Search Result
Results for "
lipophilic activities
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B2239
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- HY-N0783
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- HY-13538
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CP-4126; CO-101; Gemcitabine 5'-elaidate
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Nucleoside Antimetabolite/Analog
Autophagy
Apoptosis
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Cancer
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Gemcitabine elaidate (CP-4126) is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity .
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- HY-13538A
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CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5'-elaidate hydrochloride
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Nucleoside Antimetabolite/Analog
Autophagy
Apoptosis
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Cancer
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Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity .
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- HY-146686
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Cholinesterase (ChE)
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Neurological Disease
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BuChE-IN-3 (Compound C4) is a potent inhibitor of BuChE with an IC50 of 8.3 nM. BuChE-IN-3 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity .
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- HY-146687
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Cholinesterase (ChE)
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Neurological Disease
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BuChE-IN-4 (Compound C6) is a potent inhibitor of BuChE with an IC50 of 7.7 nM. BuChE-IN-4 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity .
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- HY-163994
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KWD 2058 hydrochloride
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Others
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Others
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Ibuterol (KWD 2058) hydrochloride, a diester of Terbutaline (HY-B0802A), is an orally active, selective and effective β-stimulating agent with lipophilic activities. Ibuterol hydrochloride is also an orally active ocular hypotensive agent. Ibuterol hydrochloride relieves bronchial obstruction in asthma without causing circulatory effects. Ibuterol hydrochloride is proming for rasearch of intraocular hypertension, asthma and bronchitis .
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- HY-151942
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Parasite
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Infection
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Antitrypanosomal agent 10 is an antitrypanosomal agent that inhibits Trypanosoma cruzi with an IC50 of 0.28 μM .
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- HY-165634
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Calcium Channel
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Cardiovascular Disease
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(R)-Azelnidipine is a highly lipophilic Calcium Channel antagonist with high affinity for vascular walls and antihypertensive activity. (R)-Azelnidipine shows potential for use in cardiovascular disease research .
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- HY-143686
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Biochemical Assay Reagents
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Cancer
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ImmTher is a liposome-encapsulated lipophilic disaccharide tripeptide derivative of muramyl dipeptide. ImmTher can up-regulate specific monocyte cytokine genes and activate monocyte-mediated tumoricidal activity .
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- HY-N12201
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Antibiotic
Fungal
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Infection
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Funiculosin is a neutral lipophilic antibiotic that inhibits DNA and RNA viruses. Funiculosin also has antifungal activity. Funiculosin inhibits infections caused by pathogenic fungi in primary chicken embryo fibroblasts .
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- HY-16055
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AR-67; DB 67
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Topoisomerase
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Cancer
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Silatecan (AR-67; DB 67) is a Camptothecin (HY-16560) analogue with improved stability and lipophilicity. Silatecan is an inhibitor for topoisomerase I, that inhibits the DNA replication and transcription, and exhibits antitumor and radiosensitizing activities
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- HY-114983
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(S)-9-Allyl-10-Hydroxycamptothecin
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Topoisomerase
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Cancer
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Chimmitecan ((S)-9-Allyl-10-Hydroxycamptothecin), a novel 9-small-alkyl-substituted lipophilic Camptothecin (HY-16560), is a potent inhibitor of topoisomerase I. Chimmitecan exhibits anticancer activity .
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- HY-N0783R
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PPAR
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Eupatilin (Standard) is the analytical standard of Eupatilin. This product is intended for research and analytical applications. Eupatilin, a lipophilic flavonoid isolated from Artemisia argyi Lévl. et Van., is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
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- HY-108474
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AG 337
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Thymidylate Synthase
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Cancer
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Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
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- HY-B0567
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Potassium Channel
nAChR
Apoptosis
Bacterial
Parasite
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Infection
Cancer
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Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
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- HY-100768
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HTHQ
2 Publications Verification
1-O-hexyl-2,3,5-trimethylhydroquinone; HX-1171; BTT-105
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Reactive Oxygen Species
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Cancer
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HTHQ (1-O-hexyl-2,3,5-trimethylhydroquinone) is a potent lipophilic phenolic antioxidant. HTHQ has considerable anti-oxidative activity by directly reacting with reactive oxygen species (ROS) and scavenging ROS to form more stable free radicals .
