ltc4

CP-96021 hydrochloride is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor receptor (Kis: 34 nM and 37 nM).

AS-35 是一种可口服且具有选择性和高效性的 leukotrienes 拮抗剂，抑制 LTC4，LTD4 和 LTE4 诱导的回肠收缩。AS-35 具有抗过敏作用，抑制白三烯合成。

RG-12525（NID 525） 是一种可口服且具有选择性和竞争性的白三烯 D （LTD）拮抗剂，对 LTC4，LTD4 和 LTE4 诱导的豚鼠薄壁带收缩有抑制作用，IC50 值分别为 2.6 nM，2.5 nM 和 7 nM。RG-12525 对 CYP3A4 有抑制作用， Ki 值为 0.5 µM。RG-12525 是一种新型高效的 PPAR-γ 激动剂（IC50 值约为 60 nM），具有物种特异性，可用于研究哮喘。

Leukotriene C4 (LTC4) 是一种类花生酸脂质介质，可调节炎症部位白细胞的募集和功能。Leukotriene C4 是支气管收缩、粘液分泌过多和嗜酸性粒细胞增多的介质，在荨麻疹中具有介导作用。

CI-949 is an allergic mediator release inhibitor, which inhibits leukotriene C4/D4 (LTC4/LTD4), histamine, and thromboxane B2 (TXB2) release (IC50s: 0.5 μM, 11.4 μM and 0.1 μM).

LM-1484 displays a higher affinity for 3H-LTC4 sites and is an antagonist of CysLT1 receptor.

Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL.

Nedocromil (FPL 59002) 对多种介质的作用或形成有抑制作用，包括组胺，前列腺素 D2和白三烯 C4。

Ablukast (Ro 23-3544) 是白三烯受体的选择性拮抗剂，也是LTD4受体拮抗剂。可改善 LTC4 和抗原诱导的支气管狭窄。

R112 是 ATP 竞争性的 Syk 激酶抑制剂，它能够抑制 Syk 激酶活性，Ki=6 nM，IC50=226 nM。

AZD9898 是一种白三烯-C4 合成酶抑制剂，IC50 为 0.28 nM。 AZD9898 可用于哮喘研究。 AZD9898 减轻 GABA 结合和肝毒性信号。

Pranlukast (ONO-1078) 是一种半胱氨酰白三烯受体 1 拮抗剂，可拮抗或减少支气管痉挛，用于哮喘研究。

Hydrocortisone (Cortisol) 是一种糖皮质激素，由肾上腺素皮质分泌。Hydrocortisone 激动糖皮质激素受体，可促进蛋白质分解代谢、糖异生、毛细血管壁稳定性、肾脏钙排泄，并抑制免疫和炎症反应。

GJG057是一种高效和选择性的Leukotriene C4 synthase (LTC4S)抑制剂，在人全血LTC4释放试验中IC50=44 nM且具有口服活性，在小鼠哮喘加重模型中具有抗炎疗效，可用于治疗过敏性炎症。

5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) 是从黄芪中分离出的多甲氧基黄酮，具有抗炎活性，可通过直接抑制 5-LOX 发挥作用，IC50为 0.1 μM。

Pranlukast hemihydrate (ONO-1078 hemihydrate) 是一种具有选择性和高效性的白三烯 （LT）拮抗剂，具有抗哮喘活性，抑制 [3H]LTD4 和 [3H]LTE4 与肺膜的结合，拮抗 LTC4 诱导的豚鼠气管收缩。Pranlukast hemihydrate 可用于研究哮喘。

HAMI 3379 (HAMI3379) 是一种选择性半胱氨酰白三烯受体2（CysLT2） 拮抗剂，以剂量和时间依赖性地减轻大鼠局灶性脑缺血后的脑损伤并抑制小胶质细胞炎症，通过抑制小胶质细胞活化来减轻缺血样神经元损伤。

TK05 is a potent and selective leukotriene C4 synthase (LTC4S) inhibitor (IC50: 95 nM).

Pirodomast 是血栓素 A（TXA2）合成酶抑制剂。Pirodomast 能抑制白三烯（LT）D4、C4、E4 的形成和血栓素 B2（TXB2）的活性，但对组胺、甲氧胆碱、血清素、LTC4 或血小板活化因子诱导的豚鼠支气管痉挛的拮抗作用较弱或无效。Pirodomast 在体外对豚鼠气管只有微弱的松弛活性。Pirodomast 是一种潜在的抗过敏化合物，在体外可抑制胰蛋白酶的蛋白水解活性，在体内可阻止抗原诱发过敏绵羊的即时和晚期哮喘反应，抑制抗原诱导的过敏绵羊对组胺和卡巴胆碱的气道高反应性。

(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.

ONO-8809 is a thromboxane A2 receptor antagonist. ONO-8809 inhibited the LTC4-induced airway hyperresponsiveness to histamine in a dose-dependent manner. Macrophage accumulation and matrix metalloproteinase-9 (MMP-9) activity in the stroke-negative area i

Leukotrienes (LTs) are a group of acute inflammatory mediators derived from arachidonic acid in leukocytes. The majority of these metabolites are formed through the 5-lipoxygenase (5-LO) pathway. 14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-LOs on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. These metabolites are classified as eoxins because they are formed mostly by eosinophils. Mast cells and nasal polyps can synthesize 14,15-LTC4 as well, however metabolism to 14,15-LTE4 in these cells and tissue has not been documented. 14,15-LTE4 increases vascular permeability of human endothelial cell monolayers with about 10-fold less potency than LTC4, but approximately 100-fold greater potency than histamine.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum as a cysteinyl leukotriene receptor preparation, the pKis for LTC4 and 11-trans LTC4 were determined to be 6.42 and 6.58, respectively.