Search Result
Results for "
PAF antagonist
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13511A
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UR-12592 Fumarate
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Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria .
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- HY-108634
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Apafant
3 Publications Verification
WEB 2086
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Platelet-activating Factor Receptor (PAFR)
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Inflammation/Immunology
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Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit .
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- HY-13511
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UR-12592
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Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria .
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- HY-109897
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- HY-128694
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SR27417
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Platelet-activating Factor Receptor (PAFR)
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Cardiovascular Disease
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Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets .
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- HY-19121A
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Platelet-activating Factor Receptor (PAFR)
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Cancer
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TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock .
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- HY-N7343
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- HY-13511AR
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UR-12592 Fumarate (Standard)
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Reference Standards
Histamine Receptor
Autophagy
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Inflammation/Immunology
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Rupatadine (Fumarate) (Standard) is the analytical standard of Rupatadine (Fumarate). This product is intended for research and analytical applications. Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria .
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- HY-N4267
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Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
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Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
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- HY-105198
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- HY-101833
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- HY-108908A
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- HY-121007
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Web2170
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Platelet-activating Factor Receptor (PAFR)
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Others
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Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guinea pigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
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- HY-U00040
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- HY-19125
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- HY-N8218
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- HY-116120
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- HY-106833
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- HY-101731
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Leukotriene Receptor
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Inflammation/Immunology
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CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Ki values of 34 nM and 37 nM, respectively .
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- HY-106899
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Platelet-activating Factor Receptor (PAFR)
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Cardiovascular Disease
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MK 287 is a potent, selective and orally active antagonist of platelet-activating factor receptor (PAFR). MK 287 can inhibit [3H]C18-PAF binding to human platelet, polymorphonuclear leukocyte (PMN) and lung membranes with K1 values of 6.1, 3.2, and 5.49 nM, respectively. MK 287 can inhibit PAF-induced aggregation of platelets in plasma or gel-filtered platelets and elastase release from PMNs with ED50 values of 56, 1.5 and 4.4 nM. MK 287 can be used for the research of cardiovascular disease, such as thrombosis .
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- HY-N11920
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- HY-N12995
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- HY-A0300
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EMD 270179
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Integrin
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Cardiovascular Disease
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Cyclopeptide-5 (EMD 270179) is an αvβ3 antagonist that can improve PAF-induced increased adhesion of sickle red blood cells, capillary post-obstruction, and enhance blood flow dynamics. Cyclopeptide-5 also has cytotoxic effects .
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- HY-19097
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Platelet-activating Factor Receptor (PAFR)
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Cardiovascular Disease
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Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action. Ro-24-4736 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-123397
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- HY-101235
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Prostaglandin Receptor
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Cardiovascular Disease
Inflammation/Immunology
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ICI 185282 is a potent, selective, orally active thromboxane A2 (TXA₂) receptor antagonist. ICI 185282 causes dose-dependent inhibition of U-46619 (HY-108566)-induced platelet aggregation ex-vivo in guinea-pig. ICI 185,282 inhibits bronchospasm induced by U-46619, PGD2 (HY-101988), PGF2α (HY-12956), arachidonic acid (HY-109590), LTD4 and PAF (HY-108635) in vivo. ICI 185282 can be used for bronchial asthma research .
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- HY-105790
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Pipethanate
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Cholinesterase (ChE)
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Cardiovascular Disease
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Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates .
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- HY-171253
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- HY-182583
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Platelet-activating Factor Receptor (PAFR)
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Cardiovascular Disease
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PAF antagonist-1 is a platelet activating factor (PAF) receptor antagonist with a target Ki of 69 nM. PAF antagonist-1 inhibits PAF binding and displays enhanced affinity at A1, A2 a, and A3 adenosine receptor subtypes compared to related dihydropyridine analogs with smaller ester groups. PAF antagonist-1 can be used for cardiovascular disorders, especially hypertension and coronary heart disease .
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- HY-134101
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- HY-101594
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- HY-101675
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- HY-19084
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- HY-N3436
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- HY-10164
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- HY-108634S
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WEB 2086-d8
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Isotope-Labeled Compounds
Platelet-activating Factor Receptor (PAFR)
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Inflammation/Immunology
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Apafant-d8 is the deuterium labeled Apafant. Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Kiof 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit .
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- HY-122126
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- HY-100153
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- HY-121377
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- HY-125309
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Platelet-activating Factor Receptor (PAFR)
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Others
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ABT-299 is a prodrug of a platelet-activating factor (PAF) antagonist that exhibits significant inhibitory activity on PAF-induced β-platelet globulin release in vitro after in vivo administration in humans, an effect that may be partially attributed to the pyridine-N-oxide metabolite.
