leukotriene b4

Leukotriene B4 (LTB4) 是一种通过 5-脂氧合酶途径从花生四烯酸衍生而来的化合物，可介导某些炎症和免疫反应。Leukotriene B4 诱导中性粒细胞胞外陷阱阻碍肺孢子菌的清除。

Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-LO pathway. It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis. 12-oxo LTB4 is an initial metabolite of LTB4 formed via the LTB4 12-hydroxydehydrogenase pathway. It is rapidly converted to 10,11-dihydro-12-oxo-LTB4, followed by reduction of the 12-oxo group to give 10,11-dihydro-LTB4. 12-oxo-LTB4 (EC50 = 33 nM) is about 70-fold less potent than LTB4 (EC50 = 0.46 nM) at stimulating Ca2+ mobilization in human neutrophils. It is also significantly less potent than LTB4 at stimulating neutrophil migration with EC50 values of 170 and 2.7 nM for 12-oxo-LTB4 and LTB4, respectively.

Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-lipoxygenase pathway. It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis. At least two LTB4 receptors, termed BLT1 and BLT2, have been identified. 14,15-dehydro LTB4 is a LTB4 receptor antagonist that has a higher binding affinity for BLT1, demonstrating a Ki value of 27 nM, compared to BLT2, which has a Ki value of 473 nM. 14,15-dehydro LTB4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC50 value of 1 μM.

LTB4 dimethyl amide is a moderate inhibitor of LTB4-induced degranulation of human neutrophils (Ki = 130 nM) and lysozyme release from rat PMNL. LTB4 dimethyl amide appears to be an antagonist of the LTB4 receptor on guinea pig lung membranes.

The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2. LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4-EA was a potent antagonist with about three times greater affinity for the receptor than LTB4 (Ki = 1.22 nM versus 3.88 nM). LTB4-EA antagonizes the LTB4-induced contractions of guinea pig lung parenchyma with an EC50 of 10 nM. LTB4-EA thus represents a potential endogenous anti-inflammatory compound functioning as a natural antagonist of BLTR1.

Leukotriene B4 (LTB4) compounds are produced by both enzymatic and non-enzymatic processes. The products of enzymatic origin, via Leukotriene A4 (LTA4) hydrolase, are stereospecifically 12(R). Non-enzymatic hydrolysis products are 50:50 mixtures at C-12, but are almost exclusively trans at C-6. Thus, the non-enzymatic hydrolysis product of LTA4 is 6-trans-12-epi LTB4. 12-epi LTB4 is an isomer which would not be expected to occur in either non-enzymatic hydrolysis products, or in the enzymatic products of LTA4 hydrolase. Compared to LTB4, 12-epi LTB4 has significantly reduced activity for the LTB4 receptor on human neutrophils (IC50 of 7.5 mM), and on guinea pig lung membranes with a (Ki of 4.7 mM). 12-epi LTB4 is an weak agonist at both the recombinant human BLT1 and BLT2 receptors, requiring approximately 10 mM for full activation of the receptor.

20-hydroxy LTB4 is a metabolite of LTB4 in human neutrophils. In human leukocytes, LTB4 is inactivated by the enzyme LTB4 20-hydroxylase. 20-hydroxy LTB4 is not only much less active (~5%) compared to LTB4 in causing degranulation of PMNL, but actually inhibits LTB4-induced degranulation of human neutrophils (Ki = 13.3 nM). However, 20-hydroxy LTB4 is as active as LTB4 in contracting parenchymal strips from guinea pig lung. 20-hydroxy LTB4 retains considerable ligand binding affinity at the BLT2 receptor, but does not appear to function as an agonist.

