thromboxane a-2

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.

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

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Ramatroban (BAY u3405) (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.

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.

NP-313 (NSC-4264) is a potent antithrombotic agent that inhibits platelet aggregation and activation by inhibiting thromboxane A 2 synthesis and selectively inhibiting SOCC-mediated Ca2+ efflux.

Imidazole-d4 is an isotope-labeled variant of imidazole, which is a heterocyclic aromatic compound. Imidazole molecules serve as inhibitors for acetylcholinesterase (AChEI) and xanthine oxidase (XO) and have been utilized as corrosion inhibitors. They display a range of biological activities, including antifungal, antitubercular, anti-inflammatory, antioxidant, and analgesic properties. Imidazole inhibits platelet microsomes from converting endoperoxides (PGG2 and PGH2) into thromboxane A2. Additionally, imidazole derivatives show inhibitory effects on the SARS-CoV-2 3CLpro enzyme, offering potential for research in Alzheimer’s disease, gout, COVID-19, and thrombotic disorders.

2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside (Astragalus polyphenols) is a compound isolated from the roots of Polygonum species, which inhibits the formation of 5-HETE, HHT, and thromboxane B2.

STA 2 is an analogue of TXA2, a thromboxane receptor in the colonic epithelium.

8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a metabolite of the isoprostane 8-iso PGF2α in rabbits, monkeys, and humans. 8-iso PGF2α is a prostaglandin-like product of non-specific lipid peroxidation. In humans and monkeys, exogenously infused 8-iso PGF2α is converted to metabolites with 2 or 4 carbon atoms removed from the top side chain by β-oxidation, with a similar pattern observed in tritiated 8-iso PGF2α-infused rabbits. Early in the infusion (within 1-2 minutes), 8-iso-15-keto PGF2α is a major component of the metabolite profile, primarily comprising unmetabolized 8-iso PGF2α. 8-iso-15-keto PGF2α is a vasoconstrictor when tested on the rat isolated thoracic aorta, acting via the TP (thromboxane) receptor.

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.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

12(S)-HETE, a 12-lipoxygenase metabolite of arachidonic acid, is mitogenic for cancer cell proliferation and enhances angiotensin II-induced contraction of BLT2 (type 2 receptor in arteries of leukotriene B4 mice) and TP (thromboxane receptor)-mediated mechanisms. 12(S)-HETE promotes superoxide and isothromboxane-like metabolites in arterial endothelial cells. production.

1,2,3-Trilinoelaidoyl-rac-glycerol is a triacylglycerol that contains linoelaidic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trilinoelaidoyl-rac-glycerol (0.6-6.3% w/w) lowers serum levels of thromboxane B2 , prostaglandin F2 (PGF2), and PGE in rats.1 |1. Bruckner, G., Goswami, S., and Kinsella, J.E. Dietary trilinoelaidate: Effects on organ fatty acid composition, prostanoid biosynthesis and platelet function in rats. J. Nutr. 114(1), 58-67 (1984).

E 3040 is a dual inhibitor of 5-lipoxygenase and thromboxane A(2) synthetase. It is involved with eicosanoid production. E 3040 also has anti-inflammatory properties.

Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously express COX-2. Lornoxicam reduces LPS-induced production of nitric oxide and IL-6 in cell-based assays with IC50 values of 65 and 54 µM, respectively. It reduces carrageenan-induced paw edema in rats when administered intravenously at doses ranging from 0.1 to 9 mg kg. Formulations containing lornoxicam have been used in the management of postoperative pain.

TP Receptor Antagonist-2 (example 7n), a thromboxane A2 receptor (TP receptor) antagonist, exhibits inhibitory activity with IC50 values of 5.64 μM for TPα and 5.27 μM for TPβ. It effectively inhibits platelet aggregation [1].

Indobufen-d5 is a deuterated compound of Indobufen. Indobufen has a CAS number of 63610-08-2. Indobufen is an inhibitor of platelet aggregation and is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.