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-N0784
    Ginkgolide B
    		Antagonist 99.96%
    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
  • HY-108634
    Apafant
    		Antagonist 99.96%
    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.
    Apafant
  • HY-112825
    TSI-01
    		Inhibitor 98.52%
    TSI-01 is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50s=0.47 versus 3.02 μM for human LPCAT2 and LPCAT1, respectively). 60 μM it is shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.
    TSI-01
  • HY-N2071
    Cedrol
    		Antagonist 99.76%
    Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
    Cedrol
  • HY-128694
    Foropafant
    		99.97%
    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.
    Foropafant
  • 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-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-109897
    CV-6209
    		98.0%
    CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats.
    CV-6209
  • HY-137257
    Carbamyl-PAF
    		Agonist 99.0%
    Carbamyl-PAF is an analog and agonist of platelet-activating factor (PAF). Carbamyl-PAF is not significantly metabolized by Raji lymphoblasts at 37°C, making it a useful tool for inflammation research. .
    Carbamyl-PAF
  • HY-114745
    MoTP
    		Antagonist 99.76%
    MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
    MoTP
  • HY-130345
    PAF (C18)
    		99.00%
    C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension.
    PAF (C18)
  • HY-101833
    YM-264
    		99.24%
    YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
    YM-264
  • HY-19121A
    TCV-309 chloride
    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.
    TCV-309 chloride
  • HY-N10663
    Kadsurenone
    		Antagonist 99.78%
    Kadsurenone is a lignan with specific antagonistic activity against platelet-activating factor. Kadsurenone can be derived from the stem of Piper kadsura.
    Kadsurenone
  • HY-P2606
    Antiflammin 2
    		Inhibitor 99.50%
    Antiflammin 2 inhibits the synthesis of platelet-activating factor (PAF) with the IC50 of 100 nM.
    Antiflammin 2
  • HY-N7343
    Pregomisin
    		Antagonist 99.87%
    Pregomisin is a natural compound isolated from the fruits of Schizandra chinensis Baill. Pregomisin showed PAF antagonistic activity and the IC50 values were 48 μM.
    Pregomisin
  • HY-141581
    Lyso-PAF C-18
    		99.7%
    Lyso-PAF C-18 is an intermediate for the synthesis of C18-PAF (HY-130345). It has an easily substituted "Lyso-PAF" structure and is easy to purify and has high yield. C18-PAF is a ligand for platelet-activating factor and PAF G protein-coupled receptor (PAFR) and has renovasodilator properties and antihypertensive lipid properties.
    Lyso-PAF C-18
  • HY-N1717
    2-Acetylbenzoic acid
    		Inhibitor 99.87%
    2-Acetylbenzoic acid, a Benzoic acid (HY-N0216) derivative, is a weak platelet aggregation inhibitor. 2-Acetylbenzoic acid inhibits Adenosine 5'-diphosphate (ADP, HY-W010918)-induced platelet aggregation.
    2-Acetylbenzoic acid
  • HY-163101
    CP-96021
    		Antagonist 98.04%
    CP-96021 is a potent and orally available leukotriene D4 (LTD4 Ki=34 μM) / platelet activating factor (PAF Ki=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and GABA receptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma.
    CP-96021
Cat. No. Product Name / Synonyms Application Reactivity