Search Result
Results for "
whole
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
7
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-159114
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-
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- HY-E70361
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Unsonicated White Blood Cell Esterase, WBC Esterase
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Biochemical Assay Reagents
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Others
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Whole Leukocyte Esterase, Human (Unsonicated White Blood Cell Esterase, WBC Esterase) is a biological material or organic compound that can be used in life science research .
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-
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- HY-137896
-
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Fluorescent Dye
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Others
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4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium is a fluorescent dye. 4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium can be used to demonstrate retrograde axonal transport to label secondary antibodies and as a fluorescent whole cell stain .
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- HY-135674
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p38 MAPK
TNF Receptor
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Inflammation/Immunology
Cancer
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SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity .
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-
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- HY-153254
-
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus .
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-
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- HY-32018
-
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MAP3K
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Cancer
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Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM .
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-
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- HY-N1027
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Others
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Others
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12α-Hydroxygrandiflorenic acid is a compound isolated from the whole plant of Wedelia chinensis (Osbeck.) .
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-
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- HY-N1020
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Others
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Others
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11-Hydroxyrankinidine is an alkaloid compound isolated from the whole plant of Gelsemium elegans .
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-
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- HY-106093
-
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COX
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Inflammation/Immunology
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Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood .
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- HY-113209A
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Endogenous Metabolite
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Metabolic Disease
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Ent-8-Iso-15(S)-prostaglandin F2α is an isomer of 8-Isoprostaglandin F2α, with a better inhibiting activity in the whole blood platelet aggregation inhibition assay .
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- HY-137892
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Epigenetic Reader Domain
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Inflammation/Immunology
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GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .
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- HY-153440
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JAK
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Cancer
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JAK-IN-25 (compound 19) is a potent JAK inhibitor with IC50s of 6 nM, 21 nM, 8 nM, 1051 nM for TYK2, JAK1, JAK2, JAK3, respectively. JAK-IN-25 inhibits human whole blood IL-12 (HEB IL-12) with an IC50 of 28 nM. JAK-IN-25 has the potential for cancer research .
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- HY-153673
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IRAK
PROTACs
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Cancer
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PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively .
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- HY-120878
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CXCR
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Inflammation/Immunology
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CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM .
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- HY-N11914
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Others
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Others
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Isolaureline can be isolated from the whole plant of Stephania longa .
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- HY-N2559
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Amylohexaose
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Endogenous Metabolite
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Others
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Maltohexaose is a natural saccharide, and can be produced from amylose, amylopectin and whole starch.
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- HY-N0463
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Others
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Others
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Blinin is a neoclerodane diterpene, isolated from the whole plant of Conyza blinii .
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- HY-N2418
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Others
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Others
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Homoarbutin is a phenolic glycoside isolated from the whole plants of Pyrola japonica .
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-
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- HY-107918
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- HY-N9273
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Others
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Others
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Taraxasterone (compound 6) is a triterpene that can be found in the whole plant of Sida acuta .
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- HY-N9072
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Others
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Others
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Lucidioline is a Alkaloids product that can be isolated from the whole plants of Lycopodium japonicum. .
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- HY-N8861
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Others
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Others
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Isoflavidinin is a Phenols product that can be isolated from the whole plants of Pholidota articulata. .
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- HY-N8966
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Others
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Others
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Saropyrone is a Phenols product that can be isolated from the whole plants of Hypericum Japonicum. .
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- HY-N8991
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Others
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Others
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Isohomoarbutin is a Phenols product that can be isolated from the whole herbs of Pyrola rotundifolia. .
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- HY-N8968
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Others
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Others
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Scillascillol is a Triterpenoids product that can be isolated from the whole plants of Scilla scilloides. .
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- HY-113486
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- HY-N3621
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Others
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Others
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Corchoionol C is a n-butanol-soluble fraction of the whole plant extract of Pulicaria undulate .
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- HY-N9028
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Others
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Others
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Scillascillone is a lanostane-type triterpenoid, which can be isolated from the whole plants of Scilla scilloides .
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- HY-N9250
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Others
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Others
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Gentiside J is a Phenols product that can be isolated from the whole plants of Gentiana rigescens Franch. .
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- HY-N1176
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(-)-Tartarinoid A
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Others
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Others
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Tatarinoid A ((-)-Tartarinoid A) is a Phenols product that can be isolated from the whole plants of Gentiana rigescens Franch. .
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-
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- HY-N11800
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Others
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Others
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Transilin is a sesquiterpene lactone. Transilin can be isolated from the whole plant of Lepisorus contortus (Christ) Ching .
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- HY-N3350
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Others
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Others
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Lycoclavanol is a serratane-type triterpenoid, which can be isolated from the dried whole plants of Lycopodium japonicum .
