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Search Results for " vascular permeability "

21

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8844	Diflapolin	Others; FLAP; Epoxide Hydrolase	Immunology/Inflammation; Metabolism; Others
	Diflapolin 是高活性的双 5-脂氧合酶激活蛋白(FLAP)/可溶性环氧化物水解酶抑制剂，具有显著的抗炎作用和较高的靶向选择性。它抑制分离的 sEH 的活性，IC50为20 nM。它还抑制完整人单核细胞和中性粒细胞中 5-LOX 产物的形成，IC50分别为 30 和 170 nM。
T2456	Tivozanib 替沃扎尼,AV-951,KRN951	VEGFR; PDGFR; Ephrin Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	Tivozanib (KRN951) 是一种选择性的 VEGFR 1/2/3抑制剂，它们的 IC50值分别为0.21 nM、0.16 nM、0.24 nM。
T5194	SPHINX31	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	SPHINX31 是丝氨酸/富含精氨酸的蛋白激酶1的选择性抑制剂，其IC50值为 5.9 nM。它有效抑制丝氨酸/丰富精氨酸的剪接因子1 磷酸化，有用于局部新生血管性眼病的研究潜力。
T63505	Tivozanib hydrochloride hydrate
	Tivozanib hydrochloride hydrate 是选择性的、有效的、口服具有活力的 VEGFR 酪氨酸激酶抑制剂，能够作用于 VEGFR-1 (IC50: 0.21 nM)、VEGFR-2 (IC50: 0.16 nM)、VEGFR-3 (IC50: 0.24 nM)。Tivozanib hydrochloride hydrate 能够抑制肿瘤组织中的血管生成和血管通透性，并具有抗肿瘤作用，对转移性肾细胞癌 (RCC) 具有研究潜力。
T6529	Halobetasol propionate 卤贝他索丙酸酯,Halobetasol Propionate,Ulobetasol propionate,BMY-30056,卤倍他索丙酸酯,CGP-14458	Phospholipase	Metabolism
	Halobetasol propionate (BMY-30056) 是一种在皮肤外使用的合成类固醇，具有抗炎，止痒和收缩血管的活性。
T2403	Bromfenac sodium hydrate Bromfenac sodium,Bromfenac monosodium salt sesquihydrate,溴芬酸钠	COX	Immunology/Inflammation; Neuroscience
	Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) 是一种可口服的 COX 抑制剂，抑制 COX-1和COX-2的IC50值分别为 5.56 和 7.45 nM。它是一种溴化非甾体类抗炎药，有用于白内障的术后炎症和疼痛以及假晶状体囊状黄斑水肿的研究。
T16344	NS-2028	Others; Guanylate cyclase	GPCR/G Protein; Others
	NS-2028 是一种高度选择性的可溶性鸟苷酸环化酶抑制剂。它抑制 3-吗啉代-sydnonimine 在人培养的脐静脉内皮细胞中形成环状 GMP，IC50为30mM。它抑制小鼠小脑匀浆和神经元 NO 合酶中的可溶性鸟苷酸环化酶活性，IC50分别为 17 和 20 mM。它可降低血管内皮生长因子诱导的血管生成和通透性。
T3979	Emedastine LY188695,依美斯汀,Emadine	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Emedastine (LY188695) 是一种可口服的，选择性和高亲和力的组胺 H1受体拮抗剂，Ki 值为 1.3 nM。它是苯并咪唑衍生物，可用于过敏性鼻炎、过敏性皮肤疾病和过敏性结膜炎的研究。
T32681	Leukotriene F-4 sulfone Ltf4 sulfone
	Leukotriene F-4 sulfone induces vascular permeability changes.
T26491	AA 2379 AA2379,AA-2379
	AA 2379, an anti inflammatory agent, inhibits the vascular permeability induced by histamine, serotonin, and bradykinin. It also has some analgesic activity.
T21388	Emedastine Difumarate Rapimine,DSSTox_CID_26911,AL-3432A,富马酸依美斯汀,KB-2413,Emedastine fumarate,KB 2413
	Emedastine Difumarate is a selective histamine H1 receptor antagonist with anti-allergic activity, prescribed for allergic conjunctivitis. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeabil
T71722	Angiogenesis inhibitor BT2
	Angiogenesis inhibitor BT2 is a novel inhibitor of angiogenesis and vascular permeability, inhibiting ERK phosphorylation and the expression of FosB/ΔFosB, VCAM-1, and many genes involved in proliferation, migration, angiogenesis, and inflammation, interacting with MEK1, suppressing retinal CD31, pERK, VCAM-1, and VEGF-A165 expression.
T37261	14,15-Leukotriene D4 14,15-Leukotriene D4
	14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both ...
T76895	Abicipar pegol
	Abicipar pegol (AGN-150998, MP0112) 是一种抗VEGFDARPin 分子，DARPin 分子是一类新型的小蛋白，含有工程化的 ankyrin 重复结构域，以高特异性和亲和力与靶蛋白结合。Abicipar pegol 可有效抑制血管生成和血管通透性，通过玻璃体内注射，降低平均视网膜厚度和渗漏面积，用于眼部炎症等相关疾病研究。
T37620	Leukotriene C4 methyl ester
	Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute all...
T70906	EHT-6706
	EHT-6706 is a novel microtubule-disrupting agent that targets the colchicine-binding site to inhibit tubulin polymerization. At low nM concentrations, EHT 6706 exhibits highly potent antiproliferative activity on more than 60 human tumor cell lines, even those described as being drug resistant. EHT 6706 also shows strong efficacy as a vascular-disrupting agent, since it prevents endothelial cell tube formation and disrupts pre-established vessels, changes the permeability of endothelial cell mon...
T77089	Mirococept
	Mirococept (APT070) 是一种抗体，靶向补体系统 (complement system) 的 C3b/C4b，也是一种膜定位的 C3转化酶抑制剂。Mirococept 减少 C 肽和促炎细胞因子的释放，并减少炎症细胞的浸润。Mirococept 减少胰岛内炎症，有利于胰岛移植。Mirococept 还抑制增加的肠和肺血管通透性以减少中性粒细胞流入。
T21547	PAF (C16) C16-PAF	ERK; MEK; MAPK; Endogenous Metabolite	MAPK; Metabolism
	PAF (C16) 是有效的 MAPK 和 MEK/ERK 激活剂，可诱导血管通透性增加。PAF (C16) (PAF (C16)) 是血小板活化因子，是一种磷脂衍生介质，也是 PAF G 蛋白偶联受体 (PAFR) 的配体。PAF (C16) 在体外实验中显示出抗凋亡和抗炎活性，通过与其受体（PAF-R）相互作用以执行细胞信号传导来抑制 caspase 依赖性凋亡。
T37262	14,15-Leukotriene E4 14,15-Leukotriene E4
	Leukotrienes (LTs) are a group of acute inflammatory mediators derived from arachidonic acid in leukocytes. The majority of these metabolites are formed through the 5-lipoxygenase (5-LO) pathway. 14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-LOs on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. These metabolites are classified as eoxins because they are formed mostly by eosinophils...
T80265	C5a Receptor agonist, mouse, human	Complement System	Immunology/Inflammation
	C5a Receptor agonist, mouse, human 是一种源自血浆蛋白C5a C末端的生物活性肽，充当C5a受体激动剂。此化合物在调控细胞炎症反应中起关键作用，包括促进趋化性、白细胞脱颗粒、增加血管通透性以及刺激细胞因子的产生。化合物的结构中，第5位环己基丙氨酸对激动剂功能至关重要，同时末端的Arg采用d-异构体形式。
T38128	Leukotriene D4 Leukotriene D4 MaxSpec® Standard,LTD4
	Leukotriene D4 (LTD4) is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. It is the first cysteinyl-leukotriene metabolite of LTC4 . Like LTC4, LTD4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute hypersensitivity. LTD4 is equipotent to LTC4 in its biological activities, except that LTD4 is nearly 100-fold more effective in the contraction of...

