Platelet-activating Factor Receptor (PAFR) Antagonist

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.

Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a K_i 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.

PAF antagonist-1 is a platelet activating factor (PAF) receptor antagonist with a target K_i of 69 nM. PAF antagonist-1 inhibits PAF binding and displays enhanced affinity at A₁, A₂^a, and A₃ adenosine receptor subtypes compared to related dihydropyridine analogs with smaller ester groups. PAF antagonist-1 can be used for cardiovascular disorders, especially hypertension and coronary heart disease.

MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.

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.

Kadsurenone is a lignan with specific antagonistic activity against platelet-activating factor. Kadsurenone can be derived from the stem of Piper kadsura.

Hexanolamino PAF C-16 (1-O-hexadecyl-2-acetyl-sn-glycero-3-phospho (N,N,N trimethyl) hexanolamine) is a Platelet-activating Factor Receptor (PAFR) Modulator with partial agonist activity. Hexanolamino PAF C-16 induces platelet aggregation and macrophage production but fails to increase [Ca2+]i in platelets, suggesting that PAF receptors may interact with PAF receptors through Ca²⁺-dependent and -independent pathways. Related to platelet aggregation.

CP-96021 is an orally active dual leukotriene D4 (LTD4) and platelet activating factor (PAF) receptor antagonist, featuring a guinea pig LTD4 receptor K_i of 34 nM and a rabbit PAF receptor K_i 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.

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.

Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC₅₀ of 29.7 μM and a K_i of 17.1 μM against human UGT1A1, and an IC₅₀ of 56.5 μM and a K_i 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.

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.

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.

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.

Clotizolam is a thienobenzodiazepine derivative that has antagonistic activity against platelet-activating factor (PAF). Clotizolam possesses sedative, anxiolytic, anticonvulsant,and muscle relaxant effects.

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 K_i of 5.4 μM (Histamine H₁ receptor binding). Sch-40338 can be used for the study of allergic disease.

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.

BN 52115, a platelet-activating factor antagonist, has demonstrated the ability to mitigate bronchopulmonary changes in vivo.

Selenotifen (BN 52256) is an antiallergic agent. Selenotifen is a highly potent antagonist to PAF receptors. Selenotifen exhibits a statistically significant antiarrhythmic effect.

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.

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).