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Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for ratliver V1A receptor and rat kidney V2 receptor respectively.
SC-26196 is a potent, orally active Delta6 desaturase (D6D, FADS2) inhibitor (IC50=0.2 μM in a ratliver microsomal assay). Antiinflammatory properties .
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
Thymine, one of the four bases of DNA, is a substrate for ratliver dihydropyrimidine dehydrogenase (DPD), with a Km value of 2.2 μM, Ki of 24 μM (using 5-FU as the DPD substrate), and a specific activity of 0.68 nmol/min/mg .
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .
MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy .
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for ratliver microsomal ACAT activity .
Testosterone/BSA, a conjugate of Testosterone (HY-113415) and bovine serum albumin (BSA), acts as a nuclear transporter and cytoplasmic accumulator. Testosterone/BSA can enter the nuclei of rat testicular spermatocytes, spermatids and ratliver endothelial cells, while the antigenicity of BSA remains intact. Testosterone/BSA accumulates in the cytoplasm of rat hepatocytes in granular form. Testosterone/BSA can be used to investigate the membrane-initiated or non-genomic activities of steroid hormones .
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
2-Phenylpropionic acid is an intermediate in the metabolism of alpha-Methylstyrene. 2-Phenylpropionic acid covalently binds to ratliver protein. 2-Phenylpropionic acid can be used in the research of nonsteroidal anti-inflammatory agents .
5α-reductase, Rat (Sprague-Dawley) Liver is an enzyme involved in steroid metabolism and participates in the androgen metabolic pathway. 5α-reductase, Rat (Sprague-Dawley) Liver catalyzes the conversion of testosterone to 5α-dihydrotestosterone (DHT). DHT plays important roles in the development of male sex organs, hair growth, prostate function, and other aspects .
2,3-Oxidosqualene (Squalene oxide) is a sterol biosynthesis precursor intermediate.2,3-Oxidosqualene participates in cyclization pathways that form sterols and triterpenes, and contributes to introduction of their characteristic 3-hydroxyl group.2,3-Oxidosqualene forms metabolically from squalene in ratliver homogenates under sterol synthesis conditions.2,3-Oxidosqualene converts to sterols including cholesterol, lathosterol, and lanost-8-en-3β-ol in ratliver homogenates under anaerobic conditions .
Mauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049) .
Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: ratliver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function .
DHPDS disodium salt is a pH-sensitive fluorescent dye. DHPDS disodium salt is used to measure intracellular pH (pHi) from the surface fluorescence of the isolated perfused ratliver .
3-Fluoro-L-tyrosine is a tyrosine analogue, inhibits transamination by tyrosine aminotransferase (TAT). And 3-FluoroL-tyrosine has been shown to be biologically incorporated into proteins in place of tyrosine. 3-Fluoro-L-tyrosine pretends to be the substrate of ratliver tyrosine aminotransferase, markedly disturbs the Tyr-TAT association .
Lignocaine N-oxide (Lidocaine N-oxide) is a compound derived from the metabolism of lidocaine. Lidocaine can be metabolized to its N-oxide in ratliver microsomes.
Coprine is an orally active disulfiram (HY-B0240)-like component and an inhibitor of aldehyde dehydrogenase. Coprine is isolated from Coprinus atranentarius. Coprine inhibits low Km aldehyde dehydrogenase in ratliver and increases blood acetaldehyde levels during in vivo ethanol metabolism. Coprine does not inhibit semi-purified low Km aldehyde dehydrogenase from ratliver in vitro. Coprine can be used in studies related to alcoholism .
Ochnaflavone is an inhibitor of IIA-type secretory phospholipase A2 (sPLA2-IIA) with an IC50 of 3.45 µM. Ochnaflavone exhibits significant anti-inflammatory and liver-protective effects, capable of inhibiting the degradation of phosphatidylethanolamine (PE) and lipid peroxidation induced by carbon tetrachloride (CCl4) in ratliver, with an IC50 of 7.16 µM for lipid peroxidation. Ochnaflavone can be used in research on liver damage and inflammatory diseases .
6-Aminochrysene (6-Aminochrysene) is an aromatic amine used as a chemotherapeutic agent in the treatment of splenomegaly, myeloid leukemia, and breast cancer. 6-Aminochrysene is activated by CYP450 in ratliver .
Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and ratliver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes .
3-Pyridineacetic acid is an orally active nicotinic acid analog. 3-Pyridineacetic acid enhances cholesterol oxidation in ratliver mitochondria. 3-Pyridineacetic acid inhibits Triton-induced hypercholesterolemia in rats. 3-Pyridineacetic acid can be used in research related to hypercholesterolemia .
PFK-IN-1 (compound 1) is a phosphofructokinase (PFK) inhibitor, with IC50 values of 0.41 and 0.23 μM against T.brucei and T.cruzi PFK, respectively, and an ED50 of 15.18 μg/mL for T.brucei. The half-lives of PFK-IN-1 in rat and mouse liver microsomes are 9.7 and 408 minutes, respectively .
Methyl propyl disulfide is an orally administrable volatile sulfide present in onions. Methyl propyl disulfide reduces the activity of spermine N'1-acetyltransferase (SAT), inhibits cell proliferation, and decreases the induction of placental glutathione S-transferase (GST-P)-positive hepatocyte foci in ratlivers. Methyl propyl disulfide can be used in studies related to the mechanism of hepatocarcinogenesis .
6"-O-Acetylgenistin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetylgenistin significantly inhibits lipid peroxidation in ratliver microsome with an IC50 of 10.6 μM .
6"-O-Acetyldaidzin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetyldaidzin significantly inhibits lipid peroxidation in ratliver microsome with an IC50 of 8.2 μM .
Mefruside is an orally active diuretic and has a mild hypotensive effect. Mefruside inhibits the synthesis of urea in an isolated ratliver perfusion model. Mefruside can be used in studies of oedema and hypertension .
MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
CGP 44 645 is the methanol metabolite of Letrozole (HY-14248) and is a molecular indicator for evaluating its metabolic kinetics in microsomes in vitro. Levels of CGP 44 645 in ratliver microsomes may be sex-specific .
DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for ratliver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis .
FASN/SCD-IN-1 is a Silybin (HY-N0779A) derivative, an orally active inhibitor of Fatty Acid Synthase (FASN)/Stearoyl-CoA Desaturase (SCD). FASN/SCD-IN-1 has shown in vitro activity in inhibiting lipid deposition, reducing FASN and SCD transcriptional levels, and exhibiting antioxidant, anti-inflammatory, and anti-fibrotic activities. FASN/SCD-IN-1 has demonstrated significant hepatoprotective effects in a rat model of acute liver injury. FASN/SCD-IN-1 ameliorates the pathological features of MASH liver, including steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative steatohepatitis (MASH). FASN/SCD-IN-1 can be used to study MASH .
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using ratliver microsomes .
Akt1&PKA-IN-2 (Compound R-29) is a AKT1 and PKA inhibitor with selectivity for CDK2, with IC50 values of 0.007 and 0.01 μM, respectively. Akt1&PKA-IN-2 is applicable for cancer research .
Z-MAL is a highly efficient and broad-spectrum HDAC substrate. Z-MAL exhibits high conversion activity for class I, II histone deacetylases, and class III SIRT1. Z-MAL can be used in studies on the structure-activity relationship, subtype selectivity, and inhibitor screening of HDAC .
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin II inhibits cell-free protein synthesis, releases adenine from ratliver ribosomes and from DNA, and has no RNase activity .
(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in ratliver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
Diallyl tetrasulfide is an orally active diallyl tetrasulfide. Diallyl tetrasulfide ameliorates cadmium-induced changes in acetylcholinesterase and adenosine triphosphatase activities as well as oxidative stress injury in the brain of rats . Diallyl tetrasulfide inhibits lipid peroxidation in ratliver microsomes . Diallyl tetrasulfide ameliorates cadmium-induced oxidative liver injury in rats . Diallyl tetrasulfide protects cells against cadmium-induced loss of cell viability, reduces apoptosis rate and ROS production. Diallyl tetrasulfide is applicable to research related to cadmium-induced neurotoxicity and cadmium-induced oxidative liver injury .
GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, ratliver GPa and human skeletal muscle GPa, respectively . GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia .
N-Nitrosometoprolol is an N-nitroso derivative formed by the in vitro reaction of β-adrenergic blockers with sodium nitrite. N-Nitrosometoprolol can induce micronuclei in ratliver, bone marrow and spleen .
SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/ratliver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
2-Phenyl-2-(2-pyridyl)acetonitrile is the major metabolite of SC 15396 metabolized by the supernatant fraction of ratliver homogenate. SC 15396 is an antigastrin that inhibits gastric secretion .
PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC50s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases .
Rat IL-10 mRNA encodes interleukin-10 (IL-10). IL-10 is expressed in tissues/cells such as hepatic stellate cells and is involved in physiological processes including liver fibrosis.
RPR107393 is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 inhibits ratliver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 reduces plasma cholesterol in rats and marmosets. RPR107393 can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis .
RPR107393 free base is an orally active potent selective squalene synthase (SQS) inhibitor. RPR107393 free base inhibits ratliver microsomal squalene synthase with an IC50 value of 0.8 nM. RPR107393 free base reduces triglyceride biosynthesis by suppressing fatty acid biosynthesis via an increase in intracellular farnesol and its derivatives. RPR107393 free base reduces plasma cholesterol in rats and marmosets. RPR107393 free base can be used for metabolic disease research, such as hypercholesterolemia, hypertriglyceridemia and atherosclerosis [1][2].
Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in ratliver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes .
Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .
Riddelline, a pyrrolizidine alkaloid, is a potent genotoxic agent. Riddelline induces significant elevations in unscheduled DNA synthesis and S-phase synthesis in ratliver .
Glomeratide A is a benzophenone C-glucoside with hepatoprotective effects. Glomeratide A has a protective effect against d-galactosamine-induced hepatotoxicity in ratliver epithelial stem-like cells.
Conivaptan (hydrochloride) (Standard) is the analytical standard of Conivaptan (hydrochloride). This product is intended for research and analytical applications. Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for ratliver V1A receptor and rat kidney V2 receptor respectively.
PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis .
(±)-Tocol is a synthetic vitamin E derivative.nlike (±)-α-tocopherol, (±)-tocol does not suppress retinol-induced erythrocyte hemolysis or increase microviscosity of ratliver phosphatidylcholine (PC) liposomes.
Phorone (Diisopropylidene acetone) is a glutathione (GSH) depletor. Phorone specifically and reversibly depletes free GSH through enzymatic binding (Glutathione S-transferase) (Km = 0.9 mM). Phorone reversibly reduces the binding and nuclear uptake of glucocorticoid receptors in ratliver, and this effect is related to the temporal changes in GSH levels. Phorone can be used for studying liver toxicity.
Perhexiline-d11 (maleate) is the deuterium labeled Perhexiline maleate. Perhexiline maleate is a potent carnitine palmitoyltransferase 1 (CPT 1) inhibitor with IC50s of 77 and 148 μM for rat heart and liver CPT 1, respectively.
Goodyeroside A is a glycoside compound derived from the plant Goodyera that exhibits significant hepatoprotective activity. It can inhibit liver damage induced by carbon tetrachloride (HY-Y0298) in primary cultured rat hepatocytes .
PDHK-IN-7 (compound 32) is an inhibitor of pyruvate dehydrogenase kinase with an IC50 value of 17 nM.PDHK-IN-7 activates PDH in ratlivers and has a glucose-lowering effect in Zucker fatty rats .
S-3483, a Chlorogenic acid (HY-N0055) derivative, is a reversible, linear competitive glucose-6-phosphatase (Glc-6-Pase) system inhibitor. S-3483 inhibits Glc-6-Pase with a Ki 129 nM in ratliver microsomes. S-3483 specifically inhibits Glc-6-P transporter of renal and liver microsomes .
Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in ratliver microsomes free from vitamin E .
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for ratliver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis .
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in ratliver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation .
Helminthosporol is a natural plant growth-regulator that can promote the growth of rice and lettuce seedlings. Helminthosporol can also inhibit the activity of acyl-CoA: cholesterol acyltransferase (ACAT) in ratliver microsomes and the synthesis of cholesterol esters in macrophages .
DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for ratliver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis .