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- HY-125965
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Bacterial
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Infection
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BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme .
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- HY-N9048
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Others
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Others
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12α-Methoxygrandiflorenic acid (compound 6) is a compound isolated from the whole plant of Wedelia chinensis (Osbeck.) .
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- HY-W001154
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Others
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Others
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Methyl 2,6-dihydroxybenzoate is a volatile, that can be isolated from whole flowers and corolla of Primula spectabilis .
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- HY-N9087
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Bacterial
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Infection
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Filicenol B can be isolated from the whole plant of Adiantum lunulatum. Filicenol B has antibacterial activity .
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-
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- HY-N9898
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Others
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Others
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Sinocrassoside C1 is a natural compound isolated from themethanolic extract of the whole plant ofSinocrassula indica (Crassulaceae) .
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- HY-13344
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-
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- HY-13344A
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-
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- HY-N3854
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Others
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Others
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Erysubin B is a prenylated isoflavonoid, which can be isolated from the whole plant (roots and aerial parts) of Erinacea anthyllis .
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- HY-N10030
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Others
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Others
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11-O-Syringylbergenin is a bergenin derivative isolated from the whole plants of Corylopsis willmottiae Rehd. et Wils
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-
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- HY-B0753
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S1702; SE1702
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Potassium Channel
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Cardiovascular Disease
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Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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- HY-N2749
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Others
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Others
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7-Hydroxy-5,8-dimethoxyflavanone is a compound isolated from the ethanol extract of the whole plants of Sarcandra hainanensis .
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- HY-N11961
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Others
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Others
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2-Hydroxy-3-methoxybenzoic acid glucose ester is a Phenols product that can be isolated from the whole plants of Gentiana scabra. .
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- HY-125115
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Others
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Others
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Jatrophane 3 is a kind of jatrophane diterpene polyester that can be isolated from the highly irritant extract of whole fresh plants of E. peplus L. (Euphorbiaceae) .
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- HY-125116
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Others
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Others
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Jatrophane 2 is a kind of jatrophane diterpene polyester that can be isolated from the highly irritant extract of whole fresh plants of E. peplus L. (Euphorbiaceae) .
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-
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- HY-N9244
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Others
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Others
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Filic-3-en-25-al is a Triterpenoids product that can be isolated from the whole plant of Adiantum lunulatum .
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- HY-163039
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-
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- HY-N3073
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Picraline, 16-de(acetoxymethyl)-16-formyl-
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COX
Lipoxygenase
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Others
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Picralinal (Picraline, 16-de(acetoxymethyl)-16-formyl-) is a Triterpenoids product that can be isolated from the whole plants of Scilla scilloides. .
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-
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- HY-107275
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Cholinesterase (ChE)
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Neurological Disease
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Ebeiedinone, a steroidal alkaloid from Fritillaria species, inhibits the bioactivity of human whole blood cholinesterase (ChE) at the concentration of 0.1 mM, with the inhibitory effects of 69.0% .
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- HY-113486S1
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- HY-134820
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MALT1
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Inflammation/Immunology
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MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research .
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- HY-12089
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CP-529414
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CETP
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Endocrinology
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Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM .
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- HY-U00170
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- HY-109066
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IW-1701
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Guanylate Cyclase
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Cardiovascular Disease
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Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay .
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- HY-135337
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Potassium Channel
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Metabolic Disease
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Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877) . Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM .
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- HY-N7932
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Others
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Others
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Kaempferol 3-O-α-L-rhamnopyranosyl(2,1)-α-L-rhamnopyranoside (compound 23) is a flavonoid isolated from the whole herb of E. wushanense .
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- HY-162664
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STING
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Inflammation/Immunology
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STING antagonist 1 (Compound 107) is the antagonist for STING with an IC50 of 3.8 nM. STING antagonist 1 exhibits inhibitory efficacy in human whole blood, with IC50 of 31 nM .
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- HY-110225
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UCB L059-d6 (ring-d6)
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Others
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Others
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Levetiracetam-d6 (ring-d6) can be used as internal standard for the determination of Levetiracetam (HY-B0106) content in whole blood .
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- HY-N9227
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Others
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Others
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7,13-Dideacetyl-9,10-didebenzoyltaxchinin C is a Diterpenoids product that can be isolated from the whole plants of Taxus chinensis var. mairei. .
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- HY-113486R
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Endogenous Metabolite
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Metabolic Disease
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Lathosterol (Standard) is the analytical standard of Lathosterol. This product is intended for research and analytical applications. Lathosterol is a cholesterol-like molecule. Serum Lathosterol concentration is an indicator of whole-body cholesterol synthesis.
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- HY-133614
-
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Potassium Channel
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Others
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Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp .
