thromboxane

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

Thromboxane A2, as an unstable intermediate between the prostaglandin endoperoxides and thromboxane B2, is a potent inducer of platelet aggregation and causes vasoconstriction.

15(R)-Pinane thromboxane A2 is the (R)-epimer of pinane thromboxane A2 . 15(R)-PTA2 does not inhibit collagen-induced platelet aggregation (IC50s = 120-130 μM). It does not affect gastric tone in isolated rat gastric fundus when used at concentrations of 0.5 or 1.5 μg/ml and is less effective than PTA2 at inhibiting prostaglandin-induced contraction of isolated rat stomach muscle.

Thromboxane B2 (TXB2) is released in substantial quantities from aggregating platelets and metabolized during circulation to 11-dehydro TXB2 and 2,3-dinor TXB2. In rats and rabbits, 2,3-dinor TXB1 has been identified as another urinary metabolite of TXB2. However in human urine, only trace amounts of 2,3-dinor TXB1 have been identified. In rats, 2,3-dinor TXB1 is excreted at a much higher rate than 2,3-dinor TXB2 (19.2 ± 4.9 ng/24 hr and 1.6 ± 0.3 ng/24 hr, respectively). Therefore, urinary 2,3-dinor TXB1 is a suitable marker of thromboxane biosynthesis in rats.

Carbocyclic Thromboxane A2 can be used in related research in the field of life sciences. Its product number is T36548 and CAS number is 74034-56-3.

Thromboxane B2 (a prostaglandin derivative released during anaphylaxis) induces platelet aggregation and arterial contraction.

Thromboxane B1 (TXB1), a member of the Thromboxane B (TXB) family, is a lipid belonging to the eicosanoid family, recognized for its function in blood clot formation (thrombosis) [1].

Thromboxane B3 (TXB3), the stable hydrolysis product of TXA3, is synthesized from eicosapentaenoic acid (EPA) through the action of COX and thromboxane synthase enzymes. This compound is biosynthesized in several tissues, including seminal vesicles, lungs, polymorphonuclear leukocytes (PMNL), and ocular tissues.

11-Dehydro Thromboxane B3 (11-dehydro TXB3) serves as a urinary metabolite of TXA3 in humans following an increased dietary intake of EPA.

Thromboxane B2 (TXB2) is a compound significantly released from aggregating platelets and undergoes metabolic transformation during circulation into 11-dehydro TXB2 and 2,3-dinor TXB2. The latter, 2,3-dinor TXB2, serves as a prevalent urinary metabolite of TXB2 and acts as an indicator for in vivo TXA2 synthesis. Studies have shown that in healthy male volunteers, the median excretion rate of 2,3-dinor TXB2 is measured at 10.3 ng/hour, equivalent to 138 pg/mg of creatinine.

11-Dehydro-2,3-dinor Thromboxane B2 (11-dehydro-2,3-dinor TXB2) is a metabolite derived from the inactive TXA2 metabolite, TXB2. Its formation involves the action of cytosolic aldehyde dehydrogenase (ALDH) and β-oxidation processes. Remarkably, levels of 11-dehydro-2,3-dinor TXB2 have been observed to increase by 5.2-fold in a surgery-induced rat model of tendon overuse, highlighting its potential role in physiological stress responses.

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.

FUREGRELATE, a thromboxane A2 (TxA2) synthase inhibitor, blunts the development of pulmonary arterial hypertension in neonatal piglets.

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

RS-601 is a potent dual leukotriene D4 thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

AZ-1355 is a novel dibenzoxepine derivative with lipid-lowering properties.

Daltroban (SKF 96148) is a specific thromboxane A2 (TXA2) receptor antagonist. Daltroban shows protective effect in reperfusion injury. Daltroban increase intracellular calcium in vascular smooth muscle cells.

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.

Linotroban(CL-871502) is a potent selective thromboxane (TXA2) receptor antagonist with antithrombotic activity.

Isbogrel (CV4151) is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor that can be used to study cardiac arrhythmias, transient ischemic attacks and thrombosis.

Dazmegrel (UK 38,485) is a potent and specific thromboxane A2 (TXA2) synthase inhibitor for the prevention of increased whole platelet aggregation in normal pregnancy.

Dazmegrel HCl is a platelet thromboxane inhibitor used in the study of myocardial infarction and arrhythmias.

pirmagrel is a potent thromboxane synthase inhibitor.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.