Search Result
Results for "
rat liver microsome
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-10864
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URB-597
5 Publications Verification
KDS-4103
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FAAH
Autophagy
Mitophagy
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Neurological Disease
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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 .
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- HY-Y0262
-
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Ethanedioic acid
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Environmental Pollutants
Endogenous Metabolite
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Infection
Inflammation/Immunology
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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 .
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- HY-150508
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MK-0159
1 Publications Verification
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CD38
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-B1311
-
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SKF-525A; U-5446; RP-5171
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Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
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Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-W010981
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Tributyl O-acetylcitrate; ATBC
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Environmental Pollutants
Biochemical Assay Reagents
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Others
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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 .
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- HY-100634
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(±)-4-hydroxy Propranolol hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
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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 .
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- HY-145628
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Sigma Receptor
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-124098
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Lidocaine N-oxide
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Drug Metabolite
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Others
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Lignocaine N-oxide (Lidocaine N-oxide) is a compound derived from the metabolism of lidocaine. Lidocaine can be metabolized to its N-oxide in rat liver microsomes.
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- HY-153508
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Chloride Channel
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Others
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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 rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
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- HY-117290
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Factor Xa
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Cardiovascular Disease
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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 .
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- HY-N3807
-
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Acyltransferase
ERK
NF-κB
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Infection
Cardiovascular Disease
Cancer
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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 rat liver 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 .
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- HY-N4031
-
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Anaplastic lymphoma kinase (ALK)
METTL3
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Inflammation/Immunology
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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 rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes .
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- HY-N3806
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Acyltransferase
ERK
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Infection
Cardiovascular Disease
Cancer
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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 rat liver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
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- HY-152118
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Cytochrome P450
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Cancer
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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 rat liver microsomes .
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- HY-128268
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Parasite
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Infection
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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 .
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- HY-N4071
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Others
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Others
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6"-O-Acetyldaidzin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetyldaidzin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 8.2 μM .
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- HY-N4070
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Others
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Others
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6"-O-Acetylgenistin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetylgenistin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 10.6 μM .
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- HY-151229
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DETC-Me; DDTC-Me; Diethyldithiocarbamic acid methyl ester
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Aldehyde Dehydrogenase (ALDH)
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Metabolic Disease
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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 rat liver 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.
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- HY-76667
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- HY-173084
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Phosphatase
MDM-2/p53
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Cancer
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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 rat liver microsomes .
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- HY-170788
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Phosphodiesterase (PDE)
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Metabolic Disease
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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 .
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Endogenous Metabolite
Progesterone Receptor
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Cancer
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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 rat liver 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 .
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- HY-W003371
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Drug Metabolite
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Others
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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 rat liver microsomes may be sex-specific .
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- HY-N8331
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- HY-169402A
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- HY-Y0262A
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Ethanedioic acid diammonium monohydrate
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Environmental Pollutants
Endogenous Metabolite
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Infection
Inflammation/Immunology
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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 .
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- HY-12835
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LPL Receptor
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Inflammation/Immunology
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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 .
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- HY-N6702
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- HY-129344
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Acyltransferase
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Metabolic Disease
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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 .
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- HY-130238
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(±)8-HDoHE; 8-hydroxy Docosahexaenoic acid; (±)8-HDoHE
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Endogenous Metabolite
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Metabolic Disease
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(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, 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.
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- HY-148868A
-
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Akt
CDK
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Cancer
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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 .
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- HY-130288
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(±)13-HDoHE; 13-hydroxy Docosahexaenoic acid; (±)13-HDoHE
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Lipoxygenase
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Inflammation/Immunology
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(±)13-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, 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.
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- HY-107534
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GnRH Receptor
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Endocrinology
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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 .
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- HY-150519
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Factor XI
Kallikrein
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Cardiovascular Disease
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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 .
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- HY-N9515
-
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Apoptosis
Reactive Oxygen Species (ROS)
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Neurological Disease
Metabolic Disease
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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 rat liver 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 .
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- HY-172147
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Somatostatin Receptor
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Neurological Disease
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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/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
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- HY-10864R
-
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KDS-4103 (Standard)
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FAAH
Autophagy
Mitophagy
Reference Standards
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Neurological Disease
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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 .
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- HY-146410
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Angiotensin Receptor
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Others
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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 .
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- HY-B0822S1
-
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GABA Receptor
Cytochrome P450
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Inflammation/Immunology
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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 rat liver microsomes.
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- HY-169332
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Piezo Channel
ERK
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Metabolic Disease
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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 .