Deacetyldiltiazem is a metabolite with coronary vasodilator activity. Deacetyldiltiazem is present in the plasma of individuals taking Diltiazem. The deacetylase activity of deacetyldiltiazem is mainly catalyzed by the rat Ces2a enzyme. In vitro experiments of deacetyldiltiazem showed that its Km value was similar to that of ratliver microsomes, showing efficient deacetylase activity. The study of deacetyldiltiazem helps to understand the differences in the metabolic kinetics of compounds between different species .
(±)16-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in ratliver, brain, and intestinal microsomes. (±)16-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
Pyridaben-d13 is the deuterium labeled Pyridaben . Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: ratliver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function .
1-Pyrenebutanoyl-CoA is a type of coenzyme A that can non-competitively inhibit (Ki = 2 μM) phosphorylating (ADP-stimulated) respiration in ratliver mitochondria, and competitively inhibit (Ki = 2.1 μM and 15 μM) carnitine palmitoyl-CoA transferase and octanoyl-CoA transferase .
ED-594 is the glucuronide form of NB-506. ED-594 is one of the major metabolites of NB-506 in rat bile, mouse liver microsomes, ratliver microsomes and human liver microsomes .
Glutathione sulfinanilide (GSOAN) is a derivative of Nitrosobenzene (HY-121641). Glutathione sulfinanilide can be generated by the reaction of Nitrosobenzene with GSH. Glutathione sulfinanilide is degradable in ratliver homogenate .
Hydroxysaikosaponin D is a hepatocytoprotective saponin found in the roots of Bupleurum scorzonerifolium WILLD. Hydroxysaikosaponin D inhibits D-galactosamine-induced cytotoxicity in primary cultured rat hepatocytes. Hydroxysaikosaponin D mitigates D-galactosamine/LPS-induced liver injury in mice. Hydroxysaikosaponin D can be used for the research of liver injury .
Mimosinamine is a hydroxylase inhibitor with Fe2+ chelating activity. Mimosinamine inhibits bovine adrenal tyrosine hydroxylase, ratliver phenylalanine hydroxylase, and rat brainstem tryptophan hydroxylase. Mimosinamine can be used in the research of hypertension .
Enzyme-IN-4 is a competitive inhibitor of glyoxalase I that can be found in Stereum hirsutum. Enzyme-IN-4 has a Ki value of 4.6 μM against ratliver glyoxalase I .
Antihepatotoxic agent-1 is a cerebroside present in Lycium chinense Fruits with antihepatotoxic activity. Antihepatotoxic agent-1 exerts a protective effect by blocking the release of alanine aminotransferase and sorbitol dehydrogenase from primary cultured rat hepatocytes intoxicated with carbon tetrachloride. Antihepatotoxic agent-1 can be used in studies related to liver injury .
(E/Z)-3-Hydroxylicochalcone A (Compound 1) is a flavonoid found in licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis), with antioxidant and anti-inflammatory activity. (E/Z)-3-Hydroxylicochalcone A inhibits lipid peroxidation in ratliver microsomes. (E/Z)-3-Hydroxylicochalcone A inhibits LPS (HY-D1056)-induced ROS, NO, IL-6, and PGE2 production .
IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in ratliver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia .
SQ 11,447 is a methylurea analogue that demonstrates remarkable resistance to hydrolysis in both in vitro (rat, dog, and human liver homogenates) and in vivo (rat) experimental models.
Clinolamide is an N-cyclohexyl linoleamide. In a rat cholesterol metabolism study, feeding it at a dose of 0.3% for 21 days had no significant effect on serum, liver or kidney cholesterol levels, but had different effects on cholesterol synthesis in liver slices under different substrates and concentrations.
DF 461 is a sterol synthase inhibitor with significant inhibitory activity. DF 461 shows high selectivity for the liver and can effectively inhibit cholesterol synthesis in ratliver. DF 461 has shown the effect of lowering plasma lipids in repeated dosing studies in non-rodents .
FK 409 is a NO donor that can penetrate cell membranes. FK 409 has a vasodilatory effect on bovine retinal arteries. FK 409 alleviates acute-phase inflammation, induces HSP, and mitigates liver transplantation injury in a rat model of orthotopic liver transplantation. FK 409 can be used in research on cardiovascular diseases and liver transplant rejection and inflammatory immune system disorders .
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in ratliver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
PF-05221304 tromethamine is an orally active, liver-directed and dual ACC1/ACC2 inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2. PF-05221304 tromethamine is a substrate for organic anion transport polypeptides. PF-05221304 tromethamine directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors .
Palmitoyl glutathione (PGSH) is a palmitoylated peptide derivative and a liver-targeted liposome-forming agent. Palmitoyl glutathione can form liposome-like vesicles with cholesterol, which can encapsulate water-soluble solutes. Palmitoyl glutathione can be used in studies related to Acetaminophen (HY-66005)-induced liver necrosis .
Zoxamide metabolite 1 (Compound M1) is a monodechlorinated Zoxamide (HY-120921) metabolite. Zoxamide metabolite 1 undergoes dechlorination most plausibly at the reactive α-chloro ketone position .
Zolertine is an α-adrenergic receptor antagonist, with a pKi of 6.35 for rabbit α1A-adrenergic receptor and a pKi of 6.81 for rat α1B-adrenergic receptor. Zolertine competitively blocks α1D-adrenergic receptor-mediated vasoconstriction and α1A-adrenergic receptor-mediated vasoconstriction in arteries. Zolertine can be used in the research of hypertension .
Plantagoside A (Compound 3) is a phenylethanoid glycoside found in Plantago asiatica. Plantagoside A has antioxidant activity and can inhibit lipid peroxidation in ratliver microsomes induced by ADP and NADPH with an IC50 of 0.54 μM .
PDE4-IN-21 (Compound L19) is a poetent PDE4 inhibitor, with an IC50 of 0.48 μM. PDE4-IN-21 exhibits good inhibitory activity and remarkable metabolic stability in ratliver microsomes .
2-(Methylamino)benzoic acid (Standard) is the analytical standard of 2-(Methylamino)benzoic acid. This product is intended for research and analytical applications. 2-(Methylamino)benzoic acid is the main metabolite of methyl-N-methylanthranilates (MMA) (HY-76705) and is the compound in which the ester group is converted. MMA can be isolated from citrus fruits and has potential analgesic activity. 2-(Methylamino)benzoic acid was used to detect the metabolic levels of MMA in ratliver[1].
Enniatin A- 13C36 is the 13C-labeled Enniatin A (HY-N6702). Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using ratliver microsomes .
CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for ratliver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation .
Pyridaben (Standard) is the analytical standard of Pyridaben. This product is intended for research and analytical applications. Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: ratliver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function .
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for ratliver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation .
5-AIQ (5-Aminoisoquinolin-1-one) is a PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver .
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
L-Octanoylcarnitine (hydrochloride) (Standard) is the analytical standard of L-Octanoylcarnitine (hydrochloride) (HY-W354498). This product is intended for research and analytical applications. L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
5-AIQ hydrochloride is a PARP-1 inhibitor. 5-AIQ hydrochloride is an important functional group in various drugs. 5-AIQ hydrochloride reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver .
L-Octanoylcarnitine (Standard) is the analytical standard of L-Octanoylcarnitine. This product is intended for research and analytical applications. L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer .
5-AIQ (5-Aminoisoquinolin-1-one) is a PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver .
2,6-Dichloro-4-nitroaniline is an orally active Herbicide, Fungicide and uncoupler. 2,6-Dichloro-4-nitroaniline uncouples oxidative phosphorylation and inhibits electron transport. 2,6-Dichloro-4-nitroaniline induces biphenyl hydroxylase activity in ratliver. 2,6-Dichloro-4-nitroaniline increases the relative liver weight of rats via hepatomegaly without altering their body weight .
PiF is a fluorescent probe with high specificity for pancreatic β-cells (Ex/Em = 535 nm/565 nm), and its fluorescence signal increases significantly with elevated insulin concentrations in in vitro experiments. PiF enables visualization of rat and human islets transplanted via the portal vein in mouse livers with low liver background signals. The fluorine atom of PiF can be replaced by radioactive 18F to prepare a PET tracer. PiF can be used for research on type 1 diabetes .
Anordrin is a contraceptive agent. Anordrin exhibits estrogenicites and can induce decrease in serum progesterone levels in rat models. Anordrin inhibits endometrial epithelial cell mitosis and NAFLD induced by Tamoxifen (HY-13757A) in mouse uterus and liver as an anti-estrogenic and estrogenic agent .
BpV(pic) potassium hydrate is a PTEN inhibitor with IC50 31 nM. BpV(pic) potassium hydrate is also an insulin simulator that activates insulin receptor kinase in cultured liver cancer cells, stimulates adipogenesis in adipocytes, and inhibits the dephosphorylation of autophosphorylated insulin receptors and epidermal growth factor receptors in rat hepatosomes .
Allocholic acid is a typically fetal bile acid found in vertebrates and reappears during liver regeneration and carcinogenesis, besides it is also a conjugate acid of allocholate and an isomer of cholic acid. Allocholic acid is a potent and specific stimulant of the adult olfactory system, it has a role as a marine metabolite, a rat metabolite and a human metabolite .
Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using ratliver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
C10 Bisphosphonate is an acid sphingomyelinase (aSMase) inhibitor with an IC50 of 0.02 μM in rats. C10 Bisphosphonate inhibits Dexamethasone (HY-14648)-induced cell apoptosis (apoptosis) and alleviates platelet-activating factor (PAF)-induced pulmonary edema. C10 Bisphosphonate can be used for the research of pulmonary edema .
2,3-Oxidosqualene-d6 (Squalene oxide-d6) is a deuterium labeled 2,3-Oxidosqualene (HY-114296). 2,3-Oxidosqualene (Squalene oxide) is a sterol biosynthesis precursor intermediate.2,3-Oxidosqualene participates in cyclization pathways that form sterols and triterpenes, and contributes to introduction of their characteristic 3-hydroxyl group.2,3-Oxidosqualene forms metabolically from squalene in ratliver homogenates under sterol synthesis conditions.2,3-Oxidosqualene converts to sterols including cholesterol, lathosterol, and lanost-8-en-3β-ol in ratliver homogenates under anaerobic conditions.
URB-597 (Standard) is the analytical standard of URB-597. This product is intended for research and analytical applications. URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
Metyrapol is a steroid 11β-hydroxylase inhibitor. Metyrapol blocks the conversion of deoxycorticosterone to corticosterone in rat adrenal homogenates. Metyrapol can be used in the study of metabolic diseases .
BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for ratliverV1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease .
G256 (Compound 1) is an amidinohydrazone. G256 can also be considered as a Schiff’s base of aminoguanidine. G256 exhibits antiarrhythmic activity. G256 is the reduced form of NOH-G256 by microsomal enzyme preparation from rabbit and ratliver homogenates in the presence of NADPH and NADH .
2-(Methylamino)benzoic acid is the main metabolite of methyl-N-methylanthranilates (MMA) (HY-76705) and is the compound in which the ester group is converted. MMA can be isolated from citrus fruits and has potential analgesic activity. 2-(Methylamino)benzoic acid was used to detect the metabolic levels of MMA in ratliver .
1-(2-Amino-3-hydroxyphenyl)ethanone is the kynuridine metabolite, which could be extracted from ratliver mitochondrium. 1-(2-Amino-3-hydroxyphenyl)ethanone is associated with tryptophan metabolism disturbances, and can be used in bladder cancer, leukemia and anemia researches .
SMW139 is a selective allosteric antagonist of P2X7 receptor, with a Ki value of 32 nM for human P2X7R. The half-life of SMW139 in ratliver microsomes is 47 minutes. SMW139 can be used for inflammation, Alzheimer’s disease, multiple sclerosis study .
Gypsetin can inhibit acylcoenzyme A, cholesterol acyltransferase (ACAT) activity, inhibit ratliver microbody ACAT with an IC50 of 18 μM, and its action is competitive with oleoyl-COA substrate, Ki value is 5.5 μM. Gypsetin also inhibits Oleic acid from forming cholesterol esters with an IC50 of 0.65 μM .
G256 (Compound 1) (dihydrochloride) is an amidinohydrazone. G256 (dihydrochloride) can also be considered as a Schiff’s base of aminoguanidine. G256 (dihydrochloride) exhibits antiarrhythmic activity. G256 (dihydrochloride) is the reduced form of NOH-G256 by microsomal enzyme preparation from rabbit and ratliver homogenates in the presence of NADPH and NADH .
Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and ratliver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
Prunasin is an orally active cyanogenic glucoside and the main metabolite of Amygdalin (HY-N0190). Prunasin can specifically inhibit ratDNA polymerase β (IC50: 98 μM). Prunasin has anti-inflammatory and anti-fibrotic activities. Prunasin can be used in the research of diseases such as liver fibrosis .
3-(Boc-amino) propyl bromide is an alkylating reagent used for the N-alkylation of benzopyranotriazolopyrimidine-based MDM2-p53 protein-protein inhibitor 4 to prepare Compound 13 .
S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) is the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram (HY-B0240). It is produced by the methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) inhibits ratliver low Km aldehyde dehydrogenase (ALDH) (ID50=15.5 mg/kg). When administered at a dose of 20.6 mg/kg, it decreases mean arterial pressure (MAP) and increases heart rate in rats during ethanol stimulation.
D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders .
A-26771B is an antibiotic can be obtained from Penicillium turbatum. A-26771B exhibits moderate antimicrobial activity against Gram-positive bacteria, mycoplasma, and fungi. A-26771B also inhibits potassium-dependent ATPase in ratliver mitochondria .
Teglicar chloride (ST1326 chloride) is an orally active, reversible, mixed-type, selective inhibitor of hepatic carnitine palmitoyltransferase I (L-CPT I), with an IC50 of 1.1 μM against rat L-CPT I. Teglicar chloride reduces serum glucose levels. Teglicar chloride exhibits antiketotic activity in normal fasted rats. Teglicar chloride can be used in research related to type 2 diabetes and ketoacidosis .
A-769662 is a AMP-activated protein kinase (AMPK) activator. A-769662 inhibits the function of the 26S proteasome by an AMPK-independent mechanism and leads to cell cycle arrest. A-769662 directly stimulates partially purified ratliver AMPK (EC50 = 0.8 μM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 μM). A-769662 can alleviate the symptoms of metabolic diseases such as type 2 diabetes .
CI-996 is a potent, selective, orally active angiotensin II (Ang II) type 1 (AT1) receptor antagonist. In ratliver membranes CI-996 displaces specifically bind [ 125I]Ang II with an IC50 of 0.8 nM. CI-996 has blood pressure-lowering activity .
CL 277082 is a potent and selective acyl CoA:cholesterol acyltransferase (ACAT) inhibitor in microsomes. CL 277082 inhibits ACAT with IC50 values of 0.14 μM for intestinal mucosal microsomes, 0.74 μM for liver, and 1.18 μM for rat adrenal. CL 277082 is a ACAT-catalyzed cholesterol esterification and cholesterol absorption inhibitor .
Dopamine D3 receptor agonist 1 is a dopamine D3 Receptor agonist with a Ki value of 0.268 nM. Dopamine D3 receptor agonist 1 exhibits metabolic stability in ratliver microsomes. Dopamine D3 receptor agonist 1 can be used to study severe mental disorders comorbid with substance use disorders .
CGP 44 645 (Standard) is the analytical standard of CGP 44 645. This product is intended for research and analytical applications. CGP 44 645 is the methanol metabolite of Letrozole (HY-14248) and is a molecular indicator for evaluating its metabolic kinetics in microsomes in vitro. Levels of CGP 44 645 in ratliver microsomes may be sex-specific .
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in ratliver microsomes .
BM 170249 is a peroxisome proliferator, particularly in the perivenous region of the central acini in the liver. BM 170249 significantly reduces serum triglyceride and cholesterol levels in rats. BM 170249 strongly induces the activity of key enzymes in the peroxisome fatty acid β-oxidation system (such as acyl-CoA oxidase AOX, multifunctional enzyme PH, and thiolase PT), but leads to decreased activity of catalase and uricase in peroxisome components. BM 170249 could be used in lipid-lowering studies .
4-Hydroxypropranolol hydrochloride is a non-cardiac selective β-adrenergic receptor antagonist and a metabolite produced after oral administration of Propranolol (HY-B0573B). 4-Hydroxypropranolol hydrochloride also acts as a membrane stabilizer and possesses intrinsic sympathomimetic inhibitory activity. 4-Hydroxypropranolol hydrochloride blocks β-adrenergic receptors to antagonize the effects of catecholamines, acts as a partial β-adrenergic receptor agonist, and induces membrane stabilization. 4-Hydroxypropranolol hydrochloride alters heart rate, left ventricular contractility, and atrioventricular conduction time. 4-Hydroxypropranolol hydrochloride can be used in research related to cardiovascular and cerebrovascular diseases .
SARS-CoV-2 3CLpro-IN-37 is a non-covalent SARS-CoV-2 3CLpro inhibitor with an IC50 of 3.2 nM. SARS-CoV-2 3CLpro-IN-37 blocks the cleavage and replication of viral polyproteins. SARS-CoV-2 3CLpro-IN-37 is applicable to research related to COVID-19 .
MD-230254 is a reversible, competitive and selective inhibitor inhibitor of MAO-B with an IC50 value of 1.8 nM. MD-230254 can be used for the study of MAO-B-related neurodegenerative diseases including Parkinson’s disease and Alzheimer’s disease .
6-Aminochrysene (Standard) is the analytical standard of 6-Aminochrysene (HY-108315). This product is intended for research and analytical applications. 6-Aminochrysene (6-Aminochrysene) is an aromatic amine used as a chemotherapeutic agent in the treatment of splenomegaly, myeloid leukemia, and breast cancer. 6-Aminochrysene is activated by CYP450 in ratliver .
CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and ratliver microsomes .
TLR9-IN-3 is a TLR9 antagonist with an IC50 of 0.4 μM. TLR9-IN-3 shows selectivity for TLR4 and TLR8, and inhibits CD69 activation in human whole blood with a corresponding IC50 of 1.1 μM. TLR9-IN-3 can be used in research related to pulmonary fibrosis .
Acetyl tributyl citrate (Tributyl O-acetylcitrate) is a pharmaceutical excipient and biodegradable hydrophobic plasticizer. Acetyl tributyl citrate can be used in cosmetics, food packaging, and as a flavoring substance for food .
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone .
Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
11-Dehydrodexamethasone, Dexamethasone (HY-14648) derivative, is a substrate for 11β-hydroxysteroid dehydrogenase (11β-HSD) 1/2. 11-Dehydrodexamethasone undergoes conversion to Dexamethasone via reductive activity of 11β-HSD .
Moveltipril calcium (MC-838 calcium) is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Moveltipril calcium binds via a stable thioester bond and exhibits relative resistance to enzymatic hydrolysis in ratliver homogenate. Moveltipril calcium effectively inhibits ACE extracted from rabbit lung in a concentration-dependent manner. Moveltipril calcium is able to highly specifically inhibit the contractile response to angiotensin-I (AI) in free rat aortic rings and guinea pig ileum preparations, while enhancing the contractile response to calcitonin .
Epyrifenacil is a protoporphyrinogen oxidase (PPO) inhibiting herbicide, potently targeting the PPO2 isoform from weeds such as Amaranthus palmeri with an IC50 of 0.637 nM. Epyrifenacil also inhibits liver mitochondrial PPO across species, with IC50 values of 2.2 nM (mouse), 2.6 nM (rat), 12.1 nM (rabbit), 7.6 nM (dog), and 10.2 nM (human). Epyrifenacil induces liver tumor development in mice. Epyrifenacil can be used for weed control, and also used as a tool compound in toxicological research to study the mechanism of PPO inhibition, chemical-induced hepatotoxicity, and the mode of action of non-genotoxic carcinogens in rodents [3].
2-Phenylpropionic acid (Standard) is the analytical standard of 2-Phenylpropionic acid (HY-W015608). This product is intended for research and analytical applications. 2-Phenylpropionic acid is an intermediate in the metabolism of alpha-Methylstyrene. 2-Phenylpropionic acid covalently binds to ratliver protein. 2-Phenylpropionic acid can be used in the research of nonsteroidal anti-inflammatory agents .
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated ratliver mitochondria .
Mycobacterium Tuberculosis-IN-5 (Compound 11) is the HCl salt form of 5-Fluoroindole (HY-40156). Mycobacterium Tuberculosis-IN-5 is an antibacterial agent, that inhibits Mycobacterium tuberculosis with a MIC of 29.1 μM. Mycobacterium Tuberculosis-IN-5 exhibits metabolic stability in ratliver microsomes. Mycobacterium Tuberculosis-IN-5 exhibits anti-tuberculosis efficacy in mice .
C22-Ceramide (d18:1/22:0) (Cer d18:1/22:0) is an endogenous bioactive sphingolipid. C22-Ceramide (d18:1/22:0) reduces the propensity of C16-ceramide channel formation in isolated ratliver mitochondria and in liposomes .
SC-26196 (Standard) is the analytical standard of SC-26196 (HY-107410). This product is intended for research and analytical applications. SC-26196 is a potent, orally active Delta6 desaturase (D6D, FADS2) inhibitor (IC50=0.2 μM in a ratliver microsomal assay). Antiinflammatory properties .
Filiformin ((-)-Filiformin) is a sesquiterpene compound that can be isolated from Laurencia filiformis forma heteroclada. Filiformin exhibits certain cytotoxicity against P388 and BSC-1 cells. Filiformin has antimicrobial activity against Bacillus subtilis, Trichophyton mentagrophytes and Candida albicans. In addition, Filiformin can inhibit oxygen uptake in isolated ratliver mitochondria at a concentration of 150 μM .
(S)-(-)-Felodipine is a S-enantiomer of Felodipine. (S)-(-)-Felodipine is an antihypertensive agent. Felodipine is a 1,4-dihydropyridine derivative and a vasoselective calcium antagonist. Felodipine can prevent the activation of the vascular effector cells and interfere with the contractile process in vitro. Felodipine lowers mean arterial blood pressure by 20% in dog model. (S)-(-)-Felodipine shows high metabolic rate in rat and dog liver microsomes .
(±)13-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in ratliver, brain, and intestinal microsomes. Fresh water hydra is shown to metabolize DHA to 13(R)-HDHA, presumably via the 11R-lipoxygenase activity. (±)13-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
Tauromustine is an orally active nitrosourea anticancer agent. Tauromustine has an alkylation effect and can damage the DNA function. Tauromustine has a high therapeutic index, especially in the study of Walker 256 rat sarcoma. It is also active against melanoma, breast cancer, pleural mesothelioma and ovarian cancer. Tauromustine is mainly metabolized in the liver, but some of its metabolites also have cytotoxicity .
Cerebrocrast (IOS-1.1212) is a 1,4-dihydropyridine (DHP) derivative. Cerebrocrast has a high affinity for the membrane lipid bilayer and it can easily penetrate the blood-brain barrier and incorporate into the plasma and organelle membranes, including those of mitochondria. Cerebrocrast promotes the cotransport of H+ and Cl- in ratliver mitochondria. Cerebrocrast also exhibits neuroprotective and cognition enhancer properties .
Cyclamidomycin (Desdanine) is an acrylamide antibiotic with antibacterial activity. Cyclamidomycin inhibits nucleoside diphosphate kinase and pyruvate kinase (in E. coli) and oxidative phosphorylation in ratliver mitochondria. Cyclamidomycin is active against S. aureus, M. flavus, S. lutea, B. subtilis, E. coli, S. flexneri, S. typhosa, P. vulgaris, and K. pneumoniae (MICs=3.12-25 mg/ml) .
CAA-0225 is a tissue protease L inhibitor that inhibits ratliver tissue protease L with a IC50 value of 1.9 nM. CAA-0225 can participate in the degradation of autophagosome membrane markers LC3-II and GABARAP (HY-P72639), improve cardiac function in mice with reperfusion injury, and kill and eliminate Trypanosoma brucei parasites [1][2][3].
3-Pyridineacetic acid (Standard) is an analytical standard for 3-Pyridineacetic acid (HY-W015806). This product is for research and analytical applications. 3-Pyridineacetic acid is an orally active nicotinic acid analog. 3-Pyridineacetic acid enhances cholesterol oxidation in ratliver mitochondria. 3-Pyridineacetic acid inhibits Triton-induced hypercholesterolemia in rats. 3-Pyridineacetic acid can be used in research related to hypercholesterolemia.
L 668411 is a β-lactone inhibitor with activity against 3-hydroxy-3-methylglutaryl-CoA synthase and cholesterol biosynthesis. L 668411 inhibits ratliver cytosolic 3-hydroxy-3-methylglutaryl-CoA synthase and [14C] acetate incorporation into sterols in cultured Hep G2 cells, and the inhibition appears to be irreversible in cells but reversible in cultured cells and animals.
