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16

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21807	INCA-6 Triptycene-1,4-quinone	Others	Others
	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。
T2690	Tranilast 曲尼司特,MK 341,SB 252218	RAAS; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	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。
T0259	Chromocarb Chromone-2-carboxylic acid,色烯卡,Chromocarbe	Others	Others
	Chromocarb (Chromone-2-carboxylic acid) 是合成的血管保护剂。
T33389	Minalrestat ARI509,WAY-121509,WAY121509,WAYARI-509,ARI-509,WAY-ARI-509	Reductase	Endocrinology/Hormones; Metabolism
	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。
T11318	Dopexamine hydrochloride 盐酸多培沙明,FPL60278AR	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Dopexamine hydrochloride (FPL60278AR) 是β2肾上腺素能受体激动剂。
T60396	JMS-053	Phosphatase	Metabolism
	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。
T3560	Desmethylanethol trithione ADT-OH	VEGFR; Akt	Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	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。
T71488	Cremastranone
	Cremastranone is a natural antiangiogenic homoisoflavanone. Cremastranone inhibits the proliferation, migration, and tube formation ability of human retinal microvascular endothelial cells.
T26589	Albifylline
	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
T27790	Labradimil RMP-7,ALK-01-040,Receptor-mediated permeabiliser-7,DRG0182,DRG 0182,DRG-0182
	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
T81935	L-Glutamic γ-monohydroxamate
	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。
T82526	Drotrecogin alfa (activated)
	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。
T36232	20-carboxy Arachidonic Acid
	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-A...
T35468	(±)19(20)-EDP Ethanolamide
	(±)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-...
T83702	E70K TFA
	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。
T83768	Zofenoprilat Zofenopril-SH,SQ 26,333
	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。

化合物

Cat.No: T21807

Synonym: Triptycene-1,4-quinone

Target: Others

Cat.No: T2690

Synonym: 曲尼司特,MK 341,SB 252218

Target: RAAS, Prostaglandin Receptor

Cat.No: T0259

Synonym: Chromone-2-carboxylic acid,色烯卡,Chromocarbe

Target: Others

Cat.No: T33389

Synonym: ARI509,WAY-121509,WAY121509,WAYARI-509,ARI-509,WAY-ARI-509

Target: Reductase

Dopexamine hydrochloride

Cat.No: T11318

Synonym: 盐酸多培沙明,FPL60278AR

Target: Adrenergic Receptor

Cat.No: T60396

Target: Phosphatase

Desmethylanethol trithione

Cat.No: T3560

Synonym: ADT-OH

Target: VEGFR, Akt

Cat.No: T71488

Cat.No: T26589

Cat.No: T27790

Synonym: RMP-7,ALK-01-040,Receptor-mediated permeabiliser-7,DRG0182,DRG 0182,DRG-0182

L-Glutamic γ-monohydroxamate

Cat.No: T81935

Drotrecogin alfa (activated)

Cat.No: T82526

20-carboxy Arachidonic Acid

Cat.No: T36232

(±)19(20)-EDP Ethanolamide

Cat.No: T35468

Cat.No: T83702

Cat.No: T83768

Synonym: Zofenopril-SH,SQ 26,333

Cat. No.	Product Name	Target	Signaling Pathways
T3S1513	(20R)-Protopanaxadiol Protopanaxadiol,20R-Protopanaxadiol,(20R)-原人参二醇,(20R)-Protopanaxdiol	Others; Antibacterial	Microbiology/Virology; Others
	(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。
T0530	Flavanone 2-Phenyl-4-chromanone,4-Flavanone,2,3-Dihydroflavone,黄烷酮,2-Phenylchroman-4-one	Others; Aromatase	Endocrinology/Hormones; Others
	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。
T5S2347	Deoxyshikonin 去氧紫草素,Arnebin 7	Others; HIF/HIF Prolyl-Hydroxylase; Antibacterial	Chromatin/Epigenetic; Metabolism; Microbiology/Virology; Others
	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。
T40942	(R)-(4′-Hydroxy)-5,7-dihydroxy-4-chromanone
	(R)-(4′-Hydroxy)-5,7-dihydroxy-4-chromanone, an antiangiogenic homoisoflavonoid, exhibits activity against human retinal microvascular endothelial cells.
TN1532	Crenulatin	BCL; Caspase	Apoptosis; Proteases/Proteasome
	Crenulatin has dual- direction effects on apoptosis of cerebral microvascular endothelial cells, inhibitive effect in 25 mg/L and stimulative effect in 100 mg/L group, respectively; the mechanism is related to the alterations of Fas/Bcl-2 expression and caspase-3 activity.
TN5942	Dammarenediol II 达玛烯二醇II,Dammar-24-ene-3,20-diol
	Dammarenediol II may have the ability to prevent diabetic microvascular complications, including diabetic retinopathy, it can inhibit vascular endothelial growth factor (VEGF)-induced intracellular reactive oxygen species generation and stress fiber forma

天然产物

(20R)-Protopanaxadiol

Cat.No: T3S1513

Synonym: Protopanaxadiol,20R-Protopanaxadiol,(20R)-原人参二醇,(20R)-Protopanaxdiol

Target: Others, Antibacterial

Cat.No: T0530

Synonym: 2-Phenyl-4-chromanone,4-Flavanone,2,3-Dihydroflavone,黄烷酮,2-Phenylchroman-4-one

Target: Others, Aromatase

Cat.No: T5S2347

Synonym: 去氧紫草素,Arnebin 7

Target: Others, HIF/HIF Prolyl-Hydroxylase, Antibacterial

(R)-(4′-Hydroxy)-5,7-dihydroxy-4-chromanone

Cat.No: T40942

Cat.No: TN1532

Target: BCL, Caspase

Dammarenediol II

Cat.No: TN5942

Synonym: 达玛烯二醇II,Dammar-24-ene-3,20-diol

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