microvascular

Tranilast (SB 252218) 是一种抗过敏药物，可抑制炎症细胞释放脂质介质和细胞因子，抑制前列腺素 D2 (PGD2)产生，IC50为 0.1 mM。它拮抗血管紧张素 II 并抑制其在血管平滑肌细胞中的生物学作用，具有抗炎和免疫调节作用。

INCA-6 (Triptycene-1,4-quinone) 是细胞渗透性的 NFAT 抑制剂。INCA-6 通过特异性阻断 NFAT 底物靶向钙调神经磷酸酶位点，有效抑制calcineurin (CN)-NFAT 信号传导。

Minalrestat(ARI-509) 是一种具有口服活性和有效性的醛糖还原酶 (aldose reductase) 抑制剂，可用于研究糖尿病患者微血管反应性受损。

Chromocarb (Chromone-2-carboxylic acid) 是合成的血管保护剂。

Flavanone (2-Phenylchroman-4-one) 是天然的黄酮类化合物，对人类雌激素合成酶芳香化酶具有抑制作用。

Dopexamine hydrochloride (FPL60278AR) 是β2肾上腺素能受体激动剂。

TGase2-IN-1（Compound 22）为一种具口服效力的TGase2抑制剂，其对TGase2的IC50值为1.12 μM，且对人视网膜微血管内皮细胞中TGase2的抑制作用的IC50为0.07 μM。此外，TGase2-IN-1展现出74.6%的口服生物利用度，并能有效抑制小鼠Streptozotocin诱导的糖尿病模型中视网膜血管渗漏。

Albifylline is a xanthine derivates with anti-asthmatic activity. Albifylline may cause a significant reduction of shock-induced leukocyte adhesions to the sinusoidal endothelium in the liver after hemorrhagic shock. Albifylline also improves microvascula

Labradimil is a bradykinin B2 receptor agonist. Labradimil increases the permeability of human brain microvascular endothelial cell monolayers. Labradimil enhances delivery of hydrophilic chemotherapeutics and increases survival in rats with metastatic tu

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-2 microglia stimulated by LPS and decreases LPS-induced cytotoxicity when used at concentrations ranging from 5 to 10 μM. It also decreases nitrite production when used at a concentration of 7.5 μM, an effect that can be partially reversed by the CB2 receptor antagonist AM630 and the PPARγ antagonist GW 9662 . (±)19(20)-EDP ethanolamide induces vasodilation of isolated preconstricted bovine coronary arteries (ED50 = 1.9 μM) and reduces tube formation by human microvascular endothelial cells (HMVECs) in a Matrigel assay.

Desmethylanethol trithione (ADT-OH) 是合成硫化氢的供体。它利用上调 FADD 诱导细胞凋亡，并对体内黑色素瘤的形成具有一定的抑制作用，可用于研究癌症疾病。

20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-AA binds to isolated ligand binding domains of peroxisome proliferator-activated receptor α (PPARα) (Kd = 0.87 ± 0.12 μM) and PPARγ (Kd = 1.7 ± 0.5 μM), and is a dual activator of PPARα and PPARγ in a transiently transfected COS-7 cell reporter system.

(20R)-Protopanaxadiol ((20R)-Protopanaxdiol) 是黑参中20(R)-人参皂甙 Rg3的一种三萜皂苷代谢物。它抑制幽门螺杆菌的生长，有抗肿瘤活性和细胞毒性。

(R)-(4′-Hydroxy)-5,7-dihydroxy-4-chromanone, an antiangiogenic homoisoflavonoid, exhibits activity against human retinal microvascular endothelial cells.

Deoxyshikonin (Arnebin 7) 是从紫草中分离的天然产物，具有抗肿瘤活性，在体外具有促血管生成作用。它和没食子酸十二烷基酯在体内外均与青霉素有显着的协同抗菌活性。

JMS-053 是一种具有有效性和选择性的磷酸酶 DUSP3 抑制剂， 抑制 PTP4A3、 PTP4A1 、 PTP4A2 和 CDC25B，抑制癌细胞迁移和球体生长，避免血管内皮生长因子或脂多糖对微血管内皮屏障功能的破坏。

Cremastranone is a natural antiangiogenic homoisoflavanone. Cremastranone inhibits the proliferation, migration, and tube formation ability of human retinal microvascular endothelial cells.

L-Glutamic γ-monohydroxamate是一种特异性抗肿瘤试剂，能够抑制癌细胞的增殖，并针对性地阻止微血管内皮细胞摄取L-组氨酸。作为钒配体，该化合物还能激活脂肪细胞对葡萄糖的摄取和代谢，进而有效降低血糖水平。

Drotrecogin alfa activated (DrotAA)为重组人活化蛋白C（APC）。该化合物能够抑制由烟雾引起的大鼠肺微血管通透性上升及促炎细胞因子IL-1β水平增加，具有抗凝血与抗炎作用，并促进纤溶过程。Drotrecogin alfa activated主要用于重症脓毒症的实验研究。

E70K是一种抑制趋化因子(C-X-C)配体8 (CXCL8)与细胞膜外的糖胺聚糖(GAGs)之间相互作用的抑制剂。它对应于CXCL8 C末端GAG结合区的氨基酸序列，并在第70位上含有谷氨酸到赖氨酸的替换。在50 nM浓度下，E70K能够抑制初级人类中性粒细胞与人类脐静脉内皮细胞(HUVECs)的结合。当使用浓度范围为1至1,000 nM时，它能降低CXCL8诱导的初级人类中性粒细胞通过HMEC-1人类微血管内皮细胞层的跨内皮迁移。

Zofenoprilat是一种血管紧张素转换酶(ACE; IC50 = 8 nM for the rabbit lung enzyme)的抑制剂，同时也是前体药zofenopril的活性代谢产物。它能够抑制分离的豚鼠小肠中由血管紧张素I或缓激肽诱导的收缩(EC50s = 3 and 1 nM, respectively)。在人类脐静脉内皮细胞(HUVECs)中，Zofenoprilat (10 nM)降低基础内皮素-1分泌和一氧化氮(NO)生成，并阻止TNF-α诱导的活性氧种(ROS)增加以及谷胱甘肽(GSH)水平降低。Zofenoprilat (10 µM)保护初级人类心脏微血管内皮细胞免受多柔比星诱导的细胞毒性。此外，Zofenoprilat (10 µM)还能增加HUVECs中的硫化氢(H2S)生成，以及细胞的黏着、迁移和增殖。在以400 µM浓度使用时，它可以减少Langendorff分离的大鼠心脏灌流缺血再灌注损伤模型中的舒张末压和乳酸脱氢酶(LDH)释放。

(±)17(18)-EpETE-Ethanolamide, an ω-3 endocannabinoid epoxide, originates from eicosapentaenoic ethanolamide (EPEA) through cytochrome P450 (CYP) epoxygenases action and is decomposed by soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FA, AH). Its endogenous synthesis occurs in LPS-stimulated and EPEA-supplemented BV-2 microglia cells, a process inhibited by the CYP inhibitor ketoconazole. This compound mitigates IL-6 and nitrite levels while enhancing IL-10 production following LPS exposure in BV-2 microglia. At a dose of 50 µM, it prevents platelet aggregation caused by arachidonic acid but not that triggered by ADP, collagen, or ristocetin. Additionally, it facilitates the dilation of constricted bovine coronary arteries (ED50= 1.1 µM) and blocks VEGF-driven tubulogenesis in human microvascular endothelial cells (HMVECs).

LY 379196 作为一种PKC-β抑制剂，展现出对PKC βI 和 βII 的高效抑制作用，其IC50分别为50 nM和30 nM。此化合物能够有效抑制由VEGF、IGF-1 和 bFGF 诱导的牛视网膜微血管内皮细胞 (BREC) 的增殖，常用于增生性视网膜病变研究中作为抗增殖剂。

Crenulatin(大花红天素)是一种天然的没食子单宁，对小鼠脑微血管内皮细胞凋亡的影响呈双向变化，通过调节 Fas Bcl-2 表达和 caspase-3 活性发挥作用。