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- HY-124887
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- HY-153717
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- HY-121394
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- HY-101654
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- HY-19205A
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LDP-392
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Lipoxygenase
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Inflammation/Immunology
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CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
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- HY-19126
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Platelet-activating Factor Receptor (PAFR)
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Infection
Cardiovascular Disease
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CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
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- HY-106833A
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- HY-123505
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- HY-100316
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- HY-133003
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- HY-117636
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- HY-19121
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- HY-163101
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Platelet-activating Factor Receptor (PAFR)
Leukotriene Receptor
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Inflammation/Immunology
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CP-96021 is an orally active dual leukotriene D4 (LTD4) and platelet activating factor (PAF) receptor antagonist, featuring a guinea pig LTD4 receptor Ki of 34 nM and a rabbit PAF receptor Ki of 37 nM. CP-96021 blocks ligand binding to its target receptors, inhibits ligand-induced bronchoconstriction, and inhibits antigen-triggered airway obstructive effects. CP-96021 can be used for the research of asthma .
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- HY-106837
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Y 24180
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Platelet-activating Factor Receptor (PAFR)
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Inflammation/Immunology
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Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca 2+ influx and intracellular Ca 2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice .
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- HY-N12707
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- HY-106899A
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(rel)-L-680573
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Platelet-activating Factor Receptor (PAFR)
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Others
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(rel)-MK 287 ((rel)-L-680573) is a relative configuration of MK 287. MK 287 is a potent, selective and orally active antagonist of platelet-activating factor receptor (PAFR). MK 287 can inhibit [3H]C18-PAF binding to human platelet, polymorphonuclear leukocyte (PMN) and lung membranes with K1 values of 6.1, 3.2, and 5.49 nM, respectively. MK 287 can inhibit PAF-induced aggregation of platelets in plasma or gel-filtered platelets and elastase release from PMNs with ED50 values of 56, 1.5 and 4.4 nM. MK 287 can be used for the research of cardiovascular disease, such as thrombosis .
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- HY-13511AS
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- HY-176466
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Platelet-activating Factor Receptor (PAFR)
TNF Receptor
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Inflammation/Immunology
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ST-899 is a novel platelet-activating factor (PAF) receptor antagonist. ST-899 can significantly reduce the mortality of mice with endotoxin (LPS)-induced shock. ST-899 can significantly inhibit the increase in serum tumor necrosis factor (TNF) levels induced by LPS, but has no effect on interleukin-6 (IL-6). The regulatory mechanism of ST-899 is to block the positive feedback loop between PAF and TNF, thereby reducing the inflammatory response. ST-899 can be used to study inflammatory diseases such as septic shock .
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- HY-13511R
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UR-12592 (Standard)
|
Reference Standards
Histamine Receptor
Autophagy
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Inflammation/Immunology
|
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Rupatadine (Standard) is the analytical standard of Rupatadine. This product is intended for research and analytical applications. Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria .
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- HY-13511S
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UR-12592-d6
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Histamine Receptor
Isotope-Labeled Compounds
Autophagy
|
Inflammation/Immunology
|
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Rupatadine-d6 (D-tartrate) is deuterated labeled Rupatadine (HY-13511). Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria .
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- HY-119035
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Platelet-activating Factor Receptor (PAFR)
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Inflammation/Immunology
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R-75317 is a specific platelet-activating factor (PAF) antagonist. R-75317 can prevent the decline in creatinine clearance (Ccr) in a rat model of glomerulonephritis induced by the injection of antibodies extracted from rabbits against rat glomerular basement membrane (GBM) antigens, delay the onset of proteinuria, and improve glomerular hypertrophy, mesangial matrix proliferation, and interstitial fibrosis. R-75317 may be useful in the study of glomerulonephritis .
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- HY-N3055
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Apoptosis
AMPK
Platelet-activating Factor Receptor (PAFR)
Caspase
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Neurological Disease
Metabolic Disease
Cancer
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Pinusolide is an AMPK activator and PAF receptor antagonist. Pinusolide activates AMPK, phosphorylates ACC, enhances IRS-1 tyrosine phosphorylation, boosts glucose uptake, and modulates insulin signaling. Pinusolide inhibits caspase-3/7 activation, intracellular calcium elevation, reactive oxygen species overproduction, lipid peroxidation, and tumor cell proliferation. Pinusolide stabilizes superoxide dismutase activity, reduces apoptotic hallmarks, induces mitochondrial pathway apoptosis, and triggers DNA fragmentation. Pinusolide can be used for the research of type 2 diabetes, neurodegenerative diseases, acute lymphoblastic leukemia, acute myeloid leukemia, and Burkitt lymphoma .
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- HY-105790A
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Cholinesterase (ChE)
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Cardiovascular Disease
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Piperilate (Pipethanate) hydrochloride is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate hydrochloride also causes hypotension and rescues mice poisoned by the organophosphates .
