Search Result
Results for "
human whole blood
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-13344A
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- HY-13344
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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-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-U00170
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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-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-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-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-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-18725
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- HY-18725A
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-
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- HY-132248
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Lenalidomide 5'-amine
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TNF Receptor
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Inflammation/Immunology
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C5 Lenalidomide (Lenalidomide 5'-amine) (Compound 8a) is a thalidomide analog and is a potent inhibitor of TNF-α production (IC50 = 100 μM in LPS stimulated human PBMC and IC50 = 480 nM in whole blood) .
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- HY-13344AR
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Phosphodiesterase (PDE)
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Inflammation/Immunology
Cancer
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PF-8380 (hydrochloride) (Standard) is the analytical standard of PF-8380 (hydrochloride). This product is intended for research and analytical applications. PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
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- HY-13344R
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Phosphodiesterase (PDE)
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Inflammation/Immunology
Cancer
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PF-8380 (Standard) is the analytical standard of PF-8380. This product is intended for research and analytical applications. PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
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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-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-156961
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GLPG3667
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JAK
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Inflammation/Immunology
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Cadefrecitinib (GLPG3667) is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. Cadefrecitinib 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. Cadefrecitinib has the potential for the study of inflammatory and autoimmune diseases .
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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-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-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-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-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-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-170364
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- HY-14166
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MK-886
Maximum Cited Publications
9 Publications Verification
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-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-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-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-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-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 . 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-15321R
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MK-0663 (Standard); L-791456 (Standard)
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Reference Standards
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-14165A
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(S)-BAY X 1005; (S)-DG-031
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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-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-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-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-156409
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JAK
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Inflammation/Immunology
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ABBV-712 is a selective and orally active inhibitor of Tyrosine kinase 2 (TYK2). ABBV-712 has EC50 values of 0.01, 0.19, and 0.17 μM for TYK2 JH2, TYK2 cells and human whole blood, respectively. ABBV-712 has anti-inflammatory activity and can be used in the research of autoimmune diseases .
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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-14166R
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FLAP
Leukotriene Receptor
PPAR
Apoptosis
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Cancer
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MK-886 (Standard) is the analytical standard of MK-886. This product is intended for research and analytical applications. 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-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-173154
-
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Molecular Glues
NEKs
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Inflammation/Immunology
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NK7-902 is a CRBN molecular glue degrader of NEK7. NK7-902 fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 leads to profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation in non-human primates by oral administration. NK7-902 shows activity in murine systems .
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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-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-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-128342
-
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Complement System
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Inflammation/Immunology
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Compound C5-IN-1 (Compound 7) is a selective allosteric inhibitor of complement component protein C5. Compound C5-IN-1 prevents C5 from being cleaved by C5 convertase, inhibits the cleavage of C5 into C5a and C5b, and thus blocks the formation of membrane attack complex (MAC). Compound C5-IN-1 has an IC50 of 0.77 μM and 5 nM in 50% human whole blood and 2% human serum to block MAC deposition induced by zymosan, respectively. Compound C5-IN-1 can be used to study diseases related to complement overactivation, such as paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS) .
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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-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-139589
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ISC-27864; GRC-27864
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PGE synthase
COX
Collagen
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Neurological Disease
Inflammation/Immunology
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Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC50 >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s ??of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases .
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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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Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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