SX-576 is a CXCR1 and CXCR2 antagonist with IC50 values of 31 nM and 21 nM, respectively. SX-576 inhibits neutrophil infiltration in a rat model of pulmonary inflammation. SX-576 can be used in studies related to pulmonary inflammation .
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .
Neomangiferin is an orally active natural flavonoid. Neomangiferin partially ameliorates non-alcoholic fatty liver disease (NAFLD) by regulating the expression of genes related to free fatty acid uptake and lipid oxidation. Neomangiferin exerts anti-colitis effects by inhibiting Th17/Treg cell differentiation. Neomangiferin exerts anti-aging and lifespan-extending effects by targeting upregulation of bas-1, which in turn activates the autophagy, IIS and MAPK pathways. Neomangiferin has the potential to prevent aseptic loosening of prostheses after total joint arthroplasty due to its significant anti-inflammatory and osteoclastogenesis-inhibiting effects .
Enniatin B- 13C33 is the 13C-labeled Enniatin B (HY-N3806). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using ratliver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in ratliver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
Imiprothrin is an inducer that induces CYP1A2 and metallothionein 1a, with significant genotoxicity and cytotoxicity. In rat hepatocytes, Imiprothrin initiates detoxification responses by triggering the overexpression of these two genes. Imiprothrin induces chromosomal aberrations and micronucleus formation in rat bone marrow cells, and causes DNA damage in hepatocytes. Imiprothrin triggers oxidative stress in rats, leading to lipid peroxidation, excessive reactive oxygen species production and redox imbalance, which in turn impairs liver and kidney functions and causes tissue damage. Imiprothrin inhibits weight gain in mice, and even causes high mortality in female mice at high doses. However, it shows no carcinogenicity in rat experiments; among relevant indicators, aspartate aminotransferase and total protein are identified as sensitive toxicity biomarkers .
Chloramphenicol succinate sodium is a prodrug of Chloramphenicol (HY-B0239), acting as a P2Y14R inhibitor with an IC50 of 1.585 nM. Chloramphenicol succinate sodium serves as a competitive substrate and inhibitor of succinate dehydrogenase (SDH), which may account for its toxicity. Chloramphenicol succinate sodium exerts a significant inhibitory effect on colitis. Chloramphenicol succinate sodium can be used in research related to myelosuppression, gray baby syndrome, aplastic anemia, bacterial meningitis and inflammatory bowel disease .
22-HDHA (22-Hydroxy Docosahexaenoic acid) is an oxidation product of docosahexaenoic acid. In vitro, it is formed upon incubation of ratliver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
1,2,3-Tritridecanoyl glycerol is a synthetic triacylglycerol that contains tridecanoic acid in the sn-1, sn-2, and sn-3 positions. It has been used as a standard for the relative quantification of triacylglycerols in C. elegans fat stores. It has also been used as an internal standard for the quantification of triacylglycerols in the serum and liver of adult rat offspring receiving dietary conjugated linoleic acids during and after gestation.
2-Phenyl-2-(2-pyridyl)acetonitrile (Standard) is the analytical standard of 2-Phenyl-2-(2-pyridyl)acetonitrile. This product is intended for research and analytical applications. 2-Phenyl-2-(2-pyridyl)acetonitrile is the major metabolite of SC 15396 metabolized by the supernatant fraction of ratliver homogenate. SC 15396 is an antigastrin that inhibits gastric secretion[1].
α-Glucosidase-IN-110 is a selective and orally active competitive inhibitor of α-Glucosidase with an IC50 of 7.09 μM and a Ki of 6.9 μM. α-Glucosidase-IN-110 can reduce fasting blood glucose levels, improve glucose tolerance, and restore the histomorphology of liver and pancreatic tissues in diabetic rat models. α-Glucosidase-IN-110 can be used for the research of diabetes .
ACT-774312 is a potent and selective CRTH2 antagonist with an IC50 of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD2-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.
ZDZ-553 is an orally active STAT1 inhibitor with an IC50 value of 0.87 μM. ZDZ-553 modulates STAT1 signaling to affect downstream lipid metabolism and inflammatory pathways. ZDZ-553 attenuates hepatic steatosis in NASH mouse models. ZDZ-553 reduces inflammatory responses in NASH mouse models. ZDZ-553 can be used for the research of nonalcoholic steatohepatitis .
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated ratliver microsomes.
4-Hydroxy nonenal glutathione (4-HNE-GSH) TFA is the primary metabolite of 4-Hydroxy-2-nonenal. 4-Hydroxy nonenal glutathionea TFA is a marker of oxidative stress in ratliver and hepatocytes. 4-Hydroxy nonenal glutathione TFA efficiently prevents formation of DNA adducts with 4-Hydroxy-2-nonenal in human cells .
NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC50 values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC50 of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis .
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research .
BMS-962212 is a factor XIa (FXIa) inhibitor with a Ki of 0.7 nM against human FXIa and a Ki of 3 nM against rabbit FXIa. BMS-962212 blocks thrombosis while preserving normal hemostatic function. BMS-962212 is applicable to thrombosis-related research .
Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain .
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and ratliver microsomes .
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
PDE1-IN-9 (Compound 7a) is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 exhibits good metabolic stability in ratliver microsomes .
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using ratliver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for ratliver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED .
A2AAR antagonist 3 is a selective and potent A2A adenosine receptor (A2A AR) antagonist with an IC50 of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A2A AR. A2AAR antagonist 3 demonstrates favorable stability in ratliver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.
PDE1-IN-9 (Compound 7a) hydrochloride is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 hydrochloride reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 hydrochloride exhibits good metabolic stability in ratliver microsomes .
Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
FXR DUBTAC modulator-1 is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC modulator-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC modulator-1 can be used in the research of cholestatic liver injury .
PDE7A-IN-1 is an orally active and selective PDE7A inhibitor with an IC50 of 0.0037 μM against PDE7A. PDE7A-IN-1 shows excellent isozyme selectivity over PDE7B. PDE7A-IN-1 elevates intracellular cAMP levels, suppresses ECR5 enhancer activity and reduces sclerostin expression. PDE7A-IN-1 significantly increases bone mineral density in rats. PDE7A-IN-1 can be used for the study of osteoporosis .
IKK2-IN-5 is a selective IKK-2 inhibitor with an IC50 of 0.025 μM. IKK2-IN-5 inhibits the production of TNF-α in LPS (HY-D1056)-stimulated human peripheral blood mononuclear cells. IKK2-IN-5 exhibits extremely low cytotoxicity against human peripheral blood mononuclear cells .
3-Ethoxybenzamide is an alkoxybenzamide compound with antibacterial activity and a FtsZ inhibitor that can cross the blood-brain barrier. 3-Ethoxybenzamide distributes widely and rapidly in vivo, rapidly reaches equilibrium between various tissues and blood, and is linearly taken up by hepatocytes. 3-Ethoxybenzamide is completely dependent on hepatic microsomal oxidation for clearance, with salicylamide as its major metabolite. 3-Ethoxybenzamide can be used for the study of bacterial infections .
ABBV-011 (SC-011) is a SEZ6-targeted, antibody-drug conjugate (ADC). ABBV-011 binds cell surface-expressed SEZ6 by anti-SEZ6 antibody Turmetabart (HY-P991041), triggers ADC-receptor complex internalization into lysosomes, releases Calicheamicin (HY-19609) payload, and mediates cytotoxicity. ABBV-011 induces tumor regression and mediates selective killing of SEZ6-positive cells. ABBV-011 can be used for the research of small cell lung cancer .
3-Methyl-2-nitrophenol is a UDP-glucuronyltransferase (EC 2.4.1.17) acceptor substrate that can be confirmed to undergo glucuronidation catalyzed by the enzyme to form a glucuronide conjugate. 3-Methyl-2-nitrophenol functions as a substrate for conjugation, with glucuronidation forming a glucuronide conjugate that eliminates the parent compound’s characteristic yellow color. 3-Methyl-2-nitrophenol has higher lipid solubility that contributes to high glucuronidation conversion rate, and exhibits lower absorbance at 340 nm to act as a less interfering substrate for the NADH-NAD +-linked UDP-glucuronyltransferase assay .
SRI-35241 is a thrombospondin TSP-1 inhibitor with a pIC50 of 8.12 nM against human targets. SRI-35241 inhibits the binding of TSP-1 to latent transforming growth factor-β-associated peptide (LAP) and blocks the activation of TGF-β. SRI-35241 shows a certain time-dependent property, with a plasma half-life of 1.8 h after intravenous administration. SRI-35241 can be used for the research of multiple myeloma and fibrotic diseases .
Enniatin A1- 13C35 is the 13C-labeled Enniatin A1 (HY-N6704). Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in ratliver microsomes .
RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .
ACC2-IN-1 is an orally active, selective inhibitor of acetyl-CoA carboxylase 2 (ACC2), with an IC50 of 1.9 nM against human targets. ACC2-IN-1 acts as a reducing agent to decrease malonyl-CoA levels in skeletal muscle and exhibits a favorable CYP450 inhibition profile. ACC2-IN-1 can be used in the research of type 2 diabetes .
Sodium Channel inhibitor 1 is a state-dependent voltage-gated NaV1.7 inhibitor with an IC50of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain .
CYP11B1-IN-1 (Compound 25) is a selective, orally active hCYP11B1 inhibitor, with an IC50 of 2 nM against hCYP11B1 and an IC50 of 1.8 μM against rat CYP11B1. CYP11B1-IN-1 can be used for the research of Cushing's disease .
Incadronate disodium (YM 175) is a bisphosphonate with strong inhibitory activity on bone resorption. Incadronate disodium indirectly stimulates renal 25-hydroxyvitamin D-1-hydroxylase by increasing circulating parathyroid hormone. Incadronate disodium, a cholesterol-lowering agent, is a potent inhibitor of ratliver microsomal squalene synthase (Ki=57 nM). Incadronate disodium inhibits sterol biosynthesis in mouse macrophage J774 cells (IC50=64 μM). Incadronate disodium has the potential for malignant tumors research .
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
4'-Hydroxychalcone (Standard) is the analytical standard of 4'-Hydroxychalcone (HY-N7056). This product is intended for research and analytical applications. 4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated ratliver mitochondria .
A-81282 (Abbott 81282) is an antagonist of angiotensin II's AT1 receptor, with a pA2 value of 9.64 at the AT1 receptor in rabbit aorta. A-81282 also demonstrates significant inhibitory action on the binding of [125i]_Sar1_lle8_Angiotensin_ll to ratliver membranes, with a pKI value of 8.505. A-81282 has antihypertensive activity and can effectively lower blood pressure in renal artery-ligated rats .
Leukotriene E3 is a cysteinyl leukotriene metabolite derived from 5,8,11-eicosatrienoic acid (HY-108398A). Leukotriene E3 acts as a smooth-muscle-contracting mediator. Leukotriene E3 can be used for the research of allergic reactions and asthma .
Chitobiose is an orally active chitosan oligosaccharide (degree of polymerization 2). Chitobiose shows hepatoprotective activity and counteracts CCl4-induced elevation of plasma aspartate transaminase and alanine transaminase activities in rats. Chitobiose can be used for the research of carbon tetrachloride-induced acute hepatotoxicity .
HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1) .
Thrombin inhibitor 11 (Compound 46) is an orally active, competitive and selective α-Thrombin inhibitor, with a Ki value of 65 nM against h-αThrombin and a Ki value of 10.3 nM against rat-derived α-thrombin. Thrombin inhibitor 11 can be used for the research of thrombotic diseases .
α-Triglycidyl isocyanurate (Teroxirone) is an antitumor compound with activity to inhibit DNA replication. α-Triglycidyl isocyanurate exerts its anticancer effect by alkylating and cross-linking DNA. α-Triglycidyl isocyanurate is relatively stable in fresh human plasma and whole blood, showing good biocompatibility. The metabolism of α-Triglycidyl isocyanurate mainly occurs in ratliver and is metabolized through an NADPH-independent pathway. The cytotoxicity of α-Triglycidyl isocyanurate can be partially restored under specific conditions, suggesting the complexity of its metabolic pathway .
Propiconazole-d3 (nitrate) is the deuterium labeled Propiconazole nitrate. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not ratliver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not ratliver, microsomal cytochrome P450 (IC50s=0.04 and >200 μM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 μg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS) .
