eosinophil

GS-143 是选择性的IκBα泛素化抑制剂，抑制 SCFβTrCP1介导的IκBα泛素化作用，IC50=5.2 μM。GS143 抑制NF-κB 的活化和靶基因的转录，并且不抑制蛋白酶体的特性，并具有抗哮喘作用。

AS1810722 是口服有效的STAT6抑制剂，IC50为 1.9 nM。它是一种稠合双环嘧啶衍生物，对有良好的CYP3A4抑制作用，具有用于过敏性疾病，如哮喘和特应性疾病的研究潜力。

Mepolizumab (SB 240563) 是一种中和 IL-5 的人源化单克隆抗体。 美泊利单抗可用于严重嗜酸性哮喘和嗜酸性肉芽肿伴多血管炎的研究。

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。

WHI-P97 是一种选择性 JAK-3抑制剂，可用于预防过敏性哮喘的研究。

Theophylline monohydrate (Quibron) 似乎抑制磷酸二酯酶和前列腺素的产生，调节钙通量和细胞内钙分布，并拮抗腺苷。茶碱是黄嘌呤的天然生物碱衍生物，从植物山茶花和小粒咖啡中分离出来。在生理上，该药剂可放松支气管平滑肌，产生血管舒张（脑血管除外），刺激中枢神经系统，刺激心肌，利尿，增加胃酸分泌；它还可以抑制炎症并改善横膈膜的收缩性。

Adriforant (PF-3893787,ZPL-3893797,阿屈仑特)是一种竞争性的H4(histamine receptor 4)拮抗剂，拮抗组胺诱导的ERK磷酸化，使肥大细胞中组胺诱导的转录变化正常化，并降低神经元中组胺依赖性Ca 2+ 通量，可减轻小鼠瘙痒和皮肤

Benralizumab (MEDI-563) 是一种靶向白介素 5 受体 α (IL-5Rα) 单克隆抗体，通过增强抗体依赖性细胞介导的细胞毒性促使嗜酸性粒细胞快速进行反应。Benralizumab 可用于严重的嗜酸性哮喘，可用于预防慢性阻塞性肺病加重。

S-Y048 是一种 Oxoeicosanoid（OXE）受体拮抗剂，抑制过敏原诱导的嗜酸性粒细胞浸润到实验中对屋尘螨敏感的恒河猴皮肤，抑制因雾化过敏原攻击引起的肺部炎症。S-Y048 可用于研究哮喘和其他嗜酸性粒细胞性疾病。

NVP-QAV-680 is a potent and selective antagonist of CRTh2 receptor. NVP-QAV-680 has nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro.

Cetirizine Impurity B dihydrochloride (De(carboxymethoxy) Cetirizine Acetic Acid Dihydrochloride) 是 Cetirizine dihydrochloride 的杂质。Cetirizine 是一种抗组胺剂，是口服有活力的、特异性 H1受体拮抗剂。它能够抑制过敏反应期间嗜酸性粒细胞趋化，可以标记抗过敏特性。

RS-25344 是一种有效的选择性磷酸二酯酶 (PDE) 4 抑制剂。它在体外抑制嗜酸性粒细胞趋化性并增加精子的进行性运动。

Dansylglycine 是一种荧光探针，用于特异性测定髓过氧化物酶和嗜酸性粒细胞过氧化物酶的卤化活性。

Reslizumab (Sch 55700) 是一种人源化免疫球蛋白 G （IgG）4 κ 单克隆抗体，可与人白细胞介素 5 结合，从而减少嗜酸性粒细胞的产生和存活。Reslizumab 可改善肺功能，可诱导嗜酸性粒细胞的产生和成熟减少，可用于研究哮喘。

Apafant (WEB 2086) 是一种高效的血小板活化因子 (PAF) 拮抗剂，可阻断嗜酸性粒细胞活化，可用于研究豚鼠实验性过敏性结膜炎。

TAK-661 是一种抑制嗜酸性粒细胞趋化性 (eosinophil chemotaxis) 的化合物。该化合物能有效缓解晚期支气管收缩，并抑制在支气管肺泡灌洗 (BAL) 过程中嗜酸性粒细胞的增多，以及其向气道壁的浸润。

Piclamilast (RP 73401) 是一种有效的磷酸二酯酶 4(PDE4)的抑制剂，对猪主动脉和可溶性嗜酸性粒细胞中的 IC50值分别为 16 nM 和 2 nM。

Israpafant is a selective antagonist for the platelet-activating factor receptor ( IC50 = 0.84nM). Israpafant inhibits PAF-induced human platelet aggregation. Israpafant inhibits the activation of eosinophil cells and consequently delays the development o

PAF C-18:1 is a naturally occurring phospholipid produced by cells upon stimulation and plays a role in the establishment and maintenance of the inflammatory response. It is less potent than PAF C-16 and PAF C-18 in the induction of neutrophil chemotaxis, but is equipotent to PAF C-16 and PAF C-18 in promoting eosinophil migration. PAF C-18:1 activates the PAF receptor and has been used in antibody binding experiments to determine the importance of an acyl linkage at the sn-2 position for recognition at this receptor.

8(S),15(S)-DiHETE is formed when 15(S)-HETE is subjected to further oxidation by 15-LO. It causes eosinophil chemotaxis with an ED50 value of 1.5 μM but is not chemotactic for neutrophils. 8(S),15(S)-DiHETE antagonizes the hyperalgesic activity of 8(R),15(S)-DiHETE and LTB4 in the rat hind paw pain model.

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物，也是一种具有选择性和强效性的 CRTH2 DP2 受体激动剂，可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50= 55.8 nM).1It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg kg. 1.Aoyagi, H., Kajiwara, D., Tsunekuni, K., et al.Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitisEur. J. Pharmacol.875173030(2020)

The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.