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- HY-128775
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Others
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Cancer
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JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) proagent. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST .
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- HY-126839
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5-Dodecanoylaminofluorescein di-β-D-Galactopyranoside
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Fluorescent Dye
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Others
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C12FDG (5-Dodecanoylaminofluorescein di-β-D-Galactopyranoside) is a lipophilic green fluorescent substrate for β-galactosidase detection. C12-FDG is more sensitive than FDG (HY-101895) for beta-galactosidase activity determinations in animal cells .
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- HY-131844
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N6-Benzoyladenosine-5'-O-monophosphate
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Others
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Others
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6-Bnz-5'-AMP is a lipophilic analogue of adenosine-5'-O-monophosphate and a potential metabolite of N 6-Benzoyl-cAMP. 6-Bnz-5'-AMP exhibits some cytokinin activity in tobacco and soybean tissue culture assays .
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- HY-106546
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KC 9147
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Fungal
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Infection
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Tolciclate (KC 9147) is an antifungal agent with in vitro inhibitory activity against dermatophytes, effective at concentrations of 0.01-0.1 μg/mL. Tolciclate is colorless and soluble in well-tolerated excipients, and it is more lipophilic than Tolnaftate (HY-B0370). Tolciclate can be used in research related to antifungal infections .
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- HY-164728
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Others
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Neurological Disease
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Pregabalin diacid is an impurity of Pregabalin, a lipophilic GABA (γ-aminobutyric acid) analog with anxiolytic and anticonvulsant activity. Pregabalin may act on the α(2)β subunit of voltage-dependent calcium channels, which are widely distributed in the peripheral and central nervous systems. Pregabalin can effectively induce hypoalgesia and improve behavioral disorders .
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- HY-147734
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Others
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Cancer
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Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
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- HY-122462
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PNU-159548
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DNA/RNA Synthesis
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Cancer
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Ladirubicin (PNU-159548) is a derivative of Daunorubicin (HY-13062A). Ladirubicin exhibits DNA intercalation and DNA alkylating properties, inhibits DNA replication and transcription, causes DNA damage, and thereby exhibits antitumor efficacy. Ladirubicin exhibits the potential to penetrate the blood-brain barrier (BBB) for its high lipophilicity. Ladirubicin exhibits toxicity through suppression of bone marrow activity .
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- HY-B0567R
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Potassium Channel
nAChR
Apoptosis
Bacterial
Parasite
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Infection
Cancer
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Dequalinium (Chloride) (Standard) is the analytical standard of Dequalinium (Chloride). This product is intended for research and analytical applications. Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
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- HY-112053
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DPPH
Maximum Cited Publications
15 Publications Verification
2,2-Diphenyl-1-picrylhydrazyl
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Others
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Metabolic Disease
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DPPH (2,2-Diphenyl-1-picrylhydrazyl) is a stable free radical that can be used to measure the radical scavenging activity of antioxidants. The odd electron of nitrogen atom in DPPH is reduced by receiving a hydrogen atom from antioxidants to the corresponding hydrazine. DPPH method may be utilized in aqueous and nonpolar organic solvents and can be used to examine both hydrophilic and lipophilic antioxidants .
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- HY-119983
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DBC
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Others
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Cancer
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7H-Dibenzo[c,g]carbazole is an azaarene with high lipophilicity. 7H-Dibenzo[c,g]carbazole has carcinogenic activity and induce DNA adducts in fish, DNA adducts, mutations in diploid human fibroblasts and micronuclei in human blood lymphocytes. 7H-Dibenzo[c,g]carbazole is activated by cytochrome P450 enzymes resulting mainly in the generation of phenolic metabolites .
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- HY-17403
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CV-4093
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Calcium Channel
NF-κB
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Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection .
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- HY-112053R
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Others
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Metabolic Disease
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DPPH (Standard) is the analytical standard of DPPH. This product is intended for research and analytical applications. DPPH (2,2-Diphenyl-1-picrylhydrazyl) is a stable free radical that can be used to measure the radical scavenging activity of antioxidants. The odd electron of nitrogen atom in DPPH is reduced by receiving a hydrogen atom from antioxidants to the corresponding hydrazine. DPPH method may be utilized in aqueous and nonpolar organic solvents and can be used to examine both hydrophilic and lipophilic antioxidants .
