36
11
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3638 |
Leukadherin-1
|
Integrin; Complement System | Cytoskeletal Signaling; Immunology/Inflammation |
Leukadherin-1 是 CD11b/CD18 的变构激活剂,可增加 CD11b/CD18 依赖性细胞对纤维蛋白原的粘附,减少白细胞运动和跨内皮迁移,具有抗炎作用。 | |||
T4435 |
E7820
ER68203-00 |
Integrin | Cytoskeletal Signaling |
E7820 (ER68203-00) 是具有口服活性芳香族磺酰胺衍生物,是一种血管生成抑制剂,可抑制内皮上整合素 α2 亚基的表达。它调节 α1,α2,α3 和 α5 整联素 mRNA 表达,具有抗血管生成和抗肿瘤活性。它抑制大鼠主动脉血管生成,IC50为 0.11 μg/ml。 | |||
T14942 |
CGP48369
|
RAAS | Endocrinology/Hormones |
CGP48369 是一种有效的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂,具有降血压作用,可增强自发性高血压大鼠冠状动脉的内皮依赖性松弛。 | |||
T16571 |
Pranidipine
普拉地平,OPC-13340 |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Pranidipine (OPC-13340) 是一种高效且长效的 1,4-二氢吡啶钙通道阻滞剂,可延长乙酰胆碱诱导的内皮松弛以及硝酸甘油诱导的内皮松弛,具有抗高血压作用。 | |||
T34541 |
SB-209670
SB 209670 |
Endothelin Receptor | GPCR/G Protein |
SB-209670是一种选择性内皮素受体拮抗剂,能够抑制大鼠血管内皮和血管平滑肌中ET(B)受体的活性。 | |||
T0370 |
Pheniramine maleate
Daneral,Inhiston,Trimetose,马来酸非尼拉敏 |
5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物,可与组胺 H1 受体结合,从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。 | |||
T4567 |
Sulfaphenazole
Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide |
P450; Antibacterial | Metabolism; Microbiology/Virology |
Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂,抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应,增加 AP-1的氧化应激和激活。 | |||
TP1277 |
Bradykinin
缓激肽 |
Endogenous Metabolite; Bradykinin Receptor | GPCR/G Protein; Metabolism |
Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。 它是炎症调节因子和神经调节因子,对几种血管和肾功能也有调节作用。 | |||
T6264 |
Bosentan
Actelion,波生坦,Ro 47-0203,Benzenesulfonamide |
Endothelin Receptor | GPCR/G Protein |
Bosentan (Benzenesulfonamide) 是 endothelin-1 (ET)拮抗剂,在人的 SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。 | |||
T27574 |
ZM 169369
ICI169369,ICI-169369 |
||
ICI 169369, a 5-HT2/5-HT1C antagonist, can evoke endothelium-dependent relaxation in rabbit aorta. | |||
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 | |||
T25748 |
L-Nabe
N(w)-nitroarginine benzyl ester,H-Arg(NO2)-Obzl,N-Nitro-L-argininebenzyl ester,NABE,Benzyl Nw-nitro-L-argininate |
Others | Others |
L-Nabe (H-Arg(NO2)-Obzl) 是一种有效的不可逆内皮依赖性舒张抑制剂。 | |||
T83164 |
Adrenomedullin (porcine)
|
||
Adrenomedullin(porcine)是一種多肽,具有调节血管舒张的功能。它在内皮依赖性条件下能诱导大鼠主动脉舒张,IC50为2.4 nM;在内皮非依赖性条件下则能诱导猪冠状动脉舒张,IC50为27.6 nM。 | |||
TP1919 |
Ac2-12
|
||
Annexin/lipocortin 1-mimetic peptide; inhibits leukocyte extravasation. Reduces neutrophil adhesion and emigration, and promotes detachment of neutrophils from activated mesenteric endothelium in mice in vivo. | |||
T76421 |
Protein Kinase C β Peptide
|
||
Protein Kinase C β Peptide为Protein Kinase Cβ的多肽片段,与高血糖降低内皮源性一氧化氮(NO)生成相关。抑制Protein Kinase Cβ能够减轻急性高血糖导致的内皮依赖性血管舒张功能障碍。 | |||
T36151 |
14,15-EE-8(Z)-E
|
||
