human platelet

TAK-024 is an inhibitor of platelet(IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively).

Platelet Factor 4 (58-70), human, is a polypeptide comprising the 58-70 amino acid sequence of Platelet Factor 4 (PF-4) residues.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

FR183998 free base is an inhibitor of Na+/Ca2+ Exchanger.

Fradafiban binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM. Fradafiban is a non-polypeptide platelet glycoprotein IIb/IIIa antagonist.

BI-9627 is a selective and potent sodium hydrogen exchange isomer 1 (NHE1) inhibitor.BI-9627 partially reverses the effects of DMA with IC50 values of 6 and 31 nM in the intracellular pH recovery (pHi) and human platelet lysis assays.BI-9627 is often used as a negative control for BI-0054, which can be used for the study of ischemia-reperfusion injury in isolated hearts. BI-9627 is often used as a negative control for BI-0054 and can be used to study ischemia-reperfusion injury in isolated hearts.

Calpeptin is a cell-permeable Calpain inhibitor (IC50 = 5 nM), and its ID50 value for human platelet Calpain I is 40 nM. Calpeptin is also an effective inhibitor of Cathepsin K (IC50 = 0.11 nM).

Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.

Furegrelate sodium (U-63557A) is a selective thromboxane synthase inhibitor with oral activity. Furegrelate sodium(U-63557A) inhibits thromboxane A2 (TXA2) synthase in human platelet microsomes with an IC50 of 15 nM.

Cerebrocrast (IOS-11212) is an anti-inflammatory and hypoglycemic activity that promotes H+ and Cl- cotransport in rat liver mitochondria, blocks human platelet activation, and can be used to study diabetes.

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.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba/F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

BIRM 271 is a novel arachidonic acid release inhibitor that blocks leukotriene B4 and platelet-activating factor biosynthesis in human neutrophils. BIRM 271 and BIRM 270 are enantiomers that inhibit the production of leukotriene B4 with IC50 of 40 nM.

PF-03049423 is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of approximately 0.2 nM for rat and human thrombomodulin. PF-03049423 can be used in studies about acute ischemic stroke studies.

Methyl acetylsalicylate (ACETYLSALICYLIC ACID METHYL ESTER) is a natural product isolated from Pisum sativum. Inhibition of collagen-induced human platelet rich plasma aggregation

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).

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.

Parmodulin 2 (ML 161) is the inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50: 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). It also inhibits thrombin-induced platelet activation.

PAR4 antagonist8 (Compound 20f) is an effective oral and selective PAR4 antagonist with an IC50 of 15.32 nM, boasting favorable pharmacokinetic properties. It effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50=6.39 nM) and also suppresses platelet aggregation in mice. PAR4 antagonist8 is utilized in anti-thrombotic research.

(E/Z)-Ozagrel (sodium) [(E/Z)-OKY-046 (sodium)] is a mixture of the EZ isomers of Ozagrel (sodium). It acts as a thromboxane A2 (TXA2) synthase inhibitor. As an antiplatelet agent, Ozagrel (sodium) selectively inhibits human platelet aggregation, with an IC50 of 53.12 μM.

KUM 32 is a potent antagonist of adrenaline-induced platelet aggregation. It acts as an inhibitor of adenylate cyclase activity and binds to the alpha 2-adrenergic receptor on human platelets.

ADP-β-S (trisodium) is an analog of ADP and acts as a partial agonist. It can induce human platelet aggregation and inhibit PGE1-stimulated adenylate cyclase.

2-MeSADP (2-Methylthioadenosine diphosphate; 2-Methylthio-ADP) is a potent agonist of purinergic (P2Y) receptors, displaying EC50 values of 19 nM for human P2Y13, 6.2 nM for mouse P2Y13, and 5 nM for human P2Y12. It also has pEC50 values of 8.29 for human P2Y1 and 5.75 for rat P2Y6. 2-MeSADP induces platelet aggregation and morphological changes, while inhibiting the accumulation of cyclic adenosine monophosphate in platelets in the presence of prostaglandin E1.

7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. This compound inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. It disrupts PAR4-mediated aggregation and related signaling pathways, including NF-κB, Ca2+/protein kinase C (PKC), Akt, ERK, and p38. In a streptozotocin (STZ)-induced diabetic mouse model, 7,4'-Dimethoxy-3-hydroxyflavone inhibits vascular PAR4 expression, improves endothelial dysfunction, and reduces oxidative stress. Additionally, it prevents thrombosis in mice without affecting bleeding time.