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- HY-113486S
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- HY-N3573
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Potassium Channel
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Others
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Chlorahololide D is a potent and selective Potassium Channel blocker with an IC50 value of 2.7 μM. Chlorahololide D is a nature product that could be isolated from the whole plant of Chloranthus holostegius .
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- HY-N8973
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Others
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Others
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2,7-Dimethyl-1,4-dihydroxynaphthalene 1-O-glucoside is a Phenols product that can be isolated from the whole plants of Pholidota articulata .
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- HY-119688
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Parasite
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Others
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Amabiline is a compound isolated from a plant that contains a variety of bioactive ingredients including Amabiline. The plant as a whole has a variety of traditional uses and also has certain pharmacological activity and toxicity.
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- HY-N7252
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Bacterial
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Infection
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Daphnin is one of the major coumarin bioactive components with antibacterial activity. Daphnin is isolated from the whole herb of Daphne odora (Thunb.), which is a folk medicine in China for the relief of fever .
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- HY-117690
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PROTACs
Epigenetic Reader Domain
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Cancer
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dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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- HY-148739
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PROTACs
Epigenetic Reader Domain
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Cancer
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dBRD 9-A is a PROTAC which can selective degrade BRD9. dBRD 9-A improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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- HY-162457
-
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DNA/RNA Synthesis
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Infection
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Mn007 is a potent inhibitor of bovine pancreatic DNase I, with the IC50 of 45 μM, by forming molecular aggregation. Mn007 shows suppression of S. pyogenes growth in human whole blood .
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- HY-169908
-
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STAT
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Cancer
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STAT3-IN-37 (Compound 101) is the inhibitor for STAT3 with an IC50 of 15 nM (measuring by DNA-HTRF assay) or 2 nM (measuring by human whole blood SOCS3 qPCR assay) .
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- HY-P1015
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Vasoactive Intestinal Peptide, guinea pig
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PACAP Receptor
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Neurological Disease
Metabolic Disease
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VIP Guinea pig (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function .
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- HY-161924
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HIV
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Infection
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HIV-1 inhibitor-73 (compound 13c) is a potent anti-HIV-1 agent, against the whole tested viral panel with EC50 ranging from 4.68 to 229 nM .
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- HY-114586
-
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Angiotensin Receptor
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Cancer
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L-158809 is an angiotensin type 1 (AT1) receptor antagonist that prevents or ameliorates fractionated whole-brain irradiation-induced cognitive impairment. L-158809 is promising for research of brain tumor .
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- HY-116205
-
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iGluR
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Others
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UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
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- HY-U00037
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PLA 725
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Phospholipase
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Inflammation/Immunology
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Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
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- HY-100686
-
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GABA Receptor
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Neurological Disease
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U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
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- HY-P1015A
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Vasoactive Intestinal Peptide, guinea pig TFA
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PACAP Receptor
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Neurological Disease
Metabolic Disease
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VIP Guinea pig TFA (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function .
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- HY-B0753R
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S1702 (Standard); SE1702 (Standard)
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Potassium Channel
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Cardiovascular Disease
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Gliclazide (Standard) is the analytical standard of Gliclazide. This product is intended for research and analytical applications. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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- HY-10437A
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MK-0633 tosylate
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Lipoxygenase
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Inflammation/Immunology
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Setileuton tosylate is an inhibitor for 5-lipoxygenase, that inhibits the oxidation of arachidonic acid by recombinant human 5-LO, and the production of LTB4 in calcium ionophore-stimulated human whole blood, with IC50 of 3.9 and 52 nM, respectively .
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- HY-70068
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-
- HY-N1782
-
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Others
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Inflammation/Immunology
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3,4-O-Isopropylidene-shikimicn acid is a natural product that can be isolated from the whole plants of Hypericum wightianum. 3,4-O-Isopropylidene-shikimic acid has anti-inflammatory effect and antioxidant activities .
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- HY-108695
-
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Apoptosis
Endogenous Metabolite
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Cancer
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Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Anti-cancer activities .
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- HY-N11912
-
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Biochemical Assay Reagents
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Cancer
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Soladulcoside A is a steroidal glycoside and antineoplastic agent that can be obtained from the whole plant of Solanum nigrum. Soladulcoside A can inhibit A549 cells and has the potential to study cancers such as non-small cell lung cancer (NSCLC) .
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- HY-163040
-
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Biochemical Assay Reagents
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Inflammation/Immunology
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DOTA-Tyr-Lys-DOTA is a DOTA-based small molecule hapten. DOTA-Tyr-Lys-DOTAexhibits rapid clearance and low whole-body retention. DOTA-Tyr-Lys-DOTA can used in study pretargeted radioimmunotherapy .
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- HY-P99725
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PF-06741086
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Thrombin
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Metabolic Disease
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Marstacimab (PF-06741086) is an anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. Marstacimab can be used for the research of hemophilia .
