2. Signaling Pathways
  3. GPCR/G Protein
  4. Platelet-activating Factor Receptor (PAFR)

Platelet-activating Factor Receptor (PAFR)

The platelet-activating factor receptor (PAFR) is a G-protein-coupled receptor involved in both normal physiological and numerous pathophysiological processes. PAFR responds to platelet-activating factor (PAF), a phospholipid mediator of cell-to-cell communication that exhibits diverse physiological effects. Stimulation of the PAFR via binding of platelet-activating factor (PAF) elicits diverse and potent biological activities and plays a profound role in acute inflammation, allergic disorders, endotoxic shock, and anaphylaxis. PAF is a potent and versatile mediator of inflammation that is produced by numerous cell types and tissues, and particularly by leukocytes.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W700638A
    Benafentrine maleate
    		Antagonist
    Benafentrine maleate is a platelet activating factor receptor (PAFR) antagonist and a PDE 4 inhibitor.
    Benafentrine maleate
  • HY-117811
    (R,R)-MK 287
    		Inhibitor
    (R,R)-MK 287 (L-680574) is a tetrahydrofuran derivative that potently inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with Ki values of 6.1, 3.2, and 5.49 nM, respectively. (R,R)-MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50=56 nM) and elastase release from PMNs (ED50=4.4 nM). (R,R)-MK 287 inhibits PAF-induced lethality in mice (ED50=0.8 mg/kg, po) and PAF-induced bronchospasm in guinea pigs (ED50=0.18 mg/kg).
    (R,R)-MK 287
  • HY-106837
    Israpafant
    		Antagonist
    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 Ca2+ influx and intracellular Ca2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice.
    Israpafant
  • HY-N9300
    1,6-Dihydro-4,7-epoxy-1-methoxy-3,4-methylenedioxy-6-oxo-3,8-lignan
    		Inhibitor
    1,6-Dihydro-4,7-epoxy-1-methoxy-3,4-methylenedioxy-6-oxo-3,8-lignan, a lignan derivative from the ethyl acetate soluble fraction of twigs of Magnolia denudate (Magnoliaceae), exhibits anti-platelet-activating factor (PAF) activity. PAF is a potent lipid mediator in inflammation and asthma.
    1,6-Dihydro-4,7-epoxy-1-methoxy-3,4-methylenedioxy-6-oxo-3,8-lignan
  • HY-118779
    Rhazimine
    		Inhibitor
    Rhazimine is an indole alkaloid that is a dual inhibitor of arachidonic acid metabolism and platelet activating factor-induced platelet aggregation.
    Rhazimine
  • HY-N12707
    Kadsurenin C
    		Antagonist
    Kadsurenin C (compound 1) is a neolignan that can be isolated from the aerial part of Piper kadsura with anti-inflammation activity. Kadsurenin C exhibits significant PAF (Platelet Activating Factor) antagonistic activity with IC50 value of 5.1 μM.
    Kadsurenin C
  • HY-141612
    Pyrrolidino PAF C-16
    		Activator
    Pyrrolidino PAF C-16 is a platelet activating factor ( PAF ) analogue that has hypohematic effects.
    Pyrrolidino PAF C-16
  • HY-101654
    Rocepafant
    		Antagonist
    Rocepafant (BN 50730) is a specific platelet activating factor (PAF) antagonist. Rocepafant can be used in rheumatoid arthritis and nervous system research.
    Rocepafant
  • HY-N8218
    Homoeriodictyol 7-O-β-D-glucoside
    Homoeriodictyol 7-O-β-D-glucoside is a natural platelet-activating factor (PAF) antagonist. Homoeriodictyol 7-O-β-D-glucoside inhibits human and rabbit platelet aggregation induced by PAF, with an IC50 of 0.8 μM.
    Homoeriodictyol 7-O-β-D-glucoside
  • HY-105198
    Lexipafant
    Lexipafant is a platelet-activating factor (PAF) antagonist that inhibits the inflammatory response and is used in the research of acute pancreatitis.
    Lexipafant
  • HY-121394
    L-659,989
    		Agonist
    L-659,989 is an orally active, extremely potent, selective and competitive platelet activating factor (PAF) receptor antagonist.
    L-659,989
  • HY-106899A
    (rel)-MK 287
    		Control
    (rel)-MK 287 ((rel)-L-680573) is a relative configuration of MK 287. MK 287, a tetrahydrofuran analog, potently inhibited [3H]C18-PAF binding to human platelet, polymorphonuclear leukocyte (PMN) and lung membranes with Kis of 6.1 nM, 3.2 nM and 5.49 nM, respectively. MK 287 inhibits PAF-induced lethality in mice and PAF-induced bronchoconstriction in guinea pigs.
    (rel)-MK 287
  • HY-10164
    E-​6123
    E-6123 is a platelet-activating factor (PAF) receptor antagonist.
    E-​6123
  • HY-121007
    Bepafant
    		Antagonist
    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.
    Bepafant
  • HY-101675
    Setipafant
    Setipafant is a platelet-activating factor (PAF) antagonist.
    Setipafant
  • HY-106833A
    SDZ-62-434
    		Antagonist
    SDZ-62-434 is a platelet-activating factor (PAF) antagonist. SDZ-62-434 has antiproliferative activity in human solid and haematological malignancies.
    SDZ-62-434
  • HY-118019
    Scandenolide
    Scandenolide is a sesquiterpene lactone that can be found in Philippines medicinal plant Mikania cordata. Scandenolide inhibits leukotriene and platelet activating factor synthesis in leukocytes.
    Scandenolide
  • HY-134101
    2-O-Ethyl PAF C-16
    2-O-Ethyl PAF C-16 is a homolog of PAF and a competitive ligand for PAF receptor (Platelet-activating Factor Receptor (PAFR)). 2-O-Ethyl PAF C-16 inhibits the binding of the PAF antagonist WEB 2086 (HY-108634) to the PAF receptor with an IC50 of 21 nM.
    2-O-Ethyl PAF C-16
  • HY-126551
    Butenoyl-PAF
    		Agonist
    Butenoyl-PAF is a phospholipid analog of platelet activating factor (PAF-like) that is generated in oxidized low-density lipoprotein (DLDR). Butenoyl-PAF can activate cells that express human PAF receptors, such as neutrophils, monocytes, and platelets, and it stimulates an increase in intracellular calcium ion concentration.
    Butenoyl-PAF
  • HY-167719
    Dersalazine
    		Inhibitor
    Dersalazine (UR-12746 free base) is an inhibitor of platelet-activating factor, exhibiting intestinal anti-inflammatory activity and potential efficacy in treating ulcerative colitis.
    Dersalazine
Cat. No. Product Name / Synonyms Application Reactivity