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- HY-118048
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- HY-W741611
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-
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- HY-182255
-
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Endogenous Metabolite
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Others
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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, rat liver microsomes and human liver microsomes .
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- HY-175078
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19(20)-DHDP; (±)19,20-DiHDoPE
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Endogenous Metabolite
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Others
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(±)19(20)-DiHDPA is one of the major metabolites produces when docosahexaenoic acid is incubated with NADPH-supplemented rat liver microsomes .
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-
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- HY-B1311R
-
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SKF-525A (Standard); U-5446 (Standard); RP-5171 (Standard)
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Reference Standards
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
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Neurological Disease
Inflammation/Immunology
Cancer
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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] .
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- HY-16442
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Phosphatase
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Metabolic Disease
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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 rat liver microsomes. S-3483 specifically inhibits Glc-6-P transporter of renal and liver microsomes .
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- HY-N15411
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Acyltransferase
Phytohormone
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Metabolic Disease
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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 rat liver microsomes and the synthesis of cholesterol esters in macrophages .
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- HY-125568
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MMP
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Others
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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 rat liver microsomes free from vitamin E .
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- HY-130287
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(±)16-HDoHE; 16-hydroxy Docosahexaenoic acid; (±)16-HDoHE
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Endogenous Metabolite
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Metabolic Disease
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(±)16-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, 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.
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- HY-113777
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22-Hydroxy Docosahexaenoic acid; 22-OH DHA
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Cytochrome P450
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Metabolic Disease
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22-HDHA (22-Hydroxy Docosahexaenoic acid) is an oxidation product of docosahexaenoic acid. In vitro, it is formed upon incubation of rat liver 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.
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- HY-126182
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Endogenous Metabolite
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Cardiovascular Disease
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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 rat liver microsomes, showing efficient deacetylase activity. The study of deacetyldiltiazem helps to understand the differences in the metabolic kinetics of compounds between different species .
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- HY-171462
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- HY-157931
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Histamine Receptor
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Neurological Disease
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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 rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
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- HY-149481
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Dopamine Receptor
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Neurological Disease
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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 .
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- HY-N6704
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ERK
Apoptosis
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Cancer
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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 rat liver microsomes .
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- HY-40156A
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Bacterial
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Infection
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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 rat liver microsomes. Mycobacterium Tuberculosis-IN-5 exhibits anti-tuberculosis efficacy in mice .
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- HY-123639
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N-(2-Phenylethyl)-indomethacin amide
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COX
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Inflammation/Immunology
Cancer
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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 .
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- HY-169402
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- HY-173024
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TRP Channel
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Neurological Disease
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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% .
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- HY-155051
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Apoptosis
Histone Methyltransferase
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Cancer
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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 rat liver microsomes .
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-
- HY-162109
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-N12571A
-
-
- HY-182800
-
|
|
Molecular Glues
Casein Kinase
|
Cancer
|
|
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 rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia .
|
-
- HY-181710
-
|
|
mTOR
PI3K
|
Cancer
|
|
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 rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
|
-
- HY-W003371R
-
|
|
Drug Metabolite
Reference Standards
|
Others
|
|
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 rat liver microsomes may be sex-specific .
|
-
- HY-182771
-
-
- HY-N17823
-
|
|
Others
|
Inflammation/Immunology
|
|
Plantagoside A (Compound 3) is a phenylethanoid glycoside found in Plantago asiatica. Plantagoside A has antioxidant activity and can inhibit lipid peroxidation in rat liver microsomes induced by ADP and NADPH with an IC50 of 0.54 μM .
|
-
- HY-169258
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
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 rat liver microsomes .
|
-
- HY-N6702S
-
|
|
Isotope-Labeled Compounds
Acyltransferase
|
Infection
|
|
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 rat liver microsomes .
|
-
- HY-181721
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
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 rat liver microsomes. Dopamine D3 receptor agonist 1 can be used to study severe mental disorders comorbid with substance use disorders .
|
-
- HY-181884
-
|
|
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-W700354
-
|
|
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
(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 .
|
-
- HY-N3806S
-
|
|
Isotope-Labeled Compounds
Acyltransferase
ERK
|
Infection
|
|
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 rat liver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
|
-
- HY-182637
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
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.
|
-
- HY-181792
-
|
|
STAT
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-182021
-
|
|
Amine N-methyltransferase
|
Endocrinology
|
|
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 .
|
-
- HY-182358
-
|
|
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-174413
-
|
|
Adenosine Receptor
|
Cancer
|
|
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 rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.