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-
- HY-B0753S
-
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Potassium Channel
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Cardiovascular Disease
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Gliclazide-d4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic[1].
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- HY-B2158
-
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Estrogen Receptor/ERR
COX
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Cardiovascular Disease
Endocrinology
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Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
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-
- HY-100937
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PD 116948
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Adenosine Receptor
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Cardiovascular Disease
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DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes .
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- HY-120865
-
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NO Synthase
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Inflammation/Immunology
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1,3-PBIT is a potent inhibitor of iNOS with a Ki of 47 nM compared to Ki values for eNOS and nNOS are 9 and 0.25 μM, respectively, for the purified human enzymes. Its inhibition in whole cells is greatly diminished, presumably to poor membrane permeability.
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- HY-19614
-
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CETP
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Cardiovascular Disease
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BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively .
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- HY-126015
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P053
1 Publications Verification
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Acyltransferase
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Metabolic Disease
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P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5 μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator .
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-
- HY-10437
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MK-0633
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Lipoxygenase
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Inflammation/Immunology
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Setileuton (MK-0633) is an inhibitor for 5-lipoxygenase, that inhibits the oxidation of arachidonic acid by recombinant human 5-LO, and the production of LTB4 in calcium ionophore-stimulated human whole blood, with IC50 of 3.9 and 52 nM, respectively .
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-
- HY-76612
-
-
- HY-32015
-
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MAP3K
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Inflammation/Immunology
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Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM .
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-
- HY-15321
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MK-0663; L-791456
|
COX
|
Inflammation/Immunology
Cancer
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Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
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-
- HY-N12339
-
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Virus Protease
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Infection
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Wulfenioidin F is a diterpenoid, that can be isolated from the whole plant of Orthosiphon wulfenioides. Wulfenioidin F exhibits activity against Zika virus (ZIKV) with an EC50 of 8.07 μM. Wulfenioidin F interferes with the replication of the ZIKV by inhibiting the expression of the ZIKV envelope (E) protein .
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- HY-N12872
-
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Others
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Endocrinology
|
(2R)-O-[4'-(3"-Hydroxypropyl)-2',6'-dimethoxyphenyl]-3-O-β-Dglucopyranosyl-sn-glycerol (compound 6) is a glycerol glycoside that can Isolated from the whole plant of genus Pilea .
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- HY-N7252R
-
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Bacterial
|
Infection
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Daphnin (Standard) is the analytical standard of Daphnin. This product is intended for research and analytical applications. Daphnin is one of the major coumarin bioactive components with antibacterial activity. Daphnin is isolated from the whole herb of Daphne odora (Thunb.), which is a folk medicine in China for the relief of fever .
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-
- HY-120606
-
|
Lipoxygenase
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Inflammation/Immunology
|
A-78773 is a 5-lipoxygenase inhibitor. A-78773 can inhibit the formation of LTB4 in human whole blood and human neutrophils, with IC50 values of 85 nM and 20 nM, respectively. A-78773 can be used in the study of inflammation-related diseases .
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-
- HY-W699533
-
Valeryl-4-hydroxyvalsartan; CGP 71580
|
Drug Metabolite
|
Cardiovascular Disease
|
4-Hydroxy valsartan is a metabolite of Valsartan (HY-18204). 4-Hydroxy valsartan regulates the expression of platelet surface receptors and inhibits conventional plasma or whole blood collagen induced platelet aggregation. 4-Hydroxy valsartan has antiplatelet activity .
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-
- HY-18725
-
-
- HY-18725A
-
-
- HY-N9000
-
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TNF Receptor
|
Inflammation/Immunology
|
Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells .
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-
- HY-145884
-
|
Btk
|
Inflammation/Immunology
|
BTK-IN-8 is a potent and selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM) .
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- HY-108695B
-
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Apoptosis
Endogenous Metabolite
|
Cancer
|
(±)-Enterodiol is the racemate of Enterodiol (HY-108695). Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Enterodiol has anti-cancer activities .
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-
- HY-12159
-
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Integrin
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Inflammation/Immunology
|
MK-0668 is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
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-
- HY-12159A
-
|
Integrin
|
Inflammation/Immunology
|
MK-0668 mesylate is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 mesylate exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
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-
- HY-P3102
-
|
GCGR
|
Metabolic Disease
|
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
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-
- HY-15321S
-
MK-0663-d4; L-791456-d4
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COX
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Others
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Etoricoxib-d4 is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
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-
- HY-B2158S
-
|
Estrogen Receptor/ERR
COX
|
Cardiovascular Disease
Endocrinology
|
Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood[1][2][3].