6-(L-1,2,3-Trihydroxybutyl)-pterin is a derivative of L-biopterin (HY-102015) and is the oxidized form of tetrahydro-L-biopterin (BH4) as well as D-biopterin. Co-ingestion of 6-(L-1,2,3-Trihydroxybutyl)-pterin (0.5%) with the carcinogen 4-dimethylaminoazobenzene reduces the incidence of 4-dimethylaminoazobenzene-induced liver tumors in rats. 6-(L-1,2,3-Trihydroxybutyl)-pterin has been used as an internal standard for the LC-MS quantification of biopterin and neopterin in rat plasma.
Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
BPN-14136 is an orally effective retinol-binding protein 4 (RBP4) inhibitor. BPN-14136 inhibits the binding of retinol to RBP4 with an IC50 of 12.8 nM. BPN-14136 inhibits retinol-dependent RBP4-transthyretin interaction (IC50 = 43.6 nM) and reduces circulating plasma RBP4 levels in vivo. BPN-14136 decreases the formation of cytotoxic bisretinoids in retinal pigment epithelial cells. BPN-14136 can be used for the research of atrophic age-related macular degeneration and Stargardt disease .
VU6077967 is a selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 8.6 nM for rCB2. VU6077967 can be used for the research of neurological disease, suah as Alzheimer’s disease .
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease . Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
Enniatin B1- 13C34 is the 13C-labeled Enniatin B1 (HY-N3807). Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using ratliver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
Ro 13-3978 is an orally active antischistosomal agent. Ro 13-3978 exhibits excellent in vivo antischistosomal activity against juvenile and adult Schistosoma mansoni infections. Ro 13-3978 shows no in vivo activity against E. caproni and F. hepatica. Ro 13-3978 blocks dihydrotestosterone-induced proliferation of androgen-dependent cells. Ro 13-3978 can be used in research related to schistosomiasis .
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
CM398 is a highly selective, orally active Sigma-2 receptor ligand with a Ki value of 0.43 nM. CM398 ameliorates age-related macular degeneration. CM398 exerts analgesic effects on visceral pain, inflammatory pain and neuropathic pain. CM398 can be used in research related to age-related macular degeneration, neuropathic pain and inflammatory pain .
Dehydromonocrotaline is a mitochondrial respiratory chain complex I NADH oxidase inhibitor, with a IC50 of 62.06 μM and a Ki of 8.1 μM in rats. Dehydromonocrotaline exerts non-competitive inhibitory effects by modifying cysteine thiol groups on complex I, and does not bind to the NADH-binding site. Dehydromonocrotaline dissipates mitochondrial membrane potential and reduces ATP levels. Dehydromonocrotaline can be used in studies related to hepatotoxicity, pulmonary hypertension and liver tumors .
IBA-12 is a IKZF2molecular glue/PROTAC degrader with a DC50 of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC50 of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research .
3-(N-Maleimidopropionyl)biocytin is a cysteine-specific labeling reagent and non-membrane-permeable probe. 3-(N-Maleimidopropionyl)biocytin covalently modifies the exposed cysteine residues of yeast Tim44, conjugating the biotin moiety to the polypeptide chain. 3-(N-Maleimidopropionyl)biocytin determines the topology of membrane proteins by modifying the exposed cysteine residues on the outer side of the inner mitochondrial membrane .
Acetaminosalol, a merged ester NSAID–APAP hybrid, is a metabolite of Benorylate (HY-107795) and a prodrug of Acetaminophen (HY-66005) and Aalicylic acid (HY-B0167). Acetaminosalol can be used for the research of acute rheumatism .
2'-Thiouridine is a key modified nucleoside at the wobble position of tRNA anticodons. 2'-Thiouridine mainly exists in tRNAs for glutamic acid, glutamine, lysine, etc., and participates in precise decoding regulation .
Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and ratliver microsomes .
Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced ratliver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis .
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
Tetrahydrocorticosterone is a glucocorticoid. One of its active forms, 5α-Tetrahydrocorticosterone (HY-113364), exerts its effects by binding to the GC receptor and inhibiting inflammatory processes. Tetrahydrocorticosterone is naturally synthesized by the adrenal glands and plays a key role in regulating the metabolism of carbohydrates, proteins and fats .
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guinea pigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .
17-Hydroxystearic acid isolable from Torulopsis magnoliae fermentation oil. 17-Hydroxystearic acid is a saturated C18 ω2-hydroxy fatty acid existing in D- and L-enantiomeric forms .
Hepcidin-25 (human) is an iron metabolism regulator and Antimicrobial agent. Hepcidin-25 (human) exerts anti-inflammatory and antimicrobial activities by regulating iron-mediated oxidative damage .
Bilirubin diglucuronide is a bilirubin glycoside conjugate with a 1-O-acyl β-D-glucuronide structure. Bilirubin diglucuronide is the major conjugated bilirubin (HY-N0323) and predominant pigment excreted in the bile of adult humans, rats, dogs and cats. Bilirubin diglucuronide is mainly synthesized via UDP-glucuronosyltransferase-mediated transfer of glucuronic acid from UDP-glucuronic acid to bilirubin monoglucuronide, or via enzymatic disproportionation of two moles of bilirubin monoglucuronide (predominantly producing the IXα configuration). In addition, Bilirubin diglucuronide can also be synthesized from bilirubin or its monoglucuronide in a UDP-glucuronic acid-dependent manner. Pretreatment with phenobarbital significantly enhances the formation process of Bilirubin diglucuronide .
Octoclothepine (Clorotepine), an analog of Clozapine (HY-14539), is a neuroleptic and antipsychotic agent. Octoclothepine exists in enantiomeric forms, where the (+)-form acts as an atypical antipsychotic, while the (-)-functions as a typical antipsychotic. (+)-Octoclothepine exhibits extremely high binding affinity for 5-HT₆ and 5-HT₇ receptors, with Ki values of 0.41 and 0.38 nM; the Ki values of (-)-Octoclothepine are 17.7 and 1.3 nM, respectively. Octoclothepine can be used in research related to schizophrenia .
MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain .
Rilmazafone (450191S) is an orally active sleep inducer. Rilmazafone targets cytochrome P-450b and cytochrome P-450e. Rilmazafone induces hepatic drug-metabolizing enzyme activity in rats, mice and dogs. Rilmazafone is applicable for insomnia-related research .
Oxalic acid, 99% (Ethanedioic acid) is a dicarboxylic acid found in a wide variety of plants. Oxalic acid, 99% shows antioxidant acyivity and suppresses lipid peroxidation. Oxalic acid, 99% is a pathogenicity factor for sclerotinia sclerotiorum, and suppresses the oxidative burst of the host plant. Oxalic acid, 99% exerts acaricidal activity. Oxalic acid can be used for the researches of sclerotinia disease, varroatosis and inflammatory diseases .
BODIPY FL-C16 is a BODIPY-labeled analog of Palmitic acid (HY-N0830), which serves as a fluorescent lipid tracer. BODIPY FL-C16 also acts as a ligand for liver fatty acid-binding protein (L-FABP) and intestinal fatty acid-binding protein (I-FABP) , with Kd values of 270 nM and 330 nM, respectively. BODIPY FL-C16 is rapidly taken up by cells, and after metabolic conversion to phospholipids, it is incorporated into the membrane structures of intracellular organelles and extracellular vesicles .
Oxalic acid (Ethanedioic acid) diammonium monohydrate is a dicarboxylic acid found in a wide variety of plants. Oxalic acid diammonium monohydrate shows antioxidant acyivity and suppresses lipid peroxidation. Oxalic acid diammonium monohydrate is a pathogenicity factor for sclerotinia sclerotiorum, and suppresses the oxidative burst of the host plant. Oxalic acid diammonium monohydrate exerts acaricidal activity. Oxalic acid can be used for the researches of sclerotinia disease varroatosis and inflammatory diseases .
Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
Anti-Mouse CD8α Antibody (2.43) is an anti-mouse CD8α IgG2b monoclonal antibody. Anti-Mouse CD8α Antibody (2.43) can significantly deplete CD8 + T cells. Anti-Mouse CD8α Antibody (2.43) can prolong the survival time of liver cell transplantation. Anti-Mouse CD8α Antibody (2.43) can be used for research on immunology. The recommend isotype control of Anti-Mouse CD8α Antibody (2.43): Rat IgG2b kappa, Isotype Control (HY-P990682) .
Xipamide is an orally active carbonic anhydrase (CA) inhibitor and Na +/Cl --potassium transporter inhibitor with diuretic and antihypertensive effects. Xipamide reduces NaCl reabsorption by inhibiting the Cl -/NaCO3- anion exchanger, and increases calcium reabsorption while promoting potassium and magnesium excretion. Xipamide is mainly cleared via the renal pathway and causes a temporary decrease in glomerular filtration rate under specific conditions. Xipamide does not affect Ca 2+ signaling induced by endothelin-1 and other factors, nor does it inhibit various ion cotransport or pump activities in red blood cells. Xipamide can be used in researches related to cardiovascular diseases, hypertension (especially with left ventricular hypertrophy), advanced renal failure, and liver cirrhosis with ascites .
ERAP1-IN-4 is an orally acvtive endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with a pIC50 of 7.9 and an LLE of 5.3. ERAP1-IN-4 inhibits hydrolysis of peptide substrates by ERAP1, with high activity against Allotype1 and Allotype2. ERAP1-IN-4 reduced efficacy against other allotypes, and modulates ERAP1-mediated peptide processing to inhibit antigenic epitope presentation. ERAP1-IN-4 can be used for the research of cancer[1].
Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies .
Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain .
BI-1388 is a macrocyclic acylsulfonamide-based HCVNS3-4A protease inhibitor. BI-1388 inhibits clinically relevant drug-resistant mutant strains (KRAS D168V gt 1b and KRAS R155K gt 1a) and exhibits high liver distribution. BI-1388 is applicable for the research of HCV infection .
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in ratliver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
Dibenzo (a,i) pyrene is a polycyclic aromatic hydrocarbon and also a carcinogenic ligand of the TCDD (Ah) receptor. Dibenzo (a,i) pyrene binds to the TCDD (Ah) receptor in ratliver. Dibenzo (a,i) pyrene induces DNA adduct formation and upregulates the protein levels of p53 and p21 WAF1 in diploid lung fibroblasts. Dibenzo (a,i) pyrene alters the cell cycle distribution of diploid lung fibroblasts, increasing the proportion of cells in the S phase, decreasing the proportions of cells in the G0/G1 and G2/M phases, and causing S phase delay/arrest. Dibenzo (a,i) pyrene is applicable for cancer research .
Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms .
Captopril disulfide (SQ 14551) is an orally active disulfide dimer prodrug. Captopril disulfide is metabolized to Captopril and acts as a Bradykinin potentiator. Captopril disulfide enhances the vasodilatory effect of Bradykinin in anesthetized rats and the contractile response of isolated guinea pig ileum to Bradykinin. Captopril disulfide exhibits antihypertensive activity in spontaneously hypertensive rats. Captopril disulfide can be used in hypertension-related research .
Dezaguanine is a purine analog. Dezaguanine exhibits antitumor activity in leukemia and breast cancer cells. Dezaguanine can be used in cancer-related research .
Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis .
Nuarimol is a fungicide used for plant protection in agriculture. Nuarimol is a phenobarbital-type inducer of hepatic drug-metabolizing enzymes. It triggers transient but robust regenerative hepatocyte proliferation accompanied by hepatomegaly by causing reversible hepatocellular injury .
Fraxinuacidoside functions as a norditerpene glucopyranoside with a unique carbon skeleton. Fraxinuacidoside can be found in the stem bark of Fraxinus sieboldiana .
Ferroptosis-IN-24 is a non-classical ferroptosis inhibitor capable of crossing the blood-brain barrier, with nanomolar inhibitory activity against ferroptosis induced by RSL3 (HY-100218A) and Erastin (HY-15763). Ferroptosis-IN-24 alleviates oxidative stress, reduces lipid peroxidation accumulation, and restores redox homeostasis. Ferroptosis-IN-24 is applicable to research related to cerebral ischemia-reperfusion injury and acute liver injury .