Epoxyeicosatrienoic acids (EETs), such as 11(12)-EET and 14(15)-EET, are cytochrome P450 metabolites of arachidonic acid that have been identified as endothelium-derived hyperpolarizing factors with vasodilator activity. 14,15-EE-8(Z)-E is a structural analog of 14(15)-EET that demonstrates potent vasodilator agonist activity in bovine coronary arteries similar to that of 14(15)-EET. | |||
T75154 | ATU027 | ||
ATU027, 一种可沉默血管内皮中PKN3表达的siRNA, 已在小鼠癌症模型中证明能有效抑制局部肿瘤侵袭及淋巴结和肺转移。 | |||
T70903 |
KRH102053
|
||
KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells. | |||
T76841 | Enlimomab | ||
Enlimomab (BI-RR 0001) 是一种针对人 ICAM-1的小鼠 IgG2a 单抗,可抑制白细胞粘附到血管内皮,从而减少白细胞外渗漏和炎症性组织损伤。Enlimomab 具有抗炎作用,可用于中风研究。 | |||
T67212 | Ligustrazine HCl | ||
Ligustrazine Hydrochloride, is a natural substance discovered in the plant Ligusticum chuanxiong Hort. It inhibits platelet aggregation, improves atherosclerosis situation, protects endothelium injury, and has antithrombotic effects.in vivo,ligustrazine hydrochloride at 10 and 20 mg/kg produced significant analgesic effects against mechanical stimuli,and ligustrazine hydrochloride at 80 mg/kg, also significantly alleviated cold hypersensitivity manifested by reduction in cold vocalization temper... | |||
T68511 |
KRH102140
|
||
KRH102140 is a potent activator of PHD2. KRH102140, which has a structure similar to KRH102053. KRH102140 more efficiently suppressed HIF-1α than KRH102053 in human osteosarcoma cells under hypoxia. Furthermore, KRH102140 decreased the mRNA levels of HIF-regulated downstream target genes associated with angiogenesis and energy metabolism such as vascular endothelial growth factor, adrenomedullin, Glut1, aldolase A, enolase 1 and monocarboxylate transporter 4. KRH102140 also inhibited tube format... | |||
T41251 |
Taprostene
|
||
Taprostene (CG-4203) 是一种合成的、化学稳定的前列环素 (PGI2) 类似物。Taprostene 对猫急性心肌缺血再灌注后内皮和心肌有保护作用。Taprostene 增强细胞保护作用,同时减少不必要的血液动力学影响。 | |||
T36150 |
14,15-EE-5(Z)-E
|
||
Epoxyeicosatrienoic acids (EETs), such as 11(12)-EET and 14(15)-EET, are cytochrome P450 metabolites of arachidonic acid that have been identified as endothelium-derived hyperpolarizing factors with vasodilator activity. 14,15-EE-5(Z)-E is a structural analog of 14,15-epoxyeicosatrienoic acids (14,15-EET) that antagonizes EET-induced relaxation of vascular smooth muscle. Relaxation of U46619-constricted bovine arteries by 14,15-EET could be inhibited approximately 80% by 14,15-EE-5(Z)-E at a con... | |||
T35600 |
NO-Losartan A
|
||
Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1) receptor. Losartan is a mammalian AT1 receptor antagonist with a Ki value of 5-20 nM. In humans, losartan effectively controls hypertension while protecting renal function. Nitric oxide (NO) causes vasodi... | |||
T37238 |
(±)19(20)-EpDPA
|
||
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic... | |||
T37234 |
(±)14(15)-EpETE
|
||
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoi... | |||
T35464 |
(±)14(15)-EET-SI
|
||