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-
- HY-113854
-
AZD2906
1 Publications Verification
|
Glucocorticoid Receptor
|
Cardiovascular Disease
Endocrinology
|
AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively .
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-
- HY-P2989
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Pyruvate carboxylase is a biotin-containing enzyme that catalyzes the HCO3 − and MgATP dependent carboxylation of pyruvate to form oxaloacetate. Pyruvate carboxylase plays an essential role in controlling whole-body energetics through regulation of gluconeogenesis in the liver, synthesis of fatty acids in adipocytes, and insulin secretion in pancreatic β cells .
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-
- HY-N12919
-
|
Others
|
Endocrinology
|
(E)-3-Dodecenol is a termite trail pheromone that can be isolated from the whole body and thymus extracts of termite workers. (E)-3-Dodecenol induces orientational and recruitment behavior effects, but its induction effect is weaker than (Z)-Dodecenol or natural thymus extracts .
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-
- HY-P3102A
-
|
GCGR
|
Metabolic Disease
|
GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
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-
- HY-116211
-
WIN-25978
|
Biochemical Assay Reagents
|
Neurological Disease
|
Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mouse brain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
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-
- HY-B2158R
-
|
Estrogen Receptor/ERR
COX
|
Cardiovascular Disease
Endocrinology
|
Chlorotrianisene (Standard) is the analytical standard of Chlorotrianisene. This product is intended for research and analytical applications. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
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-
- HY-W419570
-
|
P2Y Receptor
|
Cardiovascular Disease
|
(Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM) .
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-
- HY-B0883
-
Proflavin hemisulfate; 3,6-Diaminoacridine hemisulfate
|
Bacterial
Potassium Channel
Autophagy
|
Infection
Cancer
|
Proflavine hemisulfate, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent . Proflavine hemisulfate behaves as a pore blocker for Kir3.2. Proflavine hemisulfate is a potential lead compound for Kir3.2-associated neurological diseases .
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-
- HY-B1741
-
3,6-Diaminoacridine
|
Bacterial
Fluorescent Dye
|
Neurological Disease
Cancer
|
Proflavine, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent . Proflavine behaves as a pore blocker for Kir3.2. Proflavine is a potential lead compound for Kir3.2-associated neurological diseases .
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-
- HY-151894
-
|
Epigenetic Reader Domain
|
Cancer
|
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases .
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-
- HY-14166
-
L 663536
|
FLAP
Leukotriene Receptor
PPAR
Apoptosis
|
Cancer
|
MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis .
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-
- HY-123812
-
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
|
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research .
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-
- HY-139589
-
ISC-27864; GRC-27864
|
PGE synthase
|
Neurological Disease
Inflammation/Immunology
|
Zaloglanstat (ISC-27864) is a selective and orally active inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 5 nM. Zaloglanstat inhibits PGE2 release of IC50 at 161 nM and 154 nM in whole blood of pigs and dogs, respectively. Zaloglanstat can be used in studies of asthma, osteoarthritis and neurodegenerative diseases .
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-
- HY-N10595
-
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Others
|
Others
|
Ladanetin-6-O-β-(6′′-O-acetyl)glucoside is a flavonoid isolated from the whole plants of Dracocephalum tanguticum, with antioxidant ability. Flavonoids from Dracocephalum tanguticum show cardioprotective effects against Doxorubicin (HY-15142A)-induced toxicity in H9c2 cells .
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-
- HY-14166A
-
L 663536 sodium salt
|
PPAR
Apoptosis
Leukotriene Receptor
FLAP
|
Cancer
|
MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis .
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-
- HY-D2041
-
|
Fluorescent Dye
|
Cancer
|
3-HTC is a chemical fluorescent probe. 3-HTC reacts reversibly with thiols and disulfides, and can be used to measure dynamic GSH/GSSH ratios in vitro as well as to monitor the reversible redox status of whole cell lysates (λmax: 448 nm in its reduced thiolate form, and a λmax 370-410 nm for the oxidized mixed disulfide) .
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-
- HY-170364
-
-
- HY-100864
-
|
PGE synthase
|
Inflammation/Immunology
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM) .
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-
- HY-128338
-
|
CETP
|
Cardiovascular Disease
|
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively .
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-
- HY-N7155
-
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
2,4,7-Trihydroxy-9,10-dihydrophenanthrene is a dihydrophenanthrene derivative that can be isolated from the air-dried whole plant of Pholidota chinensis Lindl.. 2,4,7-Trihydroxy-9,10-dihydrophenanthrene shows potent activities of IC50 at 16.2 μM in DPPH radical-scavenging assay .
|
-
- HY-10885
-
ABT-472
|
PARP
|
Cancer
|
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research .
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-
- HY-156961
-
|
JAK
|
Inflammation/Immunology
|
GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases .
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-
- HY-15321R
-
MK-0663 (Standard); L-791456 (Standard)
|
COX
|
Inflammation/Immunology
Cancer
|
Etoricoxib (Standard) is the analytical standard of Etoricoxib. This product is intended for research and analytical applications. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
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-
- HY-N2574
-
|
Glycosidase
|
Metabolic Disease
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
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-
- HY-N9814
-
|
NO Synthase
|
Inflammation/Immunology
|
Shanciol B, isolated from the ethyl acetate extract of the air-dried whole plant of Pholidota imbricate Hook, inhibits nitric oxide (NO) production and 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity . Shanciol B is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with anti-inflammatory activity .
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-
- HY-15321S1
-
MK-0663-13C,d3; L-791456-13C,d3
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
Cancer
|
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
|
-
- HY-N8371
-
|
NO Synthase
COX
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression .
|
-
- HY-15321S2
-
MK-0663-d3; L-791456-d3
|
COX
|
Inflammation/Immunology
|
Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood[2][3][4].
|
-
- HY-108695BR
-
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
(±)-Enterodiol (Standard) is the analytical standard of (±)-Enterodiol. This product is intended for research and analytical applications. (±)-Enterodiol is the racemate of Enterodiol (HY-108695). Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Enterodiol has anti-cancer activities .
|
-
- HY-12995A
-
|
FLAP
|
Inflammation/Immunology
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
|
-
- HY-128342
-
|
Complement System
|
Inflammation/Immunology
|
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM .
|
-
- HY-136527
-
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .
|
-
- HY-N10623
-
|
Tyrosinase
|
Cancer
|
5-epi-Arvestonate A is a sesquiterpenoid isolated from the whole plants of Seriphidium transiliense. 5-epi-Arvestonate A promotes melanogenic production by activating the transcription of microphthalmia-associated transcription factor (MITF) and tyrosinase family genes. 5-epi-Arvestonate A inhibits the expression of IFN-γ-chemokine through the JAK/STAT signaling pathway in immortalized human keratinocyte (HaCaT) cells .
|
-
- HY-153480
-
BAX499
|
Factor Xa
|
Others
|
ARC19499 is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
|
-
- HY-153480A
-
BAX499 sodium
|
Factor Xa
Factor VIIa
|
Others
|
ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
|
-
- HY-120245
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK-340 is a BET inhibitor with high affinity and significant selectivity for BD2 from BRD4 with a pIC50 of 7.2. GSK-340 inhibits MCP-1 release in Lipopolysaccharide (HY-D1056) treated PBMCs and whole blood with the pIC50 of 7.4 and 6.0, respectively. GSK-340 has immunomodulatory activity .
|
-
- HY-102064
-
|
5-HT Receptor
|
Neurological Disease
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
|
-
- HY-150508
-
|
CD38
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
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 .
|
-
- HY-153993
-
|
Endogenous Metabolite
|
Others
|
Pyrocatechol sulfate, a phenolic metabolite present in human plasma, is associated with the consumption of specific foods such as berries and the condition of gut microbiota. It serves as a potential urinary biomarker for kidney function, dialytic clearance, whole grain consumption, and regular coffee intake. Additionally, Pyrocatechol sulfate, along with other phenolic sulfates, plays a role in modulating various biological functions, including those related to brain health and the rhythmic beating of cardiomyocytes.
|
-
- HY-150720
-
|
JAK
IFNAR
|
Inflammation/Immunology
|
TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research .
|
-
- HY-14165A
-
(S)-BAY X 1005; (S)-DG-031
|
Leukotriene Receptor
FLAP
|
Inflammation/Immunology
|
(S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood .
|
-
- HY-19443
-
|
Histamine Receptor
Lipoxygenase
|
Inflammation/Immunology
|
UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guinea pigs. UCB-35440 can be used for research on asthma and skin inflammation .
|
-
- HY-B1328R
-
|
Endogenous Metabolite
Keap1-Nrf2
|
Neurological Disease
Cancer
|
Pyridoxine (Standard) is the analytical standard of Pyridoxine. This product is intended for research and analytical applications. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
In Vitro: Pyridoxine exerts a protective potential against AD, attenuates ROS levels, decreases the expressions of cytoplasmic Nrf2, and upregulates whole-cell HO-1 expression .
|
-
- HY-18862
-
|
p38 MAPK
|
Inflammation/Immunology
|
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
|
-
- HY-D1585
-
|
Fluorescent Dye
|
Others
|
BODIPY TR methyl ester is a lipophilic GFP Counterstain. BODIPY TR methyl ester dye readily permeates cell membranes and localizes in endomembranous organelles but not localize strongly in plasma membranes. BODIPY TR methyl ester is an excellent red fluorescent vital dye (Ex=568 nm, Em=625 nm), can be used to reveal the location and shapes of cell nuclei, the shapes of cells within embryonic tissues, as well as the bound aries of organ-forming tissues within the whole embryo .