|
-
- HY-182292
-
|
|
|
Infection
|
|
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 .
|
-
- HY-N6704S
-
|
|
Isotope-Labeled Compounds
ERK
Apoptosis
|
Cancer
|
|
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 rat liver microsomes .
|
-
- HY-124183
-
|
|
CXCR
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-182612
-
|
|
TGF-β Receptor
|
Cancer
|
|
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 .
|
-
- HY-183919
-
|
|
Acetyl-CoA Carboxylase
Cytochrome P450
|
Metabolic Disease
|
|
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 .
|
-
- HY-183709
-
|
|
Sodium Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-N3807S
-
|
|
Isotope-Labeled Compounds
Acyltransferase
ERK
NF-κB
|
Infection
|
|
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 rat liver 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 .
|
-
- HY-182385
-
|
|
Lipocalin Family
|
Metabolic Disease
|
|
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 .
|
-
- HY-W006081
-
|
|
UGT
|
Others
|
|
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 .
|
-
- HY-182350
-
|
|
DUBTACs
Deubiquitinase
|
Metabolic Disease
|
|
FXR DUBTAC IN-1 (compound D11) is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC IN-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 IN-1 can be used in the research of cholestatic liver injury .
|
-
- HY-W237019
-
|
|
Bacterial
|
Infection
|
|
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 .
|
-
- HY-112481
-
|
|
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-182697
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
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 .
|
-
- HY-182799
-
|
|
PROTACs
Molecular Glues
IKZF Family
|
Cancer
|
|
IBA-12 is a IKZF2 molecular 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 .
|
-
- HY-106587
-
|
Clorotepine
|
5-HT Receptor
Drug Derivative
|
Neurological Disease
|
|
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 .
|
-
- HY-122163
-
-
- HY-181636
-
|
|
Cannabinoid Receptor
|
Neurological 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 .
|
-
- HY-183267
-
|
|
Aminopeptidase
|
Cancer
|
|
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].
|
-
- HY-181049
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
- HY-181662
-
|
|
MAP3K
|
Neurological Disease
|
|
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 .
|
-
- HY-114891
-
|
|
mGluR
|
Neurological Disease
|
|
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 .
|
-
- HY-183749
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-183647
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-186200
-
|
|
PTHR
|
Metabolic Disease
|
|
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 .
|
-
- HY-181646
-
|
|
Phosphodiesterase (PDE)
TNF Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-W009706
-
|
Allopydin; W-7320
|
Prostaglandin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
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 .
|
-
- HY-N4267
-
|
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
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 .
|
-
- HY-183776
-
|
|
Dopamine Receptor
|
Others
|
|
Dopamine D3 receptor agonist-2 is a selective dopamine D3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamine D2 receptor (Ki= 7.67nM) .
|
-
- HY-112487
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
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 .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-Y0262A
-
|
Ethanedioic acid diammonium monohydrate
|
Biochemical Assay Reagents
|
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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-Y0262
-
-
-
- HY-N3807
-
-
-
- HY-N4031
-
-
-
- HY-N3806
-
-
-
- HY-N4071
-
-
-
- HY-N4070
-
-
-
- HY-B1341
-
|
Enidrel; SC-4642; NSC 15432
|
Structural Classification
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Endocrinology
Steroids
Source Classification
|
Endogenous Metabolite
Progesterone Receptor
|
|
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 rat liver 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 .
|
-
-
- HY-N8331
-
-
-
- HY-N4267
-
|
|
Cardiovascular Disease
Structural Classification
other families
Classification of Application Fields
Lignans
Phenylpropanoids
Plants
Disease Research Fields
Source Classification
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
|
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 .
|
-
-
- HY-N6702
-
-
-
- HY-N9515
-
|
|
Structural Classification
Natural Products
Allium sativum L.
Plants
Amaryllidaceae
Source Classification
|
Apoptosis
Reactive Oxygen Species (ROS)
|
|
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 rat liver 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 .
|
-
-
- HY-N15411
-
-
-
- HY-125568
-
-
-
- HY-N6704
-
-
-
- HY-N12571A
-
-
-
- HY-N17823
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0822S1
-
|
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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 rat liver microsomes.
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- HY-169332
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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 .
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- HY-N6702S
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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 rat liver microsomes .
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- HY-N3806S
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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 rat liver microsomes . Enniatins B decreases the activation of ERK (p44/p42) .
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- HY-N6704S
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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 rat liver microsomes .
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- HY-N3807S
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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 rat liver 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 .
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Alkynes
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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 rat liver 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 .
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