Arachidonic acid is metabolized in the vascular endothelium to epoxytrienoic acids (EETs or EpETrEs) by cytochrome P450 enzymes. The EETs are released in response to acetylcholine, bradykinin, arachidonic acid, or cyclic stretch. (±)14(15)-EET-SI is the methyl sulfonamide analog of 14(15)-EET. This substitution results in a metabolically more stable compound because it is not sensitive to β-oxidation or membrane esterification. (±)14(15)-EET-SI is equipotent to 14(15)-EET in vascular agonist act... | |||
T82683 |
Connexin mimetic peptide 40GAP27
|
||
Connexin mimetic peptide 40GAP27 是一种生物活性肽,对应于主要的血管连接蛋白Cx40第二个细胞外环的GAP27结构域(40Gap27)。该化合物在研究氧化应激所致的损伤以及间隙连接通讯机制中有应用。40Gap27能够在给药后减少内皮依赖性的内膜下平滑肌的超极化现象。 | |||
T37235 |
(±)16(17)-EpDPA
(±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA |
||
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahex... | |||
T70456 |
Nolpitantium Free Base
|
||
Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no eff... | |||
T36074 |
S-NEPC
|
||
Cytochrome P450 metabolites of arachidonic acid, such as 11(12)-EpETrE and 14(15)-EpETrE have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EpETrEs to the corresponding DiHETrEs thereby diminishing their activity. Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation. S-NEPC is a colorimetric substrate used to measure sEH activity. It also is... | |||
T37969 |
12(S)-HpETE
|
||
12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LO, resulting in the synthesis of 5(S)-HETE, leukotriene B4 (LTB4), and 5(S),12(S)-DiHETE. Rat lung metabolizes 12(S)-HpETE to 8,11,12- and 10,11,12-trihydroxyeicostrienoic acids. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and e... | |||
T35598 |
Neuromedin U-25 (human) (trifluoroacetate salt)
|
||
Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery ... | |||
T82789 |
Caloxin 1B1
|
||
Caloxin 1B1是一种对PMCA4亲和力高的生物活性肽。该化合物是经由筛选与PMCA4胞外结构域1的结合而发现,能够特异性地在胞外环境中抑制PMCA。鉴于Caloxin 1B1被筛选用于与PMCA的细胞外结构域相结合,它可以被直接应用于细胞和组织中,用以评估其对平滑肌和内皮细胞功能的影响。 | |||
T82684 |
Connexin mimetic peptide 40,37GAP26
|
||
Connexin mimetic peptide 40,37GAP26是一种生物活性肽,对应Cx37和Cx40主要血管连接蛋白的胞外环GAP26结构域,命名基于Cx同源性为37,40Gap26。本化合物主要用于研究间隙连接对环吡嗪酸(CPA)通过啮齿动物髂动脉壁导致的内皮超极化扩散的影响。Cx37和Cx40形成的间隙连接斑块在内皮细胞中高度丰富,而Connexin mimetic peptide 40,37GAP26能抑制内膜下超极化。 | |||
T37495 |
Angiotensin (1-7) (acetate)
|
||
Angiotensin 1-7 (Ang-(1-7)) acetate 是RAS中的一种内源性七肽,具备心脏保护作用,主要表现为对心肌细胞的抗炎与抗纤维化活性。该化合物能抑制纯化的犬ACE活性(IC50=0.65 μM),通过降低ACE活性并促进一氧化氮释放,作为血管舒张调节的局部协同因子。此外,Angiotensin 1-7 acetate 可阻止血管紧张素Ⅱ诱发的平滑肌细胞增殖和肥大,同时对内皮细胞表现出抗血管生成和生长抑制作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3927 |
Phellopterin
|
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
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。 | |||
TMS2171 |
(±)-Naringenin
(±)-柚皮素,Salipurpol,柚皮素,Naringenine,Naringenin |
Potassium Channel | Membrane transporter/Ion channel |
(±)-Naringenin (Naringenine) 是一种天然的类黄酮。它通过激活肌细胞中 BKCa 通道发挥对内皮剥脱血管的舒张作用。 | |||
T38248 |
2-Ethylpyrazine
|