|
-
- HY-117931
-
|
Potassium Channel
|
Neurological Disease
|
NS004 is a potassium (BK) channel activator that increases Iberiotoxin (HY-P0190) or Tetraethylammonium (HY-B1793)-sensitive whole-cell efflux currents. NS004 also significantly increased the activity of individual GH3 cell BK channels and rat brain BK channels reorganized into planar lipid bilayers, causing an increase in channel mean open time, a decrease in intermittent time, and an increase in channel voltage/calcium sensitivity .
|
-
- HY-N2574R
-
|
Glycosidase
|
Metabolic Disease
|
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
- HY-10797
-
CJ-042794
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers .
|
-
- HY-15425
-
PF-543
Maximum Cited Publications
10 Publications Verification
Sphingosine Kinase 1 Inhibitor II
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy .
|
-
- HY-15425B
-
Sphingosine Kinase 1 Inhibitor II hydrochloride
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy .
|
-
- HY-125975
-
|
Lipoxygenase
|
Inflammation/Immunology
|
1-Naphthyl 3,5-dinitrobenzoate is a potent 5-lipoxygenase inhibitor with IC50 values of 1.04 µM and 3.6 µM for 5-LOX and mPGES-1, respectively. 1-Naphthyl 3,5-dinitrobenzoate has strong inhibition activity in the human whole blood (HWB) assay with an IC50 value of 8.6 μM. 1-Naphthyl 3,5-dinitrobenzoate can be used in research of inflammation .
|
-
- HY-P3071
-
Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Inflammation/Immunology
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ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
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- HY-161860
-
|
Bacterial
|
Cancer
|
Antibacterial agent 233 (Compound 7c) exhibits inhibitory efficacy against Helicobacter pylori with MIC of 0.4-1.6 μg/mL. Antibacterial agent 233 inhibits jack bean urease (IC50 is 0.27 μg/mL), changes the permeability of H. pylori cell membrane, causes the leakage of cellular contents. Antibacterial agent 233 exhibits metabolic stability in whole blood and artificial gastric fluid. Antibacterial agent 233 exhibits antitumor efficacy against U2OS in mice .
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- HY-15425A
-
PF-543 Citrate
Maximum Cited Publications
10 Publications Verification
Sphingosine Kinase 1 Inhibitor II Citrate
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy .
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-
- HY-108642
-
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
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-
- HY-108642B
-
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
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-
- HY-108642A
-
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
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-
- HY-160023
-
|
Ras
|
Cancer
|
D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
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-
- HY-122144
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Teroxirone
|
Endogenous Metabolite
|
Cancer
|
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 rat liver 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 .
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-
- HY-120059
-
|
Potassium Channel
|
Neurological Disease
|
NS4591 is a modulator of calcium-activated potassium channels with activity that enhances small (SK) and intermediate (IK) conductivity. NS4591 doubled IK-mediated currents in whole-cell patch-clamp experiments at a concentration of 45 +/- 6 nM, and doubled SK3-mediated currents at a concentration of 530 +/- 100 nM. NS4591 inhibits the number of action potentials generated by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons. NS4591 also reduced carbakol-induced detrusor ring contraction in the rat bladder, demonstrating sensitivity to apamin .
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-
- HY-123789
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
T-5342126 is a toll-like receptor 4 (TLR4) antagonist. It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50=27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s=110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.
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-
- HY-116153
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
HUHS2002 is a free fatty acid derivative with the ability to enhance α7 cholinergic receptor activity. HUHS2002 enhances whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner. The effects of HUHS2002 were blocked in the presence of the Ca2?/calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. HUHS2002 activated CaMKII in cultured rodent hippocampal neurons, and this activation was abolished by KN-93. HUHS2002 also partially inhibited the activity of protein phosphatase 1 (PP1) in a cell-free PP1 activity assay .
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-
- HY-103693
-
NAZ2329
3 Publications Verification
|
Phosphatase
|
Cancer
|
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
|
-
- HY-169430
-
|
PGE synthase
|
|
AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM against mPGES-1. AGU654 inhibits mPGES-1 to block the pathway converting arachidonic acid into prostaglandin E2 (PGE2) by COX-1/2, thereby alleviating inflammatory responses, pain, and fever. In activated human monocyte-derived macrophages and human whole blood models, AGU654 selectively suppresses bacterial exotoxin-induced PGE2 production while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, exhibiting excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a strategy for studying inflammatory diseases and pain .