(rac)-5-Hydroxykynurenine is a urinary metabolite. (rac)-5-Hydroxykynurenine is generated via indole ring oxidative cleavage of 5-hydroxytryptophan (HY-N0122) catalyzed by indoleamine 2,3-dioxygenase .
c-Met-IN-29 is an orally active c-Met inhibitor with an IC50 of 1.6 nM. c-Met-IN-29 binds to and functionally modulates c-Met protein, inhibiting tumor cell proliferation, migration and apoptosis. c-Met-IN-29 exhibits anti-tumor activity both in vitro and in vivo. c-Met-IN-29 can be used for the research of non-small cell lung cancer .
9-Oxononanoic acid (9-ONA) is an orally active acetyl-CoA carboxylase inhibitor. 9-Oxononanoic acid inhibits acetyl-CoA carboxylase via accumulation of long-chain acyl-CoA. 9-Oxononanoic acid increases carnitine palmitoyltransferase, isocitrate dehydrogenase and glucose 6-phosphate dehydrogenase activity to elevate β-oxidation and support NADPH (HY-113324) supplyactivity. 9-Oxononanoic acid stimulates phospholipase A2 activity via post-translational, non-transcriptional mechanisms. 9-Oxononanoic acid can be used for the research of atherothrombosis .
2'-Deoxy-N-methyl-AMP ammonium is an N6-substituted adenine nucleotide derivative and a glycosyl donor. On one hand, 2'-Deoxy-N-methyl-AMP ammonium acts as a specific substrate for N6-methyl-AMP aminohydrolase, and it is catalytically converted to dIMP to participate in the nucleotide metabolic cycle. On the other hand, 2'-Deoxy-N-methyl-AMP ammonium also serves as a guanosine diphosphate (GDP)-linked fucose derivative donor, driving site-specific glycoconjugation of proteins under the mediation of α-1,3-fucosyltransferase. 2'-Deoxy-N-methyl-AMP ammonium is an important molecular tool for investigating the mechanisms of nucleotide modification and protein glycosylation .
DLK-IN-2 is a selective inhibitor of DLK and neuroprotective agent. DLK-IN-2 shows no significant inhibition against CYPs 3A4, 2D6 and 2C9. DLK-IN-2 inhibits acute axonal palmitoylation of DLK, blocks DLK-dependent pro-degenerative axon-to-soma retrograde signaling and suppresses c-Jun phosphorylation. DLK-IN-2 can be used for the mechanistic study of neurodegenerative diseases .
Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis .
Azidocillin, a semi-synthetic Penicillin, is an orally active β-lactam antibiotic. Azidocillin bears an azide functionality and retains on-target activity within bacteria. Azidocillin can be used to research osteitis caused by dental surgery, otitis media, enterococcal septicemia and other bacterial infectious diseases . Azidocillin is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
R214127 is a selective mGlu1 receptor antagonist with IC50 values of 6 and 14 nM for rat and human mGlu1a. R214127 acts on a site from the glutamate binding pocket, and competes for the same transmembrane segment VII as other noncompetitive mGlu1 antagonists .
Phthalaldehyde (Phthaldialdehyde) reacts with proteins containing primary amines and blocked amino-terminal peptides of amino acids. Phthalaldehyde stabilizes bacterial outer membranes and cell walls, increases the optical density of bacterial cell suspensions, and inhibits bacterial lysis induced by ethylenediaminetetraacetic acid and sodium dodecyl sulfate. Phthalaldehyde exhibits bactericidal activity against Gram-negative vegetative bacteria .
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .
MEDICA16 is an orally active acetyl-CoA carboxylase and ATP-citrate lyase inhibitor. MEDICA16 limits the acetyl-CoA supply for acetyl-CoA carboxylase, inhibits acetyl-CoA carboxylase activity, exerts citrate-competitive inhibitory effects on ATP-citrate lyase, and reduces hepatic AMPK activity. MEDICA16 can be used in research related to insulin resistance, hyperlipidemia, and obesity .
Succinyl CoA (Succinyl-coenzyme A) is a pivotal intermediate metabolite in the tricarboxylic acid cycle and a key coenzyme A metabolite. Succinyl CoA is biosynthesized from α-ketoglutarate or propionyl-CoA. Succinyl CoA acts as a critical precursor and substrate for heme biosynthesis and gluconeogenesis. Succinyl CoA insufficiency caused by cobalamin deficiency is directly linked to growth retardation, impaired heme synthesis, tissue glycine accumulation and neurological abnormalities. Succinyl CoA can be used in research on metabolic, neurological, and hematological abnormalities (such as porphyria) caused by nutritional vitamin B12 deficiency (leading to a lack of Succinyl-Coenzyme A synthesis) .
Flutolanil is a succinate dehydrogenase complex inhibitor and fungicide. Flutolanil blocks electron transfer between the redox center of succinate dehydrogenase and coenzyme Q, inhibits mycelial oxygen consumption, and suppresses mycelial growth. Flutolanil induces acute and sublethal toxicity in zebrafish at different life stages. Flutolanil can be used in studies on plant disease control .
1-Acetamidonaphthalene (N-(Naphthalen-1-yl)acetamide) is a degradation product of Digitoxigenin (HY-B2151). 1-Acetamidonaphthalene is weakly mutagenic to Salmonella typhimurium TA98 with metabolic activation. 1-Acetamidonaphthalene can be used for the research of bacterial infection .
FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a Ki od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R.FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC50 values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders .
Carboxyatractyloside (CATR) is a tight-binding inhibitor of adenine nucleotide translocase, and represents the major toxic component of Xanthium sibiricum. Carboxyatractyloside competes with ADP for binding to the translocase, blocks the translocation of ADP/ATP across the inner mitochondrial membrane, and thereby inhibits ADP-stimulated respiration. In the presence of Cyclosporin A (HY-B0579), Carboxyatractyloside still induces permeability transition in liver mitochondria of aged rats, exhibiting significant hepatotoxicity and nephrotoxicity. Carboxyatractyloside is widely used in studies related to hepatotoxicity, nephrotoxicity and Alzheimer's disease .
FXIa/Plasma kallikrein-IN-1 is an inhibitor of coagulation factor XIa (FXIa) and plasma kallikrein with Ki values of 187.70 nM and 151.6 nM, respectively. FXIa/Plasma kallikrein-IN-1 can be used in the research of thromboembolic diseases .
LE-540 is a selective retinoic acid receptor antagonist for RARβ (Ki=0.22 μM). LE-540 shows potential for use in cancer research, particularly for breast cancer and lung cancer .
S1P1 agonist III is an orally active hS1P1 agonist with an EC50 value of 18 nM. S1P1 agonist III shows limited activity against hS1P3. S1P1 agonist III can be used in the research of multiple sclerosis .
iNOs-IN-9 (Compound 10) is a selective inducible nitric oxide synthase (iNOS) inhibitor with an IC50 of 82 nM against hiNOS. iNOs-IN-9 reduces cytokine-induced inflammatory responses and cell necrosis in inflammatory cell models. iNOs-IN-9 can be used for research related to psoriasis .
Zenagamtide (Amycretin; NN 9487) sodium is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide sodium is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide sodium improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide sodium may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases .
PF-07202954 is an orally active, highly selective DGAT2 inhibitor with an IC50 of 10 nM against human DGAT2 and an IC50 of 17 nM against rat DGAT2. PF-07202954 reduces triglyceride synthesis, decreases hepatic triglyceride content and plasma triglyceride levels, inhibits de novo lipogenesis, and suppresses the hepatic SREBP signaling pathway as well as the expression of SREBP target genes. PF-07202954 is applicable to research related to non-alcoholic steatohepatitis .
PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease .
Linoleyl carnitine is an acylcarnitine and metabolite. Linoleyl carnitine in the liver is negatively correlated with pantothenic acid and citric acid in serum. Linoleyl carnitine accumulates in mitochondrial CPT II deficiency .
PTHR1 antagonist 1 (Compound 18) is a PTHR1 antagonist with an IC50 of 0.090 µM. PTHR1 antagonist 1 is applicable to the research of calcium metabolism disorders .
Sandoz 58-035 is a selective acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. Sandoz 58-035 inhibits this enzyme in intact cells and isolated microsomal fractions. Sandoz 58-035 blocks the esterification of exogenous vesicle-derived cholesterol and the incorporation of oleic acid into cellular cholesterol esters, reducing the formation and accumulation of cholesterol esters. Sandoz 58-035 causes a slight increase in cellular free cholesterol, and at high concentrations, it also causes a slight reduction in overall cellular protein synthesis. Sandoz 58-035 can be used in studies related to cellular cholesterol regulation .
SHK1112218 is an orally active mitochondrial proton carrier with an EC50 of 0.48 μM. SHK1112218 restores proton transport and increases oxygen consumption rate. SHK1112218 can be used for the research of diabetes, obesity, and metabolic dysfunction-associated steatotic liver disease .
Alclofenac (Allopydin) is an orally active prostaglandin synthase inhibitor with anti-inflammatory, analgesic and antipyretic activities. Alclofenac irreversibly inhibits platelet aggregation. Alclofenac can be used in research related to rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, low back pain and sciatica .
Triallate is a selective thiocarbamate herbicide. Triallate regulates the biosynthesis of very-long-chain fatty acids and inhibits the elongation and division of plant cells. Triallate is used to control wild oats in barley, spring wheat, durum wheat, winter wheat and sugar beets .
Ophthalmic acid is a ubiquitous metabolite and glutathione modulator, with a Ki of 0.95 mM for glyoxalase I. Ophthalmic acid competitively inhibits glyoxalase I, glutathione S-transferase, glutaredoxin, glutamate-cysteine ligase, protein disulfide reductase (glutathione), as well as non-selective cation channels. Ophthalmic acid is applicable in diabetes-related research .
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca 2+ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy .
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
Buloxibutid (AT2 receptor agonist C21) is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis .
Dopamine D3 receptor agonist-2 is a selective dopamineD3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamineD2 receptor (Ki= 7.67nM) .
GD3 Ganglioside is an Apoptosis inducer and a biomarker for mouse neural stem cells. GD3 Ganglioside expresses in neural stem cells and the subventricular zone of the adult mouse brain. GD3 Ganglioside targets the mitochondrial permeability transition pore complex, induces pore opening, dissipates mitochondrial transmembrane potential, triggers Mitochondrial swelling, releases pro-apoptotic factors, and activates Caspase-9. GD3 Ganglioside is applicable to research related to glioblastoma .
Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache .
S-Acetonyl-CoA (Acetonyl-coenzyme A) is a non-reactive structural analog of acetyl-CoA that acts as a competitive inhibitor against multiple target enzymes. S-Acetonyl-CoA lacks the characteristic thioester group of acetyl-CoA, retaining only a thioether structure. S-Acetonyl-CoA competes with acetyl-CoA for binding to citrate synthase, phosphate transacetylase, carnitine acetyltransferase, and N-myristoyltransferase 1. S-Acetonyl-CoA serves as a reagent for investigating acetyl-CoA-dependent physiological processes .
Sulisobenzone (Benzophenone-4) is a benzophenone-type UV filter. Sulisobenzone can act as a endocrine disrupting compound. Sulisobenzone disrupts energy metabolism, nucleotide synthesis, oxidative stress response, and endocrine function. Sulisobenzone thyroid hormone biosynthesis and induces oxidative stress .
BODIPY FL-C16 is a BODIPY-labeled analog of Palmitic acid (HY-N0830), which serves as a fluorescent lipid tracer. BODIPY FL-C16 also acts as a ligand for liver fatty acid-binding protein (L-FABP) and intestinal fatty acid-binding protein (I-FABP) , with Kd values of 270 nM and 330 nM, respectively. BODIPY FL-C16 is rapidly taken up by cells, and after metabolic conversion to phospholipids, it is incorporated into the membrane structures of intracellular organelles and extracellular vesicles .
DHPDS disodium salt is a pH-sensitive fluorescent dye. DHPDS disodium salt is used to measure intracellular pH (pHi) from the surface fluorescence of the isolated perfused ratliver .
PiF is a fluorescent probe with high specificity for pancreatic β-cells (Ex/Em = 535 nm/565 nm), and its fluorescence signal increases significantly with elevated insulin concentrations in in vitro experiments. PiF enables visualization of rat and human islets transplanted via the portal vein in mouse livers with low liver background signals. The fluorine atom of PiF can be replaced by radioactive 18F to prepare a PET tracer. PiF can be used for research on type 1 diabetes .
Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca 2+ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy .
