endotoxin

Endotoxin Inhibitor acetate(147396-10-9 free base) 对细菌生理活性有很强的阻断作用，从而产生具有二硫键和大量赖氨酸的抗菌毒素抑制剂序列。内毒素抑制剂醋酸盐在酸性条件下更可能发挥生理活性

JTE-607 HCl 是高选择性的炎性细胞因子合成抑制剂，可保护小鼠免受内毒素休克。它作用于 LPS 刺激的人 PBMC，抑制TNF-α(IC50:11 nM)、IL-1β(IC50:5.9 nM)、IL-6(IC50:8.8 nM)、IL-8(IC50:7.3 nM)和IL-10(IC50:9.1 nM)。

Endotoxin inhibitor TFA 是一种可以与脂多糖(LPS)的成分脂质A高亲和力结合的合成肽，具有中和LPS毒性、预防LPS引发的细胞因子释放的作用。此外，Endotoxin inhibitor TFA能够有效抑制LPS引起的发热反应，同时具有极低的毒性和致死率。

Poly(guluronate)，low endotoxin 是 Alginate 分子中负责其胶凝特性的关键部分，并具有离子交联的功能。

Ovalbumin (low endotoxin) 是蛋清中的主要蛋白质，具有抗癌、降压、抗菌、抗氧化和免疫调节等多种生物活性。Ovalbumin (low endotoxin)是经过孕酮或雌激素处理的输卵管中合成最丰富的蛋白质，常用作研究激素对组织基因表达调控的标志物。

U-83836E (lazaroid ) 具有神经保护活性和抗肿瘤活活性，抑制神经胶质瘤细胞增殖，抑制肿瘤坏死因子并逆转内毒素诱导的休克。

Zoliprofen 是一种一种高效的且可口服的非甾体抗炎剂，具有抗炎、解热和镇痛活性，对角叉菜素、制霉菌素、刀豆球蛋白A 诱导的大鼠爪水肿，以及抗大鼠兔血清诱导的骨折或背皮水肿具有抑制作用。Zoliprofen 在大鼠和兔子中对胶原蛋白或花生四烯酸引起的血小板聚集方面比布洛芬和非诺洛芬有效20倍。Zoliprofen 对小鼠内毒素诱导的腹泻和花生四烯酸诱导的兔急性死亡抑制作用显著。

N,N-Dimethylacetamide (DMAc) 是一种具有血脑透过性的药物赋形剂，具有抗炎活性，通过抑制 NF-κB 信号通路发挥作用。N,N-Dimethylacetamide 可在体内减弱内毒素诱导的炎症反应。

5-Methyltryptamine hydrochloride 是一种高亲和力的 5-HT1C 受体配体和 5-HT 的部分激动剂。 5-Methyltryptamine hydrochloride 可保护遭受烧伤、止血带和内毒素休克的小鼠。

D(+)-Galactosamine hydrochloride (D-Galactosamine HCl) 是一种被证实的实验毒素，它能够产生自由基及UTP 核苷酸的消耗导致肝损伤，中毒剂量会造成肾功能不全，而肾功能衰竭通常和终末期肝损伤有关。脂多糖 D-Galactosamine 诱导的急性肝损伤是一种已知的暴发性肝衰竭动物模型。

Lanthanum trichloride 可用作分析试剂，可用作提取金属镧的原料和石油裂化催化剂。它在医药领域也有一定的作用。例如，研究表明，它对内毒素（LPS）体内作用的拮抗作用对寻找新的有效内毒素拮抗剂有一定的影响，为防治内毒素血症提供了实验依据。

Rupatadine(UR-12592,卢帕他定)是一种有效和可口服的PAF和组胺H1受体的双重拮抗剂，Ki 值分别为 0.55 μM 和 0.1 μM，能够缓解过敏症状并抗炎，可用于过敏性鼻炎和慢性荨麻疹。

Licochalcone B 是从Glycyrrhiza inflate 根中提取的。它能够抑制淀粉样蛋白 β 自聚集作用 (IC50=2.16 μM) ，分解预先形成的 Aβ42原纤维，并通过螯合金属离子抑制金属诱导的 Aβ42聚集。

Betamethasone 17-Propionate 在实验中主要是探讨其对大鼠内毒素诱导的葡萄膜炎的治疗潜力。通过滴眼和全身给药的方式，该化合物能在一定剂量（全身给药时为 1 mg kg）下抑制细胞在房水中的渗入，尽管其效果相比其他化合物较弱。在体外实验中，Betamethasone 17-Propionate 对大鼠腹膜渗出细胞中的白细胞介素-8（IL-8）的抑制作用也不如倍他米松。研究还发现，当与倍他米松二丙酸酯共同使用时，两者的联合效应可能减弱对细胞浸润和IL-1β基因表达的抑制。

Adenosine N1-oxide (1-Oxoadenosine) 是在蜂王浆中发现的腺苷 N1-氧化物，可抑制活化的巨噬细胞分泌炎症介质，并降低脂多糖 (LPS) 诱导的内毒素休克的致死率。

XMP-629, an endotoxin inhibitor, is used potentially for the treatment of impetigo and acne rosacea.

Epibetulinic acid 对细菌内毒素刺激的小鼠巨噬细胞 (RAW 264.7) 中 NO 和前列腺素 E(2) 的产生具有有效的抑制作用，IC50分别为 0.7 和 0.6 μM，具有抗炎活性。

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

1a,1b-dihomo Prostaglandin E2 (PGE2) is a rare polyunsaturated fatty acid first identified in extracts of sheep vesicular gland microsomes, known to contain COX, incubated with adrenic acid . 1a,1b-dihomo PGE2 has also been identified in conditioned media of RAW 264.7 macrophages stimulated with endotoxin and arachidonic acid . This product is thought to be produced by elongation of AA to adrenic acid, which is then metabolized sequentially by COX and PGE synthase.

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)

PD-149163 hydrochloride 是一种神经降压素激动剂，具有抗精神病活性，可调节小鼠模型细菌内毒素脂多糖诱导的神经炎症，可用于研究神经系统疾病。

Vipoglanstat is a prostaglandin E synthase inhibitor and an anti-inflammatory. Vipoglanstat ameliorates leukocyte infiltration and lung injury resulting from both endotoxin-induced and sepsis-induced lung injury.

AS 703026 has been shown to inhibit LPS-induced TNFα production in macrophages monocytes as well as protect from LPS-induced endotoxin shock. AS 703026 may be useful as an anti-inflammatory therapy for COPD patients.

Nebacumab (HA-1A)为一种与内毒素的脂质A部分结合的单克隆抗体，适用于败血症研究。