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
    		99.96%
    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
    Apafant
  • HY-N2071
    Cedrol
    		Antagonist ≥98.0%
    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-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-112825
    TSI-01
    		Inhibitor 98.31%
    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-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-132210
    rel-(2R,4R)-2,4-Bis(3,4,5-trimethoxyphenyl)-1,3-dioxolane
    		Antagonist
    rel-(2R,4R)-2,4-Bis(3,4,5-trimethoxyphenyl)-1,3-dioxolane (compound 6) is a platelet-activating factor receptor (PAFR) antagonist with a Ki of 0.3 µM.
    rel-(2R,4R)-2,4-Bis(3,4,5-trimethoxyphenyl)-1,3-dioxolane
  • HY-153717
    LAU-0901
    		Antagonist
    LAU-0901, a PAF receptor antagonist, possesses highly neuroprotective activity. LAU-0901 inhibits apoptosis.
    LAU-0901
  • 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-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 ≥99.0%
    Kadsurenone
  • HY-101833
    YM-264
    		98.39%
    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-N7343
    Pregomisin
    		Antagonist 98.74%
    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-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
  • 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-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-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-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-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
Cat. No. Product Name / Synonyms Application Reactivity