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Search Results for " vasculature "

12

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0119	Nitrendipine BAY-E-5009,Bayotensin,尼群地平	Calcium Channel; Autophagy	Autophagy; Membrane transporter/Ion channel; Metabolism
	Nitrendipine (BAY-E-5009) 是 Nifedipine 的类似物，是一种钙通道阻滞剂，具有显着的血管扩张作用。它是一种有效的抗高血压药且不会降低肾小球滤过率，并且具有轻微的利钠作用。
T3216	Selexipag NS-304,ACT-293987,赛乐西帕,Uptravi	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	Selexipag (ACT-293987) 是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。
T16859	SBI-425	Others	Others
	SBI-425 是一种有效且具有口服生物利用度的 TNAP 抑制剂。 SBI-425 有效抑制脉管系统中的 TNAP，改善心血管参数和存活率，而骨骼没有检测到变化。
T1608	ADH-1 trifluoroacetate Exherin trifluoroacetate	Dehydrogenase	Metabolism
	ADH-1 trifluoroacetate (Exherin trifluoroacetate) 是一种选择性的、竞争性N-钙粘蛋白拮抗剂，具有潜在抗肿瘤和抗血管生成作用。
T2090	Lexibulin CYT-997	Apoptosis; Reactive Oxygen Species; Microtubule Associated	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; NF-κB
	Lexibulin (CYT-997) 是一种微管蛋白聚集强效抑制剂，可诱导细胞凋亡，并诱导 GC 细胞中的线粒体ROS 生成。它对多种癌细胞的 IC50 值为 10-100n M，在体内外具有高细胞毒性和血管增生阻断作用。
T1577	Midodrine hydrochloride Pro-Amatine,盐酸米多君	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Midodrine hydrochloride (Pro-Amatine) 通过去甘氨酸反应转化为其活性代谢物 desglymidodrine。Desglymidodrine 选择性地结合并激活小动脉和静脉血管系统的 α-1-肾上腺素能受体。这会导致平滑肌收缩并导致血压升高。 Desglymidodrine 在血脑屏障中的扩散很差，因此与对中枢神经系统的影响无关。Midodrine hydrochloride 是 midodrine 的盐酸盐形式，是一种直接作用的前药和拟交感神经药，具有抗低血压特性。
T26905	BRL 55834 BRL55834,BRL-55834
	BRL 55834, a potassium channel activator, has shown to relax airways and vasculature in vivo.
T71032	Melafolone
	Melafolone is a natural dual inhibitor of cox-2 and egfr, improving program death 1 (pd-1) checkpoint blockade therapy through normalizing tumor vasculature and pd-l1 downregulation
T68317	VJ115
	VJ115 is a novel chemical entity that inhibits the enzyme ENOX1, a NADH oxidase. Genetic and small molecule inhibition of ENOX1 inhibits endothelial cell tubule formation and tumor-mediated neo-angiogenesis. Inhibition of ENOX1 radiosensitizes tumor vasculature, a consequence of enhanced apoptosis. VJ115 inhibition of ENOX1 can impact expression of proteins involved in cytoskeletal reorganization and support a hypothesis in which ENOX1 activity links elevated cellular NADH concentrations with cy...
T61604	PKC-IN-4
	PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]
T77031	Ifabotuzumab
	Ifabotuzumab (KB004) 是靶向 EphA3的 IgG1κ 抗体 (KD=610 pM)。Ifabotuzumab 能够导致肿瘤细胞凋亡，并激活抗体依赖性细胞介导的细胞毒作用 (ADCC)，破坏肿瘤脉管系统。Ifabotuzumab 能够减少人特发性肺纤维化 (IPF) CCR10+细胞，改善肺纤维化。
T68273	BNC105P
	BNC105P is a benzofuran-based vascular disrupting agent (VDA) prodrug with potential anti-vascular and antineoplastic activities. Upon administration vascular disrupting agent BNC105P, the disodium phosphate ester of BNC105, is rapidly converted to BNC105; in activated endothelial cells, BNC105 binds to tubulin and inhibits its polymerization, which may result in a blockage of mitotic spindle formation, cell cycle arrest, and disruption of the tumor vasculature. Hypoxic conditions ensue, deprivi...

化合物

Cat.No: T0119

Synonym: BAY-E-5009,Bayotensin,尼群地平

Target: Calcium Channel, Autophagy

Cat.No: T3216

Synonym: NS-304,ACT-293987,赛乐西帕,Uptravi

Target: Others, Prostaglandin Receptor

Cat.No: T16859

Target: Others

ADH-1 trifluoroacetate

Cat.No: T1608

Synonym: Exherin trifluoroacetate

Target: Dehydrogenase

Cat.No: T2090

Synonym: CYT-997

Target: Apoptosis, Reactive Oxygen Species, Microtubule Associated

Midodrine hydrochloride

Cat.No: T1577

Synonym: Pro-Amatine,盐酸米多君

Target: Adrenergic Receptor

Cat.No: T26905

Synonym: BRL55834,BRL-55834

Cat.No: T71032

Cat.No: T68317

Cat.No: T61604

Cat.No: T77031

Cat.No: T68273

Cat. No.	Product Name	Target	Signaling Pathways
T6272	Fosbretabulin Disodium Combretastatin A4 Phosphate,CA 4DP,CA 4P,福他布林,Combretastatin A4 disodium phosphate,Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Fosbretabulin Disodium (CA 4P) 是一种微管蛋白去稳定剂，是 Combretastatin A4 前药，可选择性靶向内皮细胞，诱导新生肿瘤新血管消退，减少肿瘤血流量并引起中央肿瘤坏死。
T2803	Monocrotaline 野百合碱,Crotaline	TGF-beta/Smad	Stem Cells
	Monocrotaline (Crotaline) 是一种吡咯里西啶生物碱，从猪屎豆植物的种子中提取得到，可诱导啮齿动物产生肺动脉高血压。
T6S1487	Ginsenoside Rg5 人参皂苷Rg5,人参皂甙 Rg5	NF-κB; COX; IGF-1R	Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors
	Ginsenoside Rg5 是红参的主要成分，可阻断IGF-1与其受体的结合，IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压，具有抗炎和治疗阿尔茨海默病的潜力。
T5S2343	Acetylshikonin 乙酰紫草素,Acetyl shikonin	Others; P450; AChE	Metabolism; Neuroscience; Others
	Acetylshikonin 来源于紫草根，具有抗癌、抗炎作用。它是一种 AChE 抑制剂，具有很强的抗凋亡活性。它是一种非选择性的细胞色素 P450抑制剂，对所有 P450 亚型抑制的 IC50值范围为 1.4-4.0 μM。

天然产物

Fosbretabulin Disodium

Cat.No: T6272

Synonym: Combretastatin A4 Phosphate,CA 4DP,CA 4P,福他布林,Combretastatin A4 disodium phosphate,Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Target: Apoptosis, Microtubule Associated

Cat.No: T2803

Synonym: 野百合碱,Crotaline

Target: TGF-beta/Smad

Ginsenoside Rg5

Cat.No: T6S1487

Synonym: 人参皂苷Rg5,人参皂甙 Rg5

Target: NF-κB, COX, IGF-1R

Cat.No: T5S2343

Synonym: 乙酰紫草素,Acetyl shikonin

Target: Others, P450, AChE

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