Phthalaldehyde (Phthaldialdehyde) reacts with proteins containing primary amines and blocked amino-terminal peptides of amino acids. Phthalaldehyde stabilizes bacterial outer membranes and cell walls, increases the optical density of bacterial cell suspensions, and inhibits bacterial lysis induced by ethylenediaminetetraacetic acid and sodium dodecyl sulfate. Phthalaldehyde exhibits bactericidal activity against Gram-negative vegetative bacteria .
C22-Ceramide (d18:1/22:0) (Cer d18:1/22:0) is an endogenous bioactive sphingolipid. C22-Ceramide (d18:1/22:0) reduces the propensity of C16-ceramide channel formation in isolated ratliver mitochondria and in liposomes .
Testosterone/BSA, a conjugate of Testosterone (HY-113415) and bovine serum albumin (BSA), acts as a nuclear transporter and cytoplasmic accumulator. Testosterone/BSA can enter the nuclei of rat testicular spermatocytes, spermatids and ratliver endothelial cells, while the antigenicity of BSA remains intact. Testosterone/BSA accumulates in the cytoplasm of rat hepatocytes in granular form. Testosterone/BSA can be used to investigate the membrane-initiated or non-genomic activities of steroid hormones .
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
Oxalic acid (Ethanedioic acid) diammonium monohydrate is a dicarboxylic acid found in a wide variety of plants. Oxalic acid diammonium monohydrate shows antioxidant acyivity and suppresses lipid peroxidation. Oxalic acid diammonium monohydrate is a pathogenicity factor for sclerotinia sclerotiorum, and suppresses the oxidative burst of the host plant. Oxalic acid diammonium monohydrate exerts acaricidal activity. Oxalic acid can be used for the researches of sclerotinia disease varroatosis and inflammatory diseases .
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in ratliver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation .
Zenagamtide (Amycretin; NN 9487) sodium is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide sodium is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide sodium improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide sodium may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases .
Hepcidin-25 (human) is an iron metabolism regulator and Antimicrobial agent. Hepcidin-25 (human) exerts anti-inflammatory and antimicrobial activities by regulating iron-mediated oxidative damage .
2-(Methylamino)benzoic acid is the main metabolite of methyl-N-methylanthranilates (MMA) (HY-76705) and is the compound in which the ester group is converted. MMA can be isolated from citrus fruits and has potential analgesic activity. 2-(Methylamino)benzoic acid was used to detect the metabolic levels of MMA in ratliver .
2-(Methylamino)benzoic acid (Standard) is the analytical standard of 2-(Methylamino)benzoic acid. This product is intended for research and analytical applications. 2-(Methylamino)benzoic acid is the main metabolite of methyl-N-methylanthranilates (MMA) (HY-76705) and is the compound in which the ester group is converted. MMA can be isolated from citrus fruits and has potential analgesic activity. 2-(Methylamino)benzoic acid was used to detect the metabolic levels of MMA in ratliver[1].
Anti-Mouse CD8α Antibody (2.43) is an anti-mouse CD8α IgG2b monoclonal antibody. Anti-Mouse CD8α Antibody (2.43) can significantly deplete CD8 + T cells. Anti-Mouse CD8α Antibody (2.43) can prolong the survival time of liver cell transplantation. Anti-Mouse CD8α Antibody (2.43) can be used for research on immunology. The recommend isotype control of Anti-Mouse CD8α Antibody (2.43): Rat IgG2b kappa, Isotype Control (HY-P990682) .
Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
Oxalic acid, 99% (Ethanedioic acid) is a dicarboxylic acid found in a wide variety of plants. Oxalic acid, 99% shows antioxidant acyivity and suppresses lipid peroxidation. Oxalic acid, 99% is a pathogenicity factor for sclerotinia sclerotiorum, and suppresses the oxidative burst of the host plant. Oxalic acid, 99% exerts acaricidal activity. Oxalic acid can be used for the researches of sclerotinia disease, varroatosis and inflammatory diseases .
Allocholic acid is a typically fetal bile acid found in vertebrates and reappears during liver regeneration and carcinogenesis, besides it is also a conjugate acid of allocholate and an isomer of cholic acid. Allocholic acid is a potent and specific stimulant of the adult olfactory system, it has a role as a marine metabolite, a rat metabolite and a human metabolite .
Tetrahydrocorticosterone is a glucocorticoid. One of its active forms, 5α-Tetrahydrocorticosterone (HY-113364), exerts its effects by binding to the GC receptor and inhibiting inflammatory processes. Tetrahydrocorticosterone is naturally synthesized by the adrenal glands and plays a key role in regulating the metabolism of carbohydrates, proteins and fats .
Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms .
Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome .
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for ratliver microsomal ACAT activity .
Prunasin is an orally active cyanogenic glucoside and the main metabolite of Amygdalin (HY-N0190). Prunasin can specifically inhibit ratDNA polymerase β (IC50: 98 μM). Prunasin has anti-inflammatory and anti-fibrotic activities. Prunasin can be used in the research of diseases such as liver fibrosis .
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated ratliver mitochondria .
Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced ratliver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis .
Ophthalmic acid is a ubiquitous metabolite and glutathione modulator, with a Ki of 0.95 mM for glyoxalase I. Ophthalmic acid competitively inhibits glyoxalase I, glutathione S-transferase, glutaredoxin, glutamate-cysteine ligase, protein disulfide reductase (glutathione), as well as non-selective cation channels. Ophthalmic acid is applicable in diabetes-related research .
2-Phenylpropionic acid is an intermediate in the metabolism of alpha-Methylstyrene. 2-Phenylpropionic acid covalently binds to ratliver protein. 2-Phenylpropionic acid can be used in the research of nonsteroidal anti-inflammatory agents .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
Neomangiferin is an orally active natural flavonoid. Neomangiferin partially ameliorates non-alcoholic fatty liver disease (NAFLD) by regulating the expression of genes related to free fatty acid uptake and lipid oxidation. Neomangiferin exerts anti-colitis effects by inhibiting Th17/Treg cell differentiation. Neomangiferin exerts anti-aging and lifespan-extending effects by targeting upregulation of bas-1, which in turn activates the autophagy, IIS and MAPK pathways. Neomangiferin has the potential to prevent aseptic loosening of prostheses after total joint arthroplasty due to its significant anti-inflammatory and osteoclastogenesis-inhibiting effects .
Chloramphenicol succinate sodium is a prodrug of Chloramphenicol (HY-B0239), acting as a P2Y14R inhibitor with an IC50 of 1.585 nM. Chloramphenicol succinate sodium serves as a competitive substrate and inhibitor of succinate dehydrogenase (SDH), which may account for its toxicity. Chloramphenicol succinate sodium exerts a significant inhibitory effect on colitis. Chloramphenicol succinate sodium can be used in research related to myelosuppression, gray baby syndrome, aplastic anemia, bacterial meningitis and inflammatory bowel disease .
Linoleyl carnitine is an acylcarnitine and metabolite. Linoleyl carnitine in the liver is negatively correlated with pantothenic acid and citric acid in serum. Linoleyl carnitine accumulates in mitochondrial CPT II deficiency .
Mauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049) .
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
Ochnaflavone is an inhibitor of IIA-type secretory phospholipase A2 (sPLA2-IIA) with an IC50 of 3.45 µM. Ochnaflavone exhibits significant anti-inflammatory and liver-protective effects, capable of inhibiting the degradation of phosphatidylethanolamine (PE) and lipid peroxidation induced by carbon tetrachloride (CCl4) in ratliver, with an IC50 of 7.16 µM for lipid peroxidation. Ochnaflavone can be used in research on liver damage and inflammatory diseases .
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using ratliver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
Bilirubin diglucuronide is a bilirubin glycoside conjugate with a 1-O-acyl β-D-glucuronide structure. Bilirubin diglucuronide is the major conjugated bilirubin (HY-N0323) and predominant pigment excreted in the bile of adult humans, rats, dogs and cats. Bilirubin diglucuronide is mainly synthesized via UDP-glucuronosyltransferase-mediated transfer of glucuronic acid from UDP-glucuronic acid to bilirubin monoglucuronide, or via enzymatic disproportionation of two moles of bilirubin monoglucuronide (predominantly producing the IXα configuration). In addition, Bilirubin diglucuronide can also be synthesized from bilirubin or its monoglucuronide in a UDP-glucuronic acid-dependent manner. Pretreatment with phenobarbital significantly enhances the formation process of Bilirubin diglucuronide .
Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and ratliver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes .
3-Pyridineacetic acid is an orally active nicotinic acid analog. 3-Pyridineacetic acid enhances cholesterol oxidation in ratliver mitochondria. 3-Pyridineacetic acid inhibits Triton-induced hypercholesterolemia in rats. 3-Pyridineacetic acid can be used in research related to hypercholesterolemia .
Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using ratliver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
Chitobiose is an orally active chitosan oligosaccharide (degree of polymerization 2). Chitobiose shows hepatoprotective activity and counteracts CCl4-induced elevation of plasma aspartate transaminase and alanine transaminase activities in rats. Chitobiose can be used for the research of carbon tetrachloride-induced acute hepatotoxicity .
Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies .
Succinyl CoA (Succinyl-coenzyme A) is a pivotal intermediate metabolite in the tricarboxylic acid cycle and a key coenzyme A metabolite. Succinyl CoA is biosynthesized from α-ketoglutarate or propionyl-CoA. Succinyl CoA acts as a critical precursor and substrate for heme biosynthesis and gluconeogenesis. Succinyl CoA insufficiency caused by cobalamin deficiency is directly linked to growth retardation, impaired heme synthesis, tissue glycine accumulation and neurological abnormalities. Succinyl CoA can be used in research on metabolic, neurological, and hematological abnormalities (such as porphyria) caused by nutritional vitamin B12 deficiency (leading to a lack of Succinyl-Coenzyme A synthesis) .
Methyl propyl disulfide is an orally administrable volatile sulfide present in onions. Methyl propyl disulfide reduces the activity of spermine N'1-acetyltransferase (SAT), inhibits cell proliferation, and decreases the induction of placental glutathione S-transferase (GST-P)-positive hepatocyte foci in ratlivers. Methyl propyl disulfide can be used in studies related to the mechanism of hepatocarcinogenesis .
6"-O-Acetylgenistin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetylgenistin significantly inhibits lipid peroxidation in ratliver microsome with an IC50 of 10.6 μM .
6"-O-Acetyldaidzin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetyldaidzin significantly inhibits lipid peroxidation in ratliver microsome with an IC50 of 8.2 μM .
2-(Methylamino)benzoic acid is the main metabolite of methyl-N-methylanthranilates (MMA) (HY-76705) and is the compound in which the ester group is converted. MMA can be isolated from citrus fruits and has potential analgesic activity. 2-(Methylamino)benzoic acid was used to detect the metabolic levels of MMA in ratliver .
Dehydromonocrotaline is a mitochondrial respiratory chain complex I NADH oxidase inhibitor, with a IC50 of 62.06 μM and a Ki of 8.1 μM in rats. Dehydromonocrotaline exerts non-competitive inhibitory effects by modifying cysteine thiol groups on complex I, and does not bind to the NADH-binding site. Dehydromonocrotaline dissipates mitochondrial membrane potential and reduces ATP levels. Dehydromonocrotaline can be used in studies related to hepatotoxicity, pulmonary hypertension and liver tumors .
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in ratliver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
9-Oxononanoic acid (9-ONA) is an orally active acetyl-CoA carboxylase inhibitor. 9-Oxononanoic acid inhibits acetyl-CoA carboxylase via accumulation of long-chain acyl-CoA. 9-Oxononanoic acid increases carnitine palmitoyltransferase, isocitrate dehydrogenase and glucose 6-phosphate dehydrogenase activity to elevate β-oxidation and support NADPH (HY-113324) supplyactivity. 9-Oxononanoic acid stimulates phospholipase A2 activity via post-translational, non-transcriptional mechanisms. 9-Oxononanoic acid can be used for the research of atherothrombosis .
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using ratliver microsomes .
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin II inhibits cell-free protein synthesis, releases adenine from ratliver ribosomes and from DNA, and has no RNase activity .