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-
- HY-118156
-
|
Others
|
Others
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
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-
-
-
HY-L022M
-
|
3,102 compounds
|
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved drugs have identified bioactivities, good pharmacokinetic characteristics and safety which are suitable for drug repurposing.
MCE owns a unique collection of 3,102 approved compounds which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties. The package of this library is 96-well microplate with peelable foil seal, which makes the screening process easier and faster.
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Cat. No. |
Product Name |
Type |
-
- HY-137896
-
|
Fluorescent Dyes/Probes
|
4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium is a fluorescent dye. 4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium can be used to demonstrate retrograde axonal transport to label secondary antibodies and as a fluorescent whole cell stain .
|
-
- HY-B0883
-
Proflavin hemisulfate; 3,6-Diaminoacridine hemisulfate
|
Fluorescent Dyes/Probes
|
Proflavine hemisulfate, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent . Proflavine hemisulfate behaves as a pore blocker for Kir3.2. Proflavine hemisulfate is a potential lead compound for Kir3.2-associated neurological diseases .
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-
- HY-D2041
-
|
Fluorescent Dyes/Probes
|
3-HTC is a chemical fluorescent probe. 3-HTC reacts reversibly with thiols and disulfides, and can be used to measure dynamic GSH/GSSH ratios in vitro as well as to monitor the reversible redox status of whole cell lysates (λmax: 448 nm in its reduced thiolate form, and a λmax 370-410 nm for the oxidized mixed disulfide) .
|
-
- HY-D1585
-
|
Fluorescent Dyes/Probes
|
BODIPY TR methyl ester is a lipophilic GFP Counterstain. BODIPY TR methyl ester dye readily permeates cell membranes and localizes in endomembranous organelles but not localize strongly in plasma membranes. BODIPY TR methyl ester is an excellent red fluorescent vital dye (Ex=568 nm, Em=625 nm), can be used to reveal the location and shapes of cell nuclei, the shapes of cells within embryonic tissues, as well as the bound aries of organ-forming tissues within the whole embryo .
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Cat. No. |
Product Name |
Type |
-
- HY-159114
-
|
Carbohydrates
|
Whole Glucan Particles is a Dectin-1a agonist. Whole Glucan Particles activates the innate immune system to improve the function of macrophages, monocytes and other immune cells .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1015
-
Vasoactive Intestinal Peptide, guinea pig
|
PACAP Receptor
|
Neurological Disease
Metabolic Disease
|
VIP Guinea pig (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function .
|
-
- HY-P3102
-
|
GCGR
|
Metabolic Disease
|
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
|
-
- HY-P1015A
-
Vasoactive Intestinal Peptide, guinea pig TFA
|
PACAP Receptor
|
Neurological Disease
Metabolic Disease
|
VIP Guinea pig TFA (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function .
|
-
- HY-P3102A
-
|
GCGR
|
Metabolic Disease
|
GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
|
-
- HY-P3071
-
Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Inflammation/Immunology
|
ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
|
-
- HY-K0311
-
1 Publications Verification
|
MCE GSH/GSSG Assay Kit is suitable for the quantitative determination of reduced and oxidized glutathione (GSH/GSSG) in whole blood, plasma, serum, urine, and tissue and cell extracts.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99725
-
PF-06741086
|
Thrombin
|
Metabolic Disease
|
Marstacimab (PF-06741086) is an anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. Marstacimab can be used for the research of hemophilia .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-108695BR
-
|
Structural Classification
Source classification
Phenols
Polyphenols
Endogenous metabolite
|
Apoptosis
Endogenous Metabolite
|
(±)-Enterodiol (Standard) is the analytical standard of (±)-Enterodiol. This product is intended for research and analytical applications. (±)-Enterodiol is the racemate of Enterodiol (HY-108695). Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Enterodiol has anti-cancer activities .
|
-
- HY-N10623
-
-
- HY-B1328R
-
-
- HY-N2574R
-
|
Tribulus terrester Linn.
Structural Classification
Zygophyllaceae
Source classification
Plants
Steroids
|
Glycosidase
|
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
Cat. No. |
Product Name |
Chemical Structure |
Cat. No. |
Product Name |
|
Classification |
-
- HY-153480A
-
BAX499 sodium
|
|
Aptamers
|
ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
|
-
- HY-153480
-
BAX499
|
|
Aptamers
|
ARC19499 is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
|
-
- HY-160067
-
|
|
Aptamers
|
T18.3 aptamer sodium is an anticoagulant RNA aptamer targeting FV/Va and eliminates the interaction of FV/FVa with phospholipid membranes. T18.3 aptamer sodium exhibits clinically relevant anticoagulant activity in plasma and whole blood and acts synergistically with low molecular weight heparin. The anticoagulant activity of T18.3 aptamer sodium is effectively and rapidly reversed by protamine sulfate .
|
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