Endogenous Metabolite; NO Synthase | Immunology/Inflammation; Metabolism |
2-Ethylpyrazine 存在与烘焙后的咖啡豆中,是一种挥发性化合物 。2-Ethylpyrazine 通过内皮衍生的松弛因子的活动诱导血管舒张。2-Ethylpyrazine 通过内皮内皮NO 合酶的作用激活NO 合成。2-Ethylpyrazine 通过诱导NO 释放和增加外周血流量来诱导血管舒张。 | |||
T37974 |
(S)-Coriolic acid
13(S)-HODE |
Lipoxygenase; Mitochondrial Metabolism; PPAR | DNA Damage/DNA Repair; Metabolism |
(S)-Coriolic acid (13(S)-HODE) 是一种重要的细胞内信号剂,是亚油酸与植物和哺乳动物脂氧合酶反应生成的,在各种生物系统中参与细胞增殖和分化。(S)-Coriolic acid 在 1 μM 左右时,它能抑制肿瘤细胞与血管内皮的粘附,能下调 IRGpIIb/IIIa 受体的表达。(S)-Coriolic acid 是15-脂氧合酶 (15-LOX) 代谢产物,常作为内源性配体激活 PPARγ。(S)-Coriolic acid 诱导线粒体功能障碍 和气道上皮损伤。 | |||
T4809 |
Pyrimidine
嘧啶,Metadiazine |
Others; Endogenous Metabolite | Metabolism; Others |
Pyrimidine (Metadiazine) 是内源性代谢产物的一种。 | |||
TN1567 |
Delphinidin chloride
|
Estrogen Receptor/ERR; VEGFR | Angiogenesis; Endocrinology/Hormones; Tyrosine Kinase/Adaptors |
Delphinidin chloride 是一种花青素,是一种可从浆果和红酒中分离得到的天然植物色素,是某些花青素的前体。Delphinidin chloride 诱导血管内皮释放一氧化氮,引起血管松弛。在1 ~ 40 μM 剂量下,对上皮生长因子受体的信号传导和雌激素受体α的表达有抑制作用,与细胞凋亡和自噬有关。Delphinidin chloride 能调节 JAK/STAT3 和 MAPKinase 信号传导。Delphinidin 还能抑制 p300/CBP 的组蛋白乙酰转移酶活性(IC50 在约为30 μM) | |||
T3794 |
Pentagalloylglucose
Penta-O-galloyl-β-D-glucose,1,2,3,4,6-O-Pentagalloylglucose,1,2,3,4,6-Penta-O-galloyl-beta-D-glucopyranose,1,2,3,4,6-五没食子酰葡萄糖 |
Influenza Virus | Microbiology/Virology |
1,2,3,4,6-O-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) 存在于多种植物中,具有重要的药理作用。Pentagalloylglucose 表现出显著的抗狂犬病病毒 (RABV) 活性。 | |||
TN1246 | 3-Deoxysappanone B | Others | Others |
3-Deoxysappanone B has vasorelaxation effects, it can mediate endothelium- independent vasodilator action in rat thoracic aortic rings. | |||
TN2534 |
1-Hydroxy-2,3,5-trimethoxyxanthone
|
IκB/IKK; Calcium Channel; NOS; 5-HT Receptor; COX | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) has vasodilator action ,which involves both an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx through L-type voltage-operated Ca(2+) channels; a minor contribution to the effects of HM-1 may be related to inhibition of the protein kinase C-mediated release of intracellular Ca(2+) stores. HM-1,at the concentration of 1 ug/mL, can effectively inhibit the osteoclast differentiation in a co-c... | |||
TN4819 | (-)-Praeruptorin A | ATPase; IL Receptor; Calcium Channel; P-gp | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience |
(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings dependent on endothelium and nitric oxide synthesis;it also can significantly suppress airway inflammation and airway remodeling induced by ovalbumin challenge, and is a potential candidate for the treatment of asthma. (-)-Praeruptorin A resensitizes Pgp-mediated MDR (Pgp-MDR) cancer cells to cancer drugs. | |||
T81324 |
Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside
|
||
Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside 是一种从天竺葵属植物中分离的酚类化合物,具有口服活性和抗炎特性,可能在治疗水肿和改善主动脉内皮依赖性舒张损伤方面有应用潜力。 |