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-163101
    CP-96021
    		Antagonist 98.04%
    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.
    CP-96021
  • HY-N0784R
    Ginkgolide B (Standard)
    		Antagonist
    Ginkgolide B (Standard) is the analytical standard of Ginkgolide B. This product is intended for research and analytical applications. Ginkgolide B (BN-52021), a terpene lactone, is a potent platelet activating factor antagonist. Ginkgolide B protects endothelial cells via the activation of PXR from injuries induced by xeno- and endobiotics. Ginkgolide B can pass through the brain-blood barrier. Ginkgolide B has anti-oxidant, anti-inflammatory, anti-tumor, and anti-apoptotic activity. Ginkgolide B has marked neuroprotective effects against ischemia-induced impairments.
    Ginkgolide B (Standard)
  • HY-115702S
    1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine-d4
    		Agonist ≥99.0%
    1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine-d4 ((Rac)-PAF (C16)-d4) is the deuterium labeled 1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine. 1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine is an endogenous inflammatory lipid mediator. 1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine acts as a high-affinity agonist for PAFR (GPCR), inducing platelet aggregation, vascular permeability, and leukocyte chemotaxis at extremely low concentrations. 1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine exerts its effects via cell surface receptors to regulate inflammation.
    1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine-d<sub>4</sub>
  • HY-N8218
    Homoeriodictyol 7-O-β-D-glucoside
    		99.84%
    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-N4267
    Yangambin
    		Antagonist 98.27%
    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 Ca2+ 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.
    Yangambin
  • HY-134101
    2-O-Ethyl PAF C-16
    		99.9%
    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-W040221
    Butanoyl PAF
    		Agonist
    Butanoyl PAF, a compound closely related to Azelaoyl PC (HY-134154), maintains over 10% of the agonist potency of platelet-activating factor (PAF). Butanoyl PAF's concentration in oxidized low-density lipoprotein surpasses that of enzymatically generated PAF by more than 100-fold.
    Butanoyl PAF
  • HY-N12995
    α-Bulnesene
    		Antagonist
    α-Bulnesene is a novel PAF receptor antagonist with the IC50 of 17.62 μM. α-Bulnesene can be isolated from Pogostemon cablin. α-Bulnesene shows inhibitory effect on platelet-activating factor and arachidonic acid induced rabbit platelet aggregation.
    α-Bulnesene
  • HY-108908A
    Modipafant
    Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.
    Modipafant
  • HY-108634S
    Apafant-d8
    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.
    Apafant-d<sub>8</sub>
  • HY-106899
    MK 287
    		Antagonist
    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.
    MK 287
  • HY-106924
    DF-1111301
    DF 1111301 is a new antiallergic compound endowed of antihistamine-H1 and anti-PAF activities.
    DF-1111301
  • HY-19126
    CL-184005
    		Antagonist
    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.
    CL-184005
  • HY-171253
    Clotizolam
    		Antagonist
    Clotizolam is a thienobenzodiazepine derivative that has antagonistic activity against platelet-activating factor (PAF). Clotizolam possesses sedative, anxiolytic, anticonvulsant,and muscle relaxant effects.
    Clotizolam
  • HY-116435
    Sch-40338
    		Antagonist
    Sch-40338 is a dual antagonist of platelet-activating factor (PAF) and histamine with an IC50 of 0.59 μM (PAF-induced platelet aggregation) and a Ki of 5.4 μM (Histamine H₁ receptor binding). Sch-40338 can be used for the study of allergic disease.
    Sch-40338
  • HY-N3436
    Kadsurin A
    		Antagonist
    Kadsurin A is a new lignan can be isolated from Piper futokadsura. Kadsurin A is a platelet activating factor (PAF) receptor antagonist that weakly inhibits the binding of PAF to its receptor.
    Kadsurin A
  • HY-136791
    BN52115
    		Antagonist
    BN 52115, a platelet-activating factor antagonist, has demonstrated the ability to mitigate bronchopulmonary changes in vivo.
    BN52115
  • HY-106833
    SDZ-62-434 free base
    		Antagonist
    SDZ-62-434 free base is a platelet-activating factor (PAF) antagonist. SDZ-62-434 free base has antiproliferative activity in human solid and haematological malignancies.
    SDZ-62-434 free base
  • HY-121377
    Epiyangambin
    		Antagonist
    Epiyangambin is a competitive platelet activating factor receptor (PAF) antagonist that dose-dependently inhibits PAF-induced platelet aggregation. Epiyangambin also inhibits the growth of human colon cancer cells (SW480 cells).
    Epiyangambin
  • HY-19125
    BN-50726
    		Antagonist
    BN-50726 is a potent platelet-activating factor (PAF) receptor antagonist. BN-50726 inhibits PAF-induced effects (e.g., [3H]-serotonin release and hypotension) (IC50=5.40 nM). BN-50726 is promising for research of PAF-mediated pathological processes (e.g., inflammation, anaphylaxis, hypotension).
    BN-50726
Cat. No. Product Name / Synonyms Application Reactivity