Platelet-activating Factor Receptor (PAFR) Inhibitor

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.

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.

Antiflammin 2 inhibits the synthesis of platelet-activating factor (PAF) with the IC₅₀ of 100 nM.

Cryptomeridiol is a platelet-activating factor (PAF) receptor binding inhibitor. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH (HY-P0252)-stimulated B16 melanoma cells.

MKC-963 is an orally active and potent inhibitor targeting platelet aggregation-related pathways. MKC-963 exerts antithrombotic activity by inhibiting platelet aggregation, and can also induce autoinduction, i.e., upregulating the mRNA expression and activity of CYP3A4 enzyme to accelerate its own metabolism in vivo. MKC-963 is promising for research of platelet aggregation-related diseases (e.g., thrombosis).

(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).

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.

Rhazimine is an indole alkaloid that is a dual inhibitor of arachidonic acid metabolism and platelet activating factor-induced platelet aggregation.

WF-5239 is a fungal metabolite can be found in Aspergillus fumigatus Fresenius. WF-5239 potently inhibits platelet aggregation. WF-5239 can be used for the research of pulmonary thrombosis.

Dersalazine (UR-12746 free base) is an inhibitor of platelet-activating factor, exhibiting intestinal anti-inflammatory activity and potential efficacy in treating ulcerative colitis.

1-Cinnamoylpyrrolidine (Compound 3), a crude extract prepared from Piper caninum, is a DNA strand scission agent, induces the relaxation of supercoiled pBR322 plasmid DNA. 1-Cinnamoylpyrrolidine (Compound 4) inhibits platelet aggregation induced by PAF with an IC₅₀ of 37.3 μM.

CV 3988 is a specific inhibitor of platelet-activating factor (PAF).

Piperulin A is a potent inhibitor of PAFR. Piperulin A inhibits the specific binding of PAFR on isolated rabbit platelet plasma membranes with an IC₅₀ of 7.3 μM.

Pinusolidic acid is a platelet-activating factor (PAF) inhibitor with an IC₅₀ of 23 μM.

Aggreceride A is a platelet aggregation inhibitor. Aggreceride A shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen.

Aggreceride B is a platelet aggregation inhibitor. Aggreceride B shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen.

Aggreceride C is a platelet aggregation inhibitor. Aggreceride C shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen.