Search Result
Results for "
whole blood
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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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- 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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- 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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- 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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- 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-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-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-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-13344A
-
-
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- HY-13344
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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-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-U00170
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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-172195
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p38 MAPK
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Inflammation/Immunology
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FS-694 is the inhibitor for p38α with an IC50 of 0.2 nM. FS-694 inhibits the TNFα release in human whole blood with an IC50 of 35.0 nM .
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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-B2158S
-
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Estrogen Receptor/ERR
COX
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Cardiovascular Disease
Endocrinology
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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-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-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-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-156961
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JAK
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Inflammation/Immunology
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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-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-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-15321S2
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MK-0663-d3; L-791456-d3
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COX
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Inflammation/Immunology
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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].
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- HY-15321
-
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MK-0663; L-791456
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COX
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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-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-120606
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Lipoxygenase
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Inflammation/Immunology
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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
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Valeryl-4-hydroxyvalsartan; CGP 71580
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Drug Metabolite
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Cardiovascular Disease
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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-145884
-
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Btk
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Inflammation/Immunology
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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-12159A
-
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Integrin
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Inflammation/Immunology
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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-12159
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Integrin
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Inflammation/Immunology
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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-18725
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- HY-18725A
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- HY-15321S
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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-113854
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AZD2906
1 Publications Verification
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Glucocorticoid Receptor
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Cardiovascular Disease
Endocrinology
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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-W419570
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P2Y Receptor
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Cardiovascular Disease
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(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-B2158R
-
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Estrogen Receptor/ERR
COX
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Cardiovascular Disease
Endocrinology
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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-14166A
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L 663536 sodium salt
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PPAR
Apoptosis
Leukotriene Receptor
FLAP
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Cancer
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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-139589
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ISC-27864; GRC-27864
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PGE synthase
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Neurological Disease
Inflammation/Immunology
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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-170364
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- HY-14166
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L 663536
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FLAP
Leukotriene Receptor
PPAR
Apoptosis
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Cancer
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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-151894
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Epigenetic Reader Domain
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Cancer
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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-B0883
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Proflavin hemisulfate; 3,6-Diaminoacridine hemisulfate
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Bacterial
Potassium Channel
Autophagy
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Infection
Cancer
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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
-
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3,6-Diaminoacridine
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Bacterial
Fluorescent Dye
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Neurological Disease
Cancer
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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-100864
-
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PGE synthase
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Inflammation/Immunology
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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-15321R
-
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MK-0663 (Standard); L-791456 (Standard)
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COX
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Inflammation/Immunology
Cancer
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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-15321S1
-
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MK-0663-13C,d3; L-791456-13C,d3
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Isotope-Labeled Compounds
COX
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Inflammation/Immunology
Cancer
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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.
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- HY-136527
-
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ROR
Interleukin Related
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Inflammation/Immunology
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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) .
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- HY-12995A
-
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FLAP
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Inflammation/Immunology
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(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 .
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- HY-120245
-
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Epigenetic Reader Domain
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Inflammation/Immunology
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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 .
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- HY-153480
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BAX499
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Factor Xa
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Others
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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.
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- HY-128342
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Complement System
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Inflammation/Immunology
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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 .
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- HY-153480A
-
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BAX499 sodium
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Factor Xa
Factor VIIa
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Others
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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.
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- HY-102064
-
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5-HT Receptor
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Neurological Disease
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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 .
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- HY-150508
-
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CD38
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
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MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
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- HY-160023
-
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D3S-001
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Ras
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Cancer
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Elisrasib is an orally active inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. Elisrasib 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-19443
-
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Histamine Receptor
Lipoxygenase
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Inflammation/Immunology
|
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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 .
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- HY-150720
-
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JAK
IFNAR
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Inflammation/Immunology
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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 .
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- HY-14165A
-
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(S)-BAY X 1005; (S)-DG-031
|
Leukotriene Receptor
FLAP
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Inflammation/Immunology
|
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(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 .
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- HY-18862
-
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p38 MAPK
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Inflammation/Immunology
|
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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) .
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- HY-10797
-
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CJ-042794
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Prostaglandin Receptor
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Inflammation/Immunology
Endocrinology
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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 .
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- 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
|
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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 .
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- HY-15425B
-
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Sphingosine Kinase 1 Inhibitor II hydrochloride
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SphK
LPL Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-161860
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Bacterial
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Cancer
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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-125975
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Lipoxygenase
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Inflammation/Immunology
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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 .
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- HY-108642B
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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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-108642
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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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-108642A
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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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-15425A
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PF-543 Citrate
Maximum Cited Publications
10 Publications Verification
Sphingosine Kinase 1 Inhibitor II Citrate
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SphK
LPL Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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-122144
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Teroxirone
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Endogenous Metabolite
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Cancer
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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-123789
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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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-169430
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PGE synthase
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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
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Others
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Others
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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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| Cat. No. |
Product Name |
Type |
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- HY-B0883
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Proflavin hemisulfate; 3,6-Diaminoacridine hemisulfate
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Fluorescent Dyes/Probes
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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-K0311
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1 Publications Verification
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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.
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| Cat. No. |
Product Name |
Target |
Research Area |
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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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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-153480A
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BAX499 sodium
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Aptamers
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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.
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- HY-160067
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Aptamers
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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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- HY-153480
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BAX499
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Aptamers
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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.
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