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- HY-182418
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Platelet-activating Factor Receptor (PAFR)
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Cardiovascular Disease
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UR-11353 is a selective platelet activating factor (PAF) antagonist with long-lasting activity. UR-11353 inhibits PAF-induced platelet aggregation in rabbit platelet-rich plasma. UR-11353 inhibits PAF-induced hypotension in normotensive rats. UR-11353 protects against PAF-induced mortality in mice .
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- HY-108634R
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WEB 2086 (Standard)
|
Reference Standards
Platelet-activating Factor Receptor (PAFR)
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Inflammation/Immunology
|
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Apafant (Standard) is the analytical standard of Apafant (HY-108634). This product is intended for research and analytical applications. Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit .
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- HY-116435
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- HY-19099
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- HY-182625
-
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Platelet-activating Factor Receptor (PAFR)
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Others
Inflammation/Immunology
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GS-1160-180 is a PAF receptor antagonist. GS-1160-180 competes with PAF for receptor binding, with no activity against collagen or adenosine diphosphate-induced platelet aggregation. GS-1160-180 can be used for research on asthma, anaphylactic shock, gastric ulceration, and transplant rejection .
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- HY-116481
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- HY-101833R
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- HY-180341
-
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Platelet-activating Factor Receptor (PAFR)
|
Inflammation/Immunology
|
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UR-12633 is a platelet-activating factor (PAF) antagonist. UR-12633 can effectively reverse hypotension, inhibit coagulation abnormalities, increased vascular permeability, and metabolic disorders in rodent models of endotoxic shock. UR-12633 can be used for research on endotoxic shock .
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- HY-182434
-
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Phosphatase
FAP
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Inflammation/Immunology
|
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CL 118326 is a potent, selective, competitive inhibitor of mammalian pancreatic phospholipase A2 (PLA2) and a weak antagonist of platelet-activating factor receptor (PAF receptor). CL 118326 competitively inhibits mammalian pancreatic PLA2 (porcine: IC50 = 1.55 μg/mL), and shows no activity against snake venom or bee venom PLA2. CL 118326 inhibits PAF-induced and thrombin-induced platelet aggregation, as well as the release of leukotriene (LTC4) and histamine from basophil-enriched leukocytes. CL 118326 can be used for research on inflammation and allergic reactions .
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- HY-19175
-
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FR-144633
|
Thrombin
Integrin
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Cardiovascular Disease
|
|
FK 633 (FR-144633) is a fibrinogen inhibitor and peptide mimetic GPⅡbⅡa receptor antagonist. FK 633 has anti-platelet and anti-thrombotic effects. FK 633 inhibits ADP-, collagen-, thrombin-, and PAF-induced platelet aggregation with IC50 values of 103, 87, 98, and 239 nM, respectively .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-A0300
-
|
EMD 270179
|
Integrin
|
Cardiovascular Disease
|
|
Cyclopeptide-5 (EMD 270179) is an αvβ3 antagonist that can improve PAF-induced increased adhesion of sickle red blood cells, capillary post-obstruction, and enhance blood flow dynamics. Cyclopeptide-5 also has cytotoxic effects .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N7343
-
-
-
- HY-N4267
-
|
|
Cardiovascular Disease
Structural Classification
other families
Classification of Application Fields
Lignans
Phenylpropanoids
Plants
Disease Research Fields
Source Classification
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
|
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
|
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- HY-N8218
-
-
-
- HY-N11920
-
-
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- HY-N12995
-
-
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- HY-N3436
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-
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- HY-121377
-
-
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- HY-N12707
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-
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- HY-N3055
-
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|
Cupressaceae
Classification of Application Fields
Terpenoids
Diterpenoids
Plants
Disease Research Fields
Calocedrus decurrens (Torr.) Florin
Source Classification
Cancer
|
Apoptosis
AMPK
Platelet-activating Factor Receptor (PAFR)
Caspase
|
|
Pinusolide is an AMPK activator and PAF receptor antagonist. Pinusolide activates AMPK, phosphorylates ACC, enhances IRS-1 tyrosine phosphorylation, boosts glucose uptake, and modulates insulin signaling. Pinusolide inhibits caspase-3/7 activation, intracellular calcium elevation, reactive oxygen species overproduction, lipid peroxidation, and tumor cell proliferation. Pinusolide stabilizes superoxide dismutase activity, reduces apoptotic hallmarks, induces mitochondrial pathway apoptosis, and triggers DNA fragmentation. Pinusolide can be used for the research of type 2 diabetes, neurodegenerative diseases, acute lymphoblastic leukemia, acute myeloid leukemia, and Burkitt lymphoma .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-108634S
-
|
|
|
Apafant-d8 is the deuterium labeled Apafant. Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Kiof 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit .
|
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- HY-13511AS
-
|
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Rupatadine-d4 fumarate is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki values of 0.55/0.1 μM (rabbit platelet membranes/guinea pig cerebellum membranes) .
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- HY-13511S
-
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Rupatadine-d6 (D-tartrate) is deuterated labeled Rupatadine (HY-13511). Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria .
|
-
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