thromboxane a-2

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

Ozagrel (Domenan) 是血栓烷 A2(TXA2) 合酶抑制剂，可抑制哮喘。它也是一种抗血小板剂，可选择性抑制人血小板聚集，IC50为 53.12 μM。

Imitrodast是一种小分子血栓素A2合成酶（TXA2 synthase）抑制剂，可用于治疗免疫系统疾病、呼吸系统疾病和心血管疾病，可用于研究动脉血栓形成、哮喘和冠状血管痉挛。

p-Hydroxycinnamic acid (NSC-59260) 是常见的食用酚，可抑制血小板活性，对血栓素 B2 和前列腺素 E2 的 IC50值分别为 371 和 126 μM。

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.

Carbocyclic Thromboxane A2 可用于生命科学领域的相关研究。其产品编号为 T36548，CAS号为 74034-56-3。

Ketoprofen (RP-19583) 是一种非甾体抗炎剂，能够有效地抑制COX 的活性，在人血单核细胞中，对 COX-1 和 COX-2 的IC50值分别为 2 nM 和 26 nM。

Ramatroban (BAY u3405) 是一种血栓素 A(2) (TxA(2)) 拮抗剂，IC50为 14 nM。它还通过抑制PGD2结合从而拮抗CRTH2，IC50为113 nM。它用于治疗过敏性鼻炎，可用于治疗哮喘的研究。

Ozagrel hydrochloride (OKY-046 HCl) 是一种选择性血栓素 A(2) 合成酶抑制剂，用于改善术后脑血管收缩和伴随的脑缺血。它是一种抗血小板剂，可选择性抑制人血小板聚集，IC50为 53.12 μM。

Imidazole-d4是一种同位素标记的Imidazole，属于杂环芳香族化合物。咪唑类分子被广泛应用于缓蚀剂以及酶抑制剂，如乙酰胆碱酯酶（AChEI）和黄嘌呤氧化酶（XO），并展示出抗真菌、抗结核、抗炎、抗氧化和镇痛等生物活性。此类化合物能够阻止血小板微粒体将内过氧化物(PGG2 和 PGH2)转化为血栓素A2。咪唑衍生物对SARS-CoV-2 3ClPro酶的抑制作用表明其在阿尔茨海默病、痛风、新冠肺炎和血栓疾病等研究中具有潜力。

NP-313 (NSC-4264) 是一种有效的抗血栓剂，对血栓素 A 2 合成和选择性抑制由 SOCC 介导的 Ca 2+ 内流有抑制作用，可以抑制血小板的聚集和活化。

2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside (Astragalus polyphenols) 是分离自蓼属植物物种的根中，对5-HETE、HHT、thromboxane B2的形成具有抑制作用。

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-isoprostane (8-iso PGF2α) is a prostaglandin-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-iso PGF2α is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-iso PGF2α is infused into rabbits. Early in the infusion (within 1-2 minutes) 8-iso -15-keto PGF2α was a major component of the metabolite profile, which was comprised mostly of 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.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2]. Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1 2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1 2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2 M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells [1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.

12(S)-HETE 是花生四烯酸的12-脂氧合酶代谢产物，对癌细胞增殖具有促有丝分裂作用，可增强血管紧张素 II 诱导的 BLT2 收缩（白三烯 B4小鼠动脉中 2 型受体）和 TP （血栓素受体） 介导的机制。12(S)-HETE促进动脉内皮细胞中超氧化物和异血栓素样代谢物的产生。

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) 为血栓素 A2受体 (TP 受体) 的拮抗剂，其对TPα和TPβ的IC50值分别为5.64 μM 和5.27 μM。此化合物具有抑制血小板聚集的功能。

Indobufen-d5 是 Indobufen 的氘代化合物。Indobufen 的 CAS 号为 63610-08-2。Indobufen 是一种血小板聚集抑制剂，是下调单核细胞中的组织因子，可逆抑制血小板环氧合酶 (Cox) 的活性和血栓素 A2 (TxA2) 的合成。