monocytes

Dexamethasone (Hexadecadrol) 是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。Dexamethasone 具有抗炎和免疫抑制活性，可诱导自噬。Dexamethasone 抑制 LPS 诱导的巨噬细胞炎症反应。

L-Leucyl-L-Leucine methyl ester hydrochloride (Leu-Leu-ome hydrochloride) 是一种人单核细胞或多形核白细胞产生的 L-亮氨酸甲酯的二肽缩合产物。L-Leucyl-L-Leucine methyl ester hydrochloride 可选择性消除具有细胞毒性潜能的淋巴细胞，也可诱导溶酶体途径应激。

Phellopterin 是一种分离自P. trifoliata 中的天然产物。它能够调节 Akt 和 PKC 通路，抑制 TNF-alpha 诱导的 VCAM-1 表达，进而减少单核细胞与内皮细胞的粘附。

Adalimumab 是一种特异性靶向人 TNF-α 的全人重组 IgG1 单克隆抗体。Adalimumab 可以用于治疗类风湿关节炎、强直性脊柱炎、银屑病等。

LM-1685是一种有效且具有选择性的人单核细胞和全血中COX-2抑制剂，IC50分别为0.65 µM 和IC50 = 4.3 μM，是治疗炎症的潜在化合物。

GLPG3312是一种选择性和有效的泛SIK抑制剂，具有口服活性的优点，对SIK1、SIK2和SIK3的IC50=0.6-2.0 nM，在人原代髓细胞和小鼠模型中均表现出抗炎和免疫调节活性。

IL-4-inhibitor-1 是 IL-4 的抑制剂 (EC50 = 1.81 µM)。

Indobufen (Ibustrin) 是一种血小板聚集抑制剂，是下调单核细胞中的组织因子，可逆抑制血小板环氧合酶 (Cox) 的活性和血栓素 A2 (TxA2) 的合成。

Geranylgeraniol (FT0626663) 是一种类异戊二烯，存在于水果、蔬菜和谷物中，包括大米。 Geranylgeraniol (FT0626663) 抑制生长并诱导各种肿瘤细胞的凋亡。 Geranylgeraniol (FT0626663) 保护单核细胞免受他汀类药物诱导的细胞毒性并抑制分枝杆菌的生长。

SKF-86002 是一种可口服的 p38 MAPK 抑制剂，具有抗炎和抗关节炎活性，可用于缓解疼痛的研究。它能抑制脂氧合酶和环氧合酶介导的花生四烯酸代谢，还抑制脂多糖 (LPS) 刺激人单核细胞产生 IL-1 和 TNF-α，IC50为 1 μM。

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

ACT-389949 是一种高效的甲酰肽受体 2 脂蛋白 A4 受体(FPR2) (ALX)选择性激动剂，对 FPR2 ALX 进行内化入单核细胞的EC50值为 3 nM。它对炎性疾病具有潜在的研究价值。

LR-90, 作为一种高级糖基化终产品(AGE)抑制剂，在糖尿病动物模型研究中被广泛使用。LR-90 有效地抑制了人类单核细胞中的炎症反应。

CCX140 (CCX140-B) 是 CCR2 的拮抗剂。

Lobucavir inhibits the replication of the HIV virus in T cells, monocytes & macrophages in vitro by inhibiting DNA polymerase and viral DNA synthesis.

IX-207-887是一种新型抗关节炎化合物，能在体外有效抑制来自人类单核细胞和小鼠腹膜巨噬细胞的白细胞介素-1（IL-1）的释放，其作用浓度能在人类风湿性关节炎及动物关节炎模型中达到治疗水平。此外，IX-207-887具有抑制IL-1释放的新颖特性。

GHN105 是一种具有口服活性的STING抑制剂，能够在THP-1人单核细胞中以IC50为4.4 μM的浓度抑制STING依赖性的IFN-β分泌。GHN105 可降低小鼠血清中的IFN-β、IL-6和CXCL10水平，并在DSS诱发的急性结肠炎小鼠模型中缓解结肠炎。该化合物在小鼠体内展示了良好的药代动力学参数，口服生物利用度为43%，半衰期为1.1小时。

LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂，抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。

DA-E 5090 is a pharmacologically active metabolite of E 5090, is an interleukin-1 antagonist. DA-E 5090 is a novel inhibitor of IL-1 generation, in vitro inhibitory effects on the generation of IL-1 by human monocytes.

3M-003 与 Toll 样受体 7 (TLR-7) 和 TLR-8 相互作用。 3M-003 直接作用于巨噬细胞，增强真菌杀伤力，并刺激 PBMC 产生可溶性因子，增强中性粒细胞、巨噬细胞和单核细胞的杀伤力。 3M-003 可能是抗真菌免疫疗法的候选药物。

CC-3052 is a water-soluble, highly stable thalidomide analogue that is an effective inhibitor of HIV-1 expression and activation-induced TNF-α production. CC-3052 also inhibited PHA-induced and rTNF-α induced TNF-α transcription in PBMC, as well as TNF-α

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

(±)13-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of LDL, to 13-HODE cholesteryl ester.

(±)9-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of LDL, to 9-HODE cholesteryl ester.