platelets

Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.

Atopaxar, a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

Cycloolivil (Isoolivil) is a natural polyphenolic compound found in olive trees that exhibits significant radical scavenging and antioxidant activities. It may prevent thrombotic complications associated with platelet hyperaggregability and serve as a foundational compound for further research.

Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

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.

Megakaryocytes/platelets inducing agent being useful in treating diseases involving thrombopenia. Megakaryocytes/platelets inducing agent is an inducing agent for megakaryocytes and/or platelets from pluripotent stem cells.

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).

Timegadine is a competitive inhibitor of COX and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates and in washed rabbit platelets.

RHC 80267 (U-57908) is a selective inhibitor of DAGL, with an IC50 of 4 μM in canine platelets.

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.

BIX HCl is a sodium-hydrogen exchange type 1 inhibitor.

Aglafoline inhibits in a concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.

Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog that preferentially activates cGMP-dependent protein kinase (PKG). It inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma thrombin and can induce peripheral analgesia by activating ATP-sensitive K+ channels.

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM. Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

Zoniporide hydrochloride is a selective inhibitor of NHE-1 with IC50 of 14 nM which is >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride shows an IC50 of 59 nM for NHE-1-dependent swelling of human platelets.

(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.

Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) , a selective, high-affinity P2Y12 receptor antagonist, suppressess fibrinogen binding to platelets and platelet adhesion and aggregation.

Carbazochrome (Adchnon) is an antihemorrhagic, or hemostatic, agent that will cease blood flow by causing the aggregation and adhesion of platelets in the blood to form a platelet plug, ceasing blood flow from an open wound. It is hoped that this drug can be used in the future for preventing excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on its effectiveness and the severity of possible side effects remains to be fairly inconclusive. Carbazochrome has been investigated for use in the treatment of hemorrhoids in a mixture with troxerutin.

Elaidic acid (trans-Oleic Acid) is the 9-trans isomer of oleic acid. It is a monounsaturated trans-fatty acid which can be found in partially hydrogenated cooking oils. In human platelets incubated with arachidonic acid, elaidic acid inhibits HHT and HETE formation while inducing prostaglandin and thromboxane synthesis.

Chlorobutanol hemihydrate (Chlorbutol hemihydrate) is an orally toxic preservative with antimicrobial activity that inhibits Gram-positive and Gram-negative bacteria and fungi, inhibits the aggregation and release of human platelets in vitro, and is commonly used in cosmetics.

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).