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- HY-W099563
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Biochemical Assay Reagents
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Others
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4-Nitrophenyl stearate, which is an ester formed by the condensation of stearic acid and 4-nitrophenol, is commonly used as a substrate for enzymatic assays, where the hydrolysis of ester bonds by esterase and lipase can be measured by absorbance or ratio In addition, 4-Nitrophenyl stearate has been used as a model compound to study the enzymatic activity and selectivity of lipases and esterases from various sources. The long hydrophobic tail of the molecule makes it suitable for use in lipophilic Good solubility in the environment makes it a useful probe for studying lipid metabolism.
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- HY-N8572
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PARP
Reactive Oxygen Species
Aryl Hydrocarbon Receptor
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects .
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- HY-117204
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Antibiotic
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Infection
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AA-57 is an acidic lipophilic antibiotic isolated from the fermentation broth of Actinomycetes strain AA-57. The AA-57 strain was isolated from a soil sample collected in Koriyama City, Fukushima Prefecture, Japan. AA-57 has antibacterial properties against Gram-positive bacteria, Gram-negative bacteria, and acid-fast bacteria. AA-57 was discovered by screening actinomycete cultures for antibacterial properties. AA-57 exhibits significant antibacterial activity and has inhibitory effects against a variety of bacteria. The discovery of AA-57 provides new possibilities for antibacterial therapy.
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- HY-124187
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Ethyl pinolenate
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Biochemical Assay Reagents
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Others
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Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
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HY-L170
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190 compounds
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An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 190 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
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Cat. No. |
Product Name |
Type |
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- HY-126839
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5-Dodecanoylaminofluorescein di-β-D-Galactopyranoside
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Fluorescent Dyes/Probes
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C12FDG (5-Dodecanoylaminofluorescein di-β-D-Galactopyranoside) is a lipophilic green fluorescent substrate for β-galactosidase detection. C12-FDG is more sensitive than FDG (HY-101895) for beta-galactosidase activity determinations in animal cells .
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Cat. No. |
Product Name |
Type |
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- HY-W099563
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Enzyme Substrates
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4-Nitrophenyl stearate, which is an ester formed by the condensation of stearic acid and 4-nitrophenol, is commonly used as a substrate for enzymatic assays, where the hydrolysis of ester bonds by esterase and lipase can be measured by absorbance or ratio In addition, 4-Nitrophenyl stearate has been used as a model compound to study the enzymatic activity and selectivity of lipases and esterases from various sources. The long hydrophobic tail of the molecule makes it suitable for use in lipophilic Good solubility in the environment makes it a useful probe for studying lipid metabolism.
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- HY-124187
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Ethyl pinolenate
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Drug Delivery
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Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
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- HY-143686
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Drug Delivery
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ImmTher is a liposome-encapsulated lipophilic disaccharide tripeptide derivative of muramyl dipeptide. ImmTher can up-regulate specific monocyte cytokine genes and activate monocyte-mediated tumoricidal activity .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0783
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- HY-N8572
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Structural Classification
Flavonoids
other families
Flavones
Coniogramme japonica (Thunb.) Diels
Plants
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PARP
Reactive Oxygen Species
Aryl Hydrocarbon Receptor
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3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects .
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- HY-N12201
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- HY-N0783R
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- HY-117204
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Structural Classification
Natural Products
Microorganisms
Source classification
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Antibiotic
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AA-57 is an acidic lipophilic antibiotic isolated from the fermentation broth of Actinomycetes strain AA-57. The AA-57 strain was isolated from a soil sample collected in Koriyama City, Fukushima Prefecture, Japan. AA-57 has antibacterial properties against Gram-positive bacteria, Gram-negative bacteria, and acid-fast bacteria. AA-57 was discovered by screening actinomycete cultures for antibacterial properties. AA-57 exhibits significant antibacterial activity and has inhibitory effects against a variety of bacteria. The discovery of AA-57 provides new possibilities for antibacterial therapy.
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