6-trans-12-epi-Leukotriene B4 是一种花生四烯酸代谢物，是一种有效的抗炎剂。

20-Carboxy-Leukotriene B4 (20-COOH LTB4) 是 Leukotriene B4 (LTB4) 的代谢物。20-Carboxy-Leukotriene B4 以高亲和力与 BLT1 受体结合。20-Carboxy-Leukotriene B4 抑制 LTB4 介导的中性粒细胞反应，迁移、脱粒、白三烯生物合成。

18-Carboxy dinor Leukotriene B4 (18-carboxy dinor LTB4) represents a β-oxidation metabolite of Leukotriene B4 (LTB4). Initially, LTB4 is metabolized in the liver to 20-carboxy LTB4, which subsequently undergoes β-oxidation to form 18-carboxy dinor LTB4.

20-trifluoro Leukotriene B4 是一种活性分子，可用于生命科学相关研究，其 CAS 号为 115178-97-7。

5-Oxo Leukotriene B4 (5-oxo LTB4) serves as an intermediate metabolite in the production of 12-oxo LTB4.

Leukotriene B4 (LTB4)-3-aminopropylamide is an analog of LTB4 that exhibits potent and selective binding to the BLT1 receptor with Ki values of 5.1 nM at BLT1 and 1,227 nM at BLT2, indicating its high affinity for BLT1 over BLT2. This compound's effects are mediated through interactions with two receptors, BLT1 and BLT2.

Sulfasalazine (Azulfidine) 是一种合成的水杨酸衍生物，对含有弹性蛋白的结缔组织具有亲和力，并配制成前药。Sulfasalazine 可以诱导铁死亡，抑制 NF-κB、TGF-β 和 COX-2。

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。

Bunaprolast (U66858) 是一种新型有效的白三烯 B4 (LTB4) 抑制剂。Bunaprolast 具有氧化降解活性，对脂氧合酶 (lipoxygenase)和 TXB2 释放具有抑制作用。

CJ-13,610 是一种具有口服活性的非氧化还原型 5-脂氧合酶 (5-LOX) 抑制剂。 CJ-13,610 抑制白三烯 B4 的生物合成并调节巨噬细胞中 IL-6 mRNA 的表达。

Ticolubant 是一种具有口服活性的白三烯 B4 拮抗剂，对人类中性粒细胞 LTB4 受体具有很高的亲和力（Ki = 0.78 nM），能阻断 LTB4 诱导的 Ca2+ 迁移，IC50 为 6.6±1.5 nM，并在小鼠皮肤炎症模型中显示出局部抗炎活性。

Moxilubant 是一种小分子白三烯B4受体1（LTB4R）拮抗剂，可用于治疗免疫系统疾病、皮肤和肌肉骨骼疾病，可用于研究银屑病和类风湿关节炎。

Ontazolast 是一种小分子白三烯B4受体（LTB4R）拮抗剂，可用于治疗免疫系统疾病和呼吸系统疾病。Ontazolast 是治疗哮喘的候选化合物。

BIRM 271 是一种新型花生四烯酸释放抑制剂，可阻断白三烯B4和人中性粒细胞中的血小板活化因子生物合成。BIRM 271 和 BIRM 270 属于对映异构体，对白三烯B4 的产生有抑制作用，IC50 为40 nM。

Croconazole 对中性粒细胞的 5-脂氧合酶 (5-LOX) 表现出剂量依赖性抑制活性。Croconazole 是一种抗真菌剂。Croconazole 对合成白三烯 B4 (LTB4) 和 5-羟基二十碳四烯酸 (5-HETE) 的 IC50 分别为 7.8 ± 1.7 和 7.6 ± 0.3 μM。

Moxilubant HCl 是一种小分子白三烯 B4 受体 1（LTB4R）拮抗剂，可用于治疗免疫系统疾病、皮肤和肌肉骨骼疾病，可用于研究银屑病和类风湿关节炎。

BIIL-260 hydrochloride 是一种具口服活性和高效性的白三烯 B(4) 受体 (LTB4) 拮抗剂，具有抗炎活性，以可饱和、可逆和竞争的方式与 LTB（4） 受体相互作用，抑制 LTB（4） 诱导的人中性粒细胞细胞内 Ca（2+） 释放 。