leukotriene d4

Leukotriene D4 (LTD4) 是一种由花生四烯酸形成的强效促炎介质，是一种支气管收缩剂，可诱导成骨细胞衰老。Leukotriene D4 诱导潜在致癌基因的转录活性，可用于研究哮喘。

RS-601 是一种有效的 leukotriene D4 thromboxane A2 双重抑制剂，对抗原诱导的气道高反应性 （AHR）有抑制作用且在豚鼠哮喘模型中显示出平喘作用。

14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both guinea pig ileum and pulmonary parenchyma in contrast to the effects of 5-LO-derived LTs. However, in an in vitro permeability assay, 14,15-LTD4 can increase vascular permeability of human endothelial cell monolayers, with similar potency to that of 5-LO-derived LTs, resulting in plasma leakage, a hallmark of inflammation.

11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guinea pig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea.

Amlexanox (AA673) 是一种特异性的 IKKε和 TBK1抑制剂，其 IC50=1-2 μM。

ONO4057 是一种具有有效性和口服活性的 Leukotriene B4 受体拮抗剂，其 IC50 值为 0.7±0.3 μM。 ONO4057 对大鼠同种异体移植的免疫抑制作用。

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。

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

RG 7152 是白三烯 D4 拮抗剂,具有抗哮喘作用，可作用于研究哮喘。

Masilukast(MCC-847) 是一种口服的白三烯D4 (LTD4) 受体拮抗剂，可用于研究与炎症相关的疾病。

Cilastatin (MK0791) 是一种可逆的竞争性的肾脏脱氢肽酶 I 抑制剂，IC50为 0.1 μM。它抑制细菌金属叶内酰胺酶CphA 的IC50为 178 μM，可用作抗菌辅助剂。

CP-96486 is a potent and orally active antagonist of leukotriene D4 (LTD4) platelet activating factor (PAF) receptor (Kis: 20 and 24 nM).

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM(rabbit platelet membranes guinea pig cerebellum membranes).IC50 value:Target: PAF H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 + - 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 + - 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+ -0.4 microM, 3.2+ -0.7 microM and 1.5+ -0.4 microM, respectively whereas for loratadine the IC50 was 2.1+ -0.9 microM, 4.0+ -1.3 M and 1.7+ -0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.

Zafirlukast (ICI 204219) 是一种白三烯 D4 受体 (LTD4) 拮抗剂 (IC50=0.6 μM)，具有口服活性。Zafirlukast 具有平喘、抗炎和抗菌作用，被用于哮喘的预防和治疗。

SR 2640 hydrochloride 是白三烯 D4 和 E4 的竞争性拮抗剂，可用于研究人类哮喘中的白三烯。

Cilastatin is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor.

KP496 is a selective, dual antagonist for Thromboxane A2 receptor and Leukotriene D4 receptor.

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).

Triptinin A and triptinin B are leukotriene D4 antagonist constituents.

MDL-28753 is an antagonist of leukotriene D4 and antagonist of leukotrine C4.

LY 203647 is a antagonist of leukotriene D4 and E4 receptor.

Zafirlukast-d7 是 Zafirlukast 的氘代化合物。Zafirlukast 的 CAS 号为 107753-78-6。Zafirlukast 是一种可口服的白三烯 D4受体拮抗剂，具有平喘、抗炎和抗菌作用。

LTD4 antagonist 1 is a potent and orally active antagonist of leukotriene D4 (LTD4; Ki: 0.57 nM).

Way 126299a is a dual-acting 5-lipoxygenase inhibitor and leukotriene D4 antagonist.