Diallyl tetrasulfide is an orally active diallyl tetrasulfide. Diallyl tetrasulfide ameliorates cadmium-induced changes in acetylcholinesterase and adenosine triphosphatase activities as well as oxidative stress injury in the brain of rats . Diallyl tetrasulfide inhibits lipid peroxidation in ratliver microsomes . Diallyl tetrasulfide ameliorates cadmium-induced oxidative liver injury in rats . Diallyl tetrasulfide protects cells against cadmium-induced loss of cell viability, reduces apoptosis rate and ROS production. Diallyl tetrasulfide is applicable to research related to cadmium-induced neurotoxicity and cadmium-induced oxidative liver injury .
Filiformin ((-)-Filiformin) is a sesquiterpene compound that can be isolated from Laurencia filiformis forma heteroclada. Filiformin exhibits certain cytotoxicity against P388 and BSC-1 cells. Filiformin has antimicrobial activity against Bacillus subtilis, Trichophyton mentagrophytes and Candida albicans. In addition, Filiformin can inhibit oxygen uptake in isolated ratliver mitochondria at a concentration of 150 μM .
Riddelline, a pyrrolizidine alkaloid, is a potent genotoxic agent. Riddelline induces significant elevations in unscheduled DNA synthesis and S-phase synthesis in ratliver .
Glomeratide A is a benzophenone C-glucoside with hepatoprotective effects. Glomeratide A has a protective effect against d-galactosamine-induced hepatotoxicity in ratliver epithelial stem-like cells.
Phorone (Diisopropylidene acetone) is a glutathione (GSH) depletor. Phorone specifically and reversibly depletes free GSH through enzymatic binding (Glutathione S-transferase) (Km = 0.9 mM). Phorone reversibly reduces the binding and nuclear uptake of glucocorticoid receptors in ratliver, and this effect is related to the temporal changes in GSH levels. Phorone can be used for studying liver toxicity.
Goodyeroside A is a glycoside compound derived from the plant Goodyera that exhibits significant hepatoprotective activity. It can inhibit liver damage induced by carbon tetrachloride (HY-Y0298) in primary cultured rat hepatocytes .
Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in ratliver microsomes free from vitamin E .
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in ratliver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation .
Helminthosporol is a natural plant growth-regulator that can promote the growth of rice and lettuce seedlings. Helminthosporol can also inhibit the activity of acyl-CoA: cholesterol acyltransferase (ACAT) in ratliver microsomes and the synthesis of cholesterol esters in macrophages .
L-Octanoylcarnitine (Standard) is the analytical standard of L-Octanoylcarnitine. This product is intended for research and analytical applications. L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
Gypsetin can inhibit acylcoenzyme A, cholesterol acyltransferase (ACAT) activity, inhibit ratliver microbody ACAT with an IC50 of 18 μM, and its action is competitive with oleoyl-COA substrate, Ki value is 5.5 μM. Gypsetin also inhibits Oleic acid from forming cholesterol esters with an IC50 of 0.65 μM .
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in ratliver microsomes .
2-Phenylpropionic acid (Standard) is the analytical standard of 2-Phenylpropionic acid (HY-W015608). This product is intended for research and analytical applications. 2-Phenylpropionic acid is an intermediate in the metabolism of alpha-Methylstyrene. 2-Phenylpropionic acid covalently binds to ratliver protein. 2-Phenylpropionic acid can be used in the research of nonsteroidal anti-inflammatory agents .
Cyclamidomycin (Desdanine) is an acrylamide antibiotic with antibacterial activity. Cyclamidomycin inhibits nucleoside diphosphate kinase and pyruvate kinase (in E. coli) and oxidative phosphorylation in ratliver mitochondria. Cyclamidomycin is active against S. aureus, M. flavus, S. lutea, B. subtilis, E. coli, S. flexneri, S. typhosa, P. vulgaris, and K. pneumoniae (MICs=3.12-25 mg/ml) .
Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
Hydroxysaikosaponin D is a hepatocytoprotective saponin found in the roots of Bupleurum scorzonerifolium WILLD. Hydroxysaikosaponin D inhibits D-galactosamine-induced cytotoxicity in primary cultured rat hepatocytes. Hydroxysaikosaponin D mitigates D-galactosamine/LPS-induced liver injury in mice. Hydroxysaikosaponin D can be used for the research of liver injury .
Mimosinamine is a hydroxylase inhibitor with Fe2+ chelating activity. Mimosinamine inhibits bovine adrenal tyrosine hydroxylase, ratliver phenylalanine hydroxylase, and rat brainstem tryptophan hydroxylase. Mimosinamine can be used in the research of hypertension .
Enzyme-IN-4 is a competitive inhibitor of glyoxalase I that can be found in Stereum hirsutum. Enzyme-IN-4 has a Ki value of 4.6 μM against ratliver glyoxalase I .
Antihepatotoxic agent-1 is a cerebroside present in Lycium chinense Fruits with antihepatotoxic activity. Antihepatotoxic agent-1 exerts a protective effect by blocking the release of alanine aminotransferase and sorbitol dehydrogenase from primary cultured rat hepatocytes intoxicated with carbon tetrachloride. Antihepatotoxic agent-1 can be used in studies related to liver injury .
(E/Z)-3-Hydroxylicochalcone A (Compound 1) is a flavonoid found in licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis), with antioxidant and anti-inflammatory activity. (E/Z)-3-Hydroxylicochalcone A inhibits lipid peroxidation in ratliver microsomes. (E/Z)-3-Hydroxylicochalcone A inhibits LPS (HY-D1056)-induced ROS, NO, IL-6, and PGE2 production .
Zoxamide metabolite 1 (Compound M1) is a monodechlorinated Zoxamide (HY-120921) metabolite. Zoxamide metabolite 1 undergoes dechlorination most plausibly at the reactive α-chloro ketone position .
Plantagoside A (Compound 3) is a phenylethanoid glycoside found in Plantago asiatica. Plantagoside A has antioxidant activity and can inhibit lipid peroxidation in ratliver microsomes induced by ADP and NADPH with an IC50 of 0.54 μM .
2-(Methylamino)benzoic acid (Standard) is the analytical standard of 2-(Methylamino)benzoic acid. This product is intended for research and analytical applications. 2-(Methylamino)benzoic acid is the main metabolite of methyl-N-methylanthranilates (MMA) (HY-76705) and is the compound in which the ester group is converted. MMA can be isolated from citrus fruits and has potential analgesic activity. 2-(Methylamino)benzoic acid was used to detect the metabolic levels of MMA in ratliver[1].
L-Octanoylcarnitine (hydrochloride) (Standard) is the analytical standard of L-Octanoylcarnitine (hydrochloride) (HY-W354498). This product is intended for research and analytical applications. L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
3-Pyridineacetic acid (Standard) is an analytical standard for 3-Pyridineacetic acid (HY-W015806). This product is for research and analytical applications. 3-Pyridineacetic acid is an orally active nicotinic acid analog. 3-Pyridineacetic acid enhances cholesterol oxidation in ratliver mitochondria. 3-Pyridineacetic acid inhibits Triton-induced hypercholesterolemia in rats. 3-Pyridineacetic acid can be used in research related to hypercholesterolemia.
4'-Hydroxychalcone (Standard) is the analytical standard of 4'-Hydroxychalcone (HY-N7056). This product is intended for research and analytical applications. 4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated ratliver mitochondria .
17-Hydroxystearic acid isolable from Torulopsis magnoliae fermentation oil. 17-Hydroxystearic acid is a saturated C18 ω2-hydroxy fatty acid existing in D- and L-enantiomeric forms .
Fraxinuacidoside functions as a norditerpene glucopyranoside with a unique carbon skeleton. Fraxinuacidoside can be found in the stem bark of Fraxinus sieboldiana .
(rac)-5-Hydroxykynurenine is a urinary metabolite. (rac)-5-Hydroxykynurenine is generated via indole ring oxidative cleavage of 5-hydroxytryptophan (HY-N0122) catalyzed by indoleamine 2,3-dioxygenase .
The GFER protein is a FAD-dependent sulfhydryl oxidase that restores redox-active disulfide bonds in CHCHD4/MIA40, an important partner for protein folding in the mitochondrial intermembrane space.GFER Protein, Rat (His-SUMO) is the recombinant rat-derived GFER protein, expressed by E.coli , with N-His, N-SUMO labeled tag.
The PKLR protein is a pyruvate kinase that plays a critical role in glycolysis, converting phosphoenolpyruvate to pyruvate and producing ATP.As a key enzyme, PKLR mediates the final steps of glycolysis, contributing to energy production.PKLR Protein, Rat (P.pastoris, His) is the recombinant rat-derived PKLR protein, expressed by P.pastoris , with N-6*His labeled tag.
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
2,3-Oxidosqualene-d6 (Squalene oxide-d6) is a deuterium labeled 2,3-Oxidosqualene (HY-114296). 2,3-Oxidosqualene (Squalene oxide) is a sterol biosynthesis precursor intermediate.2,3-Oxidosqualene participates in cyclization pathways that form sterols and triterpenes, and contributes to introduction of their characteristic 3-hydroxyl group.2,3-Oxidosqualene forms metabolically from squalene in ratliver homogenates under sterol synthesis conditions.2,3-Oxidosqualene converts to sterols including cholesterol, lathosterol, and lanost-8-en-3β-ol in ratliver homogenates under anaerobic conditions.
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated ratliver microsomes.
Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis .
Perhexiline-d11 (maleate) is the deuterium labeled Perhexiline maleate. Perhexiline maleate is a potent carnitine palmitoyltransferase 1 (CPT 1) inhibitor with IC50s of 77 and 148 μM for rat heart and liver CPT 1, respectively.
Pyridaben-d13 is the deuterium labeled Pyridaben . Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: ratliver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function .
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer .
Propiconazole-d3 (nitrate) is the deuterium labeled Propiconazole nitrate. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not ratliver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not ratliver, microsomal cytochrome P450 (IC50s=0.04 and >200 μM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 μg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS) .
Enniatin A- 13C36 is the 13C-labeled Enniatin A (HY-N6702). Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using ratliver microsomes .
Enniatin B- 13C33 is the 13C-labeled Enniatin B (HY-N3806). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using ratliver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
Enniatin A1- 13C35 is the 13C-labeled Enniatin A1 (HY-N6704). Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in ratliver microsomes .
Enniatin B1- 13C34 is the 13C-labeled Enniatin B1 (HY-N3807). Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using ratliver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
Azidocillin, a semi-synthetic Penicillin, is an orally active β-lactam antibiotic. Azidocillin bears an azide functionality and retains on-target activity within bacteria. Azidocillin can be used to research osteitis caused by dental surgery, otitis media, enterococcal septicemia and other bacterial infectious diseases . Azidocillin is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in ratliver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
Imiprothrin is an inducer that induces CYP1A2 and metallothionein 1a, with significant genotoxicity and cytotoxicity. In rat hepatocytes, Imiprothrin initiates detoxification responses by triggering the overexpression of these two genes. Imiprothrin induces chromosomal aberrations and micronucleus formation in rat bone marrow cells, and causes DNA damage in hepatocytes. Imiprothrin triggers oxidative stress in rats, leading to lipid peroxidation, excessive reactive oxygen species production and redox imbalance, which in turn impairs liver and kidney functions and causes tissue damage. Imiprothrin inhibits weight gain in mice, and even causes high mortality in female mice at high doses. However, it shows no carcinogenicity in rat experiments; among relevant indicators, aspartate aminotransferase and total protein are identified as sensitive toxicity biomarkers .
Thymine, one of the four bases of DNA, is a substrate for ratliver dihydropyrimidine dehydrogenase (DPD), with a Km value of 2.2 μM, Ki of 24 μM (using 5-FU as the DPD substrate), and a specific activity of 0.68 nmol/min/mg .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
Rat IL-10 mRNA encodes interleukin-10 (IL-10). IL-10 is expressed in tissues/cells such as hepatic stellate cells and is involved in physiological processes including liver fibrosis.
2'-Deoxy-N-methyl-AMP ammonium is an N6-substituted adenine nucleotide derivative and a glycosyl donor. On one hand, 2'-Deoxy-N-methyl-AMP ammonium acts as a specific substrate for N6-methyl-AMP aminohydrolase, and it is catalytically converted to dIMP to participate in the nucleotide metabolic cycle. On the other hand, 2'-Deoxy-N-methyl-AMP ammonium also serves as a guanosine diphosphate (GDP)-linked fucose derivative donor, driving site-specific glycoconjugation of proteins under the mediation of α-1,3-fucosyltransferase. 2'-Deoxy-N-methyl-AMP ammonium is an important molecular tool for investigating the mechanisms of nucleotide modification and protein glycosylation .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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