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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(34)

Melanocortin Receptor

Neuropeptide FF Receptor

(9)

Neuropeptide W

(3)

Neuropeptide Y Receptor

Prostaglandin Receptor

(434)

Protease-activated Receptor

Succinate Receptor 1 (SUCNR1)

PAFR

The platelet-activating factor receptor is a G-protein coupled receptor which binds platelet-activating factor. The PAF receptor shows structural characteristics of the rhodopsin (MIM 180380) gene family and binds platelet-activating factor (PAF). PAF is a phospholipid (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine) that has been implicated as a mediator in diverse pathologic processes, such as allergy, asthma, septic shock, arterial thrombosis, and inflammatory processes.[supplied by OMIM][7] Its pathogenetic role in chronic kidney failure has also been reported recently.

Filter HomeSignaling PathwaysGPCR/G ProteinPAFR

48740 RP

T1015993363-11-2In house

48740 RP (RP 55779) is an antagonist of platelet-activating factor.

$375

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Niranthin

TN466050656-77-4

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

$198

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Tulopafant

T17178116289-53-3In house

Tulopafant (RP 59227) is a potent platelet-activating factor (PAF) antagonist that increases capillary patency and prolongs allograft heart survival.

$700

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(Rac)-Modipafant

T28081122956-68-7In house

(Rac)-Modipafantis an orally available and selective platelet-activating factor receptor (PAFR) antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits, and can be used to study arthritis and ischemia reperfusion (I R) in the superior mesenteric artery (SMA) of the rat.

$219

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Yangambin

TN232213060-14-5

Yangambin is a selective antagonist of the cardiovascular effects of platelet activating factor (PAF); it has hypotensive effect, which is probably due to a peripheral vasodilatation that involves, at least, the inhibition the Ca2+ influx through voltage-gated Ca2+ channels. Yangambin also has central nervous system activity.

$126

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Ginkgolide B

T275115291-77-7

Ginkgolide B (BN-52021) is a PAFR antagonist(IC50=3.6 μM) isolated from Ginkgo biloba.

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SDZ-62-434

T28740115621-95-9In house

SDZ-62-434, a platelet-activating factor inhibitor with antitumor activity, inhibits bombesin- and platelet-derived growth factor-induced DNA synthesis in quiescent Swiss 3T3 cells, making it a potential candidate for studying leukemia, human xenograft colorectal cancer, and lung cancer.

$293

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CV-6209

T27102100488-87-7In house

CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor.

$129

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Apafant

T14300105219-56-5

Apafant (WEB 2086) is a highly potent platelet activating factor (PAF) antagonist that blocks eosinophil activation and can be used to study experimental allergic conjunctivitis in guinea pigs.

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Zingiberen newsaponin

TN232991653-50-8

Zingiberen newsaponin is a steroidal saponin from Dioscorea zingiberensis.

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Scutellarein tetramethyl ether

TN12711168-42-9

Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is extracted from Siam weeds and demonstrates anti-inflammatory activity via the NF-κB pathway.

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Foropafant

T15338136468-36-5

Foropafant (SR27417) is a highly potent and selective platelet-activating factor (PAF) receptor antagonist (Ki: 57 pM). Foropafant potently inhibits the PAF-induced aggregation of rabbit and human platelets.

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Chamigrenal

T3P285519912-84-6

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

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PAF C-18

T3676374389-69-8

PAF C-18 is a naturally occurring phospholipid molecule belonging to the platelet-activating factor (PAF) family, which acts as an intercellular signaling molecule involved in platelet aggregation, vasodilatation, and inflammatory responses.PAF C-18 is involved in hemostasis and thrombosis by binding to its specific G-protein-coupled receptor (PAFR) and activating.

$126

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(-)-Denudatin B

TN383187402-88-8

(-)-Denudatin B (Denudatin B) is derived from Magnolia fargesii. (-)-Denudatin B has nonspecific antiplatelet action at high concentration by inhibiting phosphoinositides breakdown induced by collagen and thrombin.

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Compound TN1643(SC)

TN164361012-31-5

Ferulamide (4-Hydroxy-3-methoxycinnamide), a Ferulic acid derivative, shows potent inhibitory activity against arachidonic acid-induced platelet aggregation.

$185

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Rocepafant

T28607132579-32-9In house

Rocepafant (LAU8080) is a platelet-activating factor (PAF) antagonist that attenuates hypoxic-ischemic brain damage in neonatal rats.Rocepafant inhibits tumor necrosis factor-Afa-mediated cytotoxicity in mouse L929 tumor cells.

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Rupatadine

T36618158876-82-5

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

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Rupatadine Fumarate

T6242182349-12-8

Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM.

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PAF-AN-1

T14007115621-84-6In house

PAF-AN-1 is a novel potent platelet-activating factor receptor (PAF) antagonist involved in the study of anaphylactic death.

$700

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CP 96021

T10872L139401-43-7In house

CP 96021 is a group of 5-HT1 receptors and 5-HT2 receptors antagonists that have anti-inflammatory properties and are non-non-self anti-ulcer compounds for the treatment of gastrointestinal tract and respiratory asthma.

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SCH-37370

T19686117796-52-8

SCH-37370 is an effective and orally active dual antagonist of platelet-activating factor and histamine. Sch 37370 blocks the binding of [3H]pyrilamine to histamine-H1 receptors in rat brain membranes. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets (IC50 : 0.6 mM) and also competes with PAF binding to specific sites in membrane preparations from human lungs (IC50 : 1.2 mM).

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TSI-01

T24904704878-75-1

TSI-01, a pro-inflammatory phospholipid mediator, is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: LPCAT1, predominantly expressed in lungs, and LPCAT2, expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50 values of 0.47 μM and 3.02 μM for human LPCAT2 and LPCAT1, respectively). At 60 μM, it suppresses PAF biosynthesis in calcium ionophore-stimulated mouse peritoneal macrophages.

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Methylcarbamyl PAF C-16

T3620591575-58-5

Methylcarbamyl PAF C-16 (Carbamyl-PAF) is a platelet-activating factor analogue with PAF agonist properties, activating inflammation in pregnancy tissues and promoting preterm birth.

$185

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