化合物

Cat.No: T8844

Target: Others, FLAP, Epoxide Hydrolase

Cat.No: T2456

Synonym: 替沃扎尼,AV-951,KRN951

Target: VEGFR, PDGFR, Ephrin Receptor

Cat.No: T5194

Target: Serine/threonin kinase

Tivozanib hydrochloride hydrate

Cat.No: T63505

Halobetasol propionate

Cat.No: T6529

Synonym: 卤贝他索丙酸酯,Halobetasol Propionate,Ulobetasol propionate,BMY-30056,卤倍他索丙酸酯,CGP-14458

Target: Phospholipase

Bromfenac sodium hydrate

Cat.No: T2403

Synonym: Bromfenac sodium,Bromfenac monosodium salt sesquihydrate,溴芬酸钠

Target: COX

Cat.No: T16344

Target: Others, Guanylate cyclase

Cat.No: T3979

Synonym: LY188695,依美斯汀,Emadine

Target: Histamine Receptor

Leukotriene F-4 sulfone

Cat.No: T32681

Synonym: Ltf4 sulfone

Cat.No: T26491

Synonym: AA2379,AA-2379

Emedastine Difumarate

Cat.No: T21388

Synonym: Rapimine,DSSTox_CID_26911,AL-3432A,富马酸依美斯汀,KB-2413,Emedastine fumarate,KB 2413

Angiogenesis inhibitor BT2

Cat.No: T71722

14,15-Leukotriene D4

Cat.No: T37261

Synonym: 14,15-Leukotriene D4

Cat.No: T76895

Leukotriene C4 methyl ester

Cat.No: T37620

Cat.No: T70906

Cat.No: T77089

Cat.No: T21547

Synonym: C16-PAF

Target: ERK, MEK, MAPK, Endogenous Metabolite

14,15-Leukotriene E4

Cat.No: T37262

Synonym: 14,15-Leukotriene E4

C5a Receptor agonist, mouse, human

Cat.No: T80265

Target: Complement System

Cat.No: T38128

Synonym: Leukotriene D4 MaxSpec® Standard,LTD4

Cat. No.	Product Name	Target	Signaling Pathways
T5S1889	Yunaconitine Guayewuanine B,滇乌头碱	Others	Others
	Yunaconitine (Guayewuanine B) 是一种乌头类生物碱，具有剧毒。
T2520	Desloratadine Sch34117,地氯雷他定,NSC 675447	Endogenous Metabolite; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Desloratadine (Sch34117) 是非镇静H1抗组胺药 Loratadine 的主要口服代谢物，可减少对支气管平滑肌、毛细血管和胃肠道平滑肌中 H1 受体的典型组胺能作用，包括血管舒张、支气管收缩、血管通透性增加、疼痛、瘙痒和胃肠道平滑肌的痉挛性收缩。它是一种选择性H1受体拮抗剂，具有抗过敏和抗炎活性。
TN5575	Coronarin D methyl ether
	Coronarin D methyl ether has inhibitory effects on the increase in vascular permeability, nitric oxide production, and inducible nitric oxide synthase induction.

天然产物

Cat.No: T5S1889

Synonym: Guayewuanine B,滇乌头碱

Target: Others

Cat.No: T2520

Synonym: Sch34117,地氯雷他定,NSC 675447

Target: Endogenous Metabolite, Histamine Receptor

Coronarin D methyl ether

Cat.No: TN5575

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