antiplatelet aggregation

Paeoniflorin (Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall.

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

LCB-2853 is a potent thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor antagonist with antiplatelet aggregation, antivasospasm, and antithrombotic effects.

Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots.

Vicagrel is an effective, orally active antiplatelet compound that enhances the inhibitory effect of aspirin on platelet aggregation and thrombosis in rodents by irreversibly inhibiting P2Y12 receptors and reducing metabolic inactivation. Viagrel can be used to treat blood clots in coronary artery disease, peripheral vascular disease and cerebrovascular disease.

Roxifiban acetate(DMP 754 acetate) is a potent GP IIb / IIIa antagonist that exhibits antiplatelet aggregation activity via immune mediation and can be used in the study of human thrombocytopenia.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg/mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

Prasugrel (CS-747) is a piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Prasugrel Hydrochloride (LY 640315 Hydrochloride) is a piperazine derivative and pletelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.

UDM-001651 is an effective and orally bioavailable protease-activated receptor 4 antagonists (IC50=4 nM; Kd=1.4 nM). UDM-001651 displays antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay.

(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.

Antiplatelet agent 3 (Compound K-10) is a compound with antiplatelet aggregation activity, exhibiting IC50 values of 2.55, 3.22, and 2.09 mg/mL for platelet aggregation induced by ADP, AA, and COL, respectively. It holds potential for research in cardiovascular diseases.

GR 144053 trihydrochloride is a potent and selective GPIIb/IIIa receptor antagonist (IC50 = 20 nM). It inhibits fibrinogen-mediated platelet aggregation, used for thrombosis and antiplatelet drug discovery research.

Rhamnetin tetraacetate is a potent antiplatelet compound that strongly inhibits platelet aggregation induced by arachidonic acid, collagen and PAF.

Salvianolic acid B (Dan Shen Suan B), a natural product from Salvia miltiorrhiza, is a water-soluble antioxidant. Salvianolic acid B has antiplatelet aggregation, anticoagulant, and antithrombotic effects, and is commonly used in the study of microcirculatory disorders.

MIPS-9922 is a potent and selective PI3Kβ inhibitor with antiplatelet activity. MIPS-9922 inhibited integrin αIIbβ3 activation and αIIbβ3 dependent platelet adhesion to immobilized vWF under high shear. MIPS-9922 also potently inhibited ADP-induced washe

1. Skimmianine (Chloroxylonine) is a spasmolytic agent. 2. Skimmianine (Chloroxylonine) shows pharmacol. props. similar to 2-(Methylamino)-1-phenyl-1-propanol BCJ45-G.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

6-keto Prostaglandin E1 is a bioactive derivative of PGE1 that plays a role in antiplatelet aggregation and depolymerization.

Rubiayannone A, an anthraquinone glycoside, exhibits antiplatelet aggregation activity.