipose tissue weight in a rat model of high-fat diet-induced obesity. It also reduces lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
ST-148 is a novel small molecule compound that has potent inhibitory effects against all four dengue virus serotypes. In the nonlethal AG129 mouse dengue virus infection model, ST-148 significantly reduced viremia and viral load in vital organs and tended to reduce plasma cytokine levels. Compound resistance was associated with the dengue virus capsid (C) gene, and the direct interaction of ST-148 with the C protein was presumed to be achieved through the protein's built-in fluorescence change in the presence of the compound. Therefore, ST-148 appears to interact with the dengue virus C protein and inhibit one or more unique steps of the viral replication cycle.
Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300 .
Dieugenol is a neolignan that has been found in N. leucantha and has antioxidative and antiprotozoal activities. It inhibits the formation of thiobarbituric acid reactive substances (TBARS) and scavenges superoxide anions, but not hydroxyl radicals, in cell-free assays. It has anti-trypanosomal activity against T. cruzi amastigotes and trypomastigotes (IC50s=15.1 and 11.5 μM, respectively) but is cytotoxic to NCTC L-929 fibroblasts with a 50% cytotoxic concentration (CC50) value of 58.2 μM.2 Dieugenol (15 μM) disrupts the integrity of the T. cruzi trypomastigote plasma membrane but does not induce the production of reactive oxygen species (ROS) in trypomastigotes or LPS-stimulated and unstimulated isolated mouse peritoneal macrophages.
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
BH-Vis is a two-photon fluorescent probe that inhibits cell plasma membrane (CPM). BH-Vis has great potential to accurately identify pyroptosis at the cellular level during AAA development in the mouse abdominal aortic aneurysm AAA model .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
Garcinia cambogia extract contains several active compounds, including hydroxycitric acid (HCA) (an ECC inhibitor), xanthones, benzophenones, hydroxycitric acid (an ATP-citrate lyase inhibitor). Garcinia cambogia extract lowers the body weight gain, visceral fat accumulation, blood and hepatic lipid concentrations, and plasma insulin and leptin levels in a high-fat diet (HFD)-induced obesity mouse model. Garcinia cambogia extract is promising for research of fatty liver, dyslipidemia, hyperinsulinemia and hyperleptinemia rendered by HFD .
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface.It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin.This underscores the diverse and essential functions of Plasma kallikrein/KLKB1 in various physiological processes.Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag.
RBP4 Protein transports retinol in blood plasma, delivering it from liver stores to peripheral tissues. Binding to all-trans retinol, it transfers it to STRA6 for efficient cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further supports STRA6 in retinol transport. RBP4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Mouse (HEK293, His) is 183 a.a., with molecular weight of ~22.8 kDa.
Serpin A5 protein is a heparin-dependent serine protease inhibitor that controls proteolytic activity in body fluids. It binds irreversibly to the serine activation site, inactivating serine proteases and regulating intravascular and extravascular proteolysis. Serpin A5 Protein, Mouse (Baculovirus, His) is the recombinant mouse-derived Serpin A5 protein, expressed by Sf9 insect cells , with N-10*His labeled tag. The total length of Serpin A5 Protein, Mouse (Baculovirus, His) is 381 a.a., with molecular weight of ~45.3 kDa.
Serpin G1 protein, also known as C1 inhibitor, regulates complement activation, coagulation, fibrinolysis, and kinin production. It forms an inactive complex with C1r or C1s protease and controls C1 complex activation. Serpin G1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin G1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Serpin G1 Protein, Mouse (HEK293, His) is 485 a.a., with molecular weight of 92-95 kDa.
PGCP is a carboxypeptidase with a potentially critical role in the hydrolysis of circulating peptides. It catalyzes the cleavage of terminally unsubstituted dipeptides, releasing amino acids. PGCP Protein, Mouse (HEK293, His) is the recombinant mouse-derived PGCP protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PGCP Protein, Mouse (HEK293, His) is 452 a.a., with molecular weight of ~60.0 kDa.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses.It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups.PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by Sf9 insect cells , with C-Myc, N-10*His labeled tag.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses.It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups.PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by HEK293 , with C-Myc, N-10*His labeled tag.
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