51
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T21965 |
MBCQ
|
PDE | Metabolism |
MBCQ 是选择性 cGMP 特异性磷酸二酯酶 (PDE V; PDE5) 抑制剂,IC50=19 nM。它通过特异性抑制 cGMP-PDE 来扩张冠状动脉。它对其他 PDE 同工酶没有抑制活性,IC50均大于 100 µM。 | |||
T11339 |
Furegrelate sodium
U-63557A |
PPAR | DNA Damage/DNA Repair; Metabolism |
Furegrelate sodium (U-63557A) 是口服有效的、血栓素合酶选择性抑制剂,抑制人血小板微粒体血栓素 A2 (TxA2) 合酶的 IC50为 15 nM。它正在开发作为抗血小板药物。 | |||
T22459 |
Xanthinol Nicotinate
Angioamin,烟酸占替诺,Complamin |
Others | Others |
Xanthinol Nicotinate (Complamin) 是血管扩张剂,可直接作用于小动脉和毛细血管的平滑肌,能够扩大血管,改善血液流变学并降低外周血管阻力。 | |||
T8236 |
RHC 80267
U-57908 |
Others; Phospholipase; COX; Acyltransferase; AChR | Immunology/Inflammation; Metabolism; Neuroscience; Others |
RHC 80267 (U-57908) 是一种选择性二酰基甘油脂酶(DAGL)抑制剂,对犬血小板的IC50为 4 μM。它抑制COX 活性和磷脂酰胆碱的水解,还抑制胆碱酯酶活性,IC50为 4 μM,增强乙酰胆碱引起的松弛。 | |||
T2441 |
TAS-301
TAS 301 |
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
TAS-301 是一种平滑肌迁移和增殖抑制剂,能够抑制 PDGF 诱导的 PKC 的活化,可抑制大鼠颈动脉球囊损伤后的内膜增厚。 | |||
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。 | |||
T0362 |
Ticlopidine hydrochloride
Ticlodone,Ticlopidine HCl,Ticlodix,盐酸噻氯匹定 |
Adenosine Receptor | GPCR/G Protein; Neuroscience |
Ticlopidine hydrochloride (Ticlodix) 是一种 ADP 受体抑制剂,对血小板凝集的IC50为2 μM。 | |||
T16669 |
PRX-08066
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
PRX-08066是5-HT 受体2B 拮抗剂,IC50为3.4 nM,可诱导肺动脉的选择性血管舒张。 | |||
T12478L |
Pinacidil
吡那地尔,S 1230,P 1134,S-1230,P-1134,P1134 |
Potassium Channel | Membrane transporter/Ion channel |
Pinacidil (P 1134) 是钾通道的有效激活剂。Pinacidil 通过打开 K+-通道使血管平滑肌超极化,显示出抗高血压活性。它显著改善再灌注功能和心脏顺应性。它具有直接的心脏保护作用。 | |||
T3996 |
Dapiprazole Hydrochloride
盐酸达哌唑,Glamidolo Hydrochloride,Reversil Hydrochloride |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Dapiprazole Hydrochloride (Glamidolo Hydrochloride) 是 α-adrenergic 阻断剂的药物。 | |||
T7391 |
SAR407899
|
ROCK; Rho | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SAR407899 是一种选择性的 ATP 竞争性ROCK 抑制剂,对ROCK-2的IC50值为 135 nM,对人和大鼠ROCK-2的Ki 值分别为 36 和 41 nM。它是 Rho 激酶抑制剂,有效抑制 endothelin-1 诱导的肾阻力动脉收缩。 | |||
T8960 |
MONNA
|
Chloride channel | Membrane transporter/Ion channel |
MONNA 是 TMEM16A (Anoctamin-1)阻滞剂,IC50为 80 nM。它在氯离子存在或不存在的情况下诱导啮齿动物抵抗动脉的血管舒张。 | |||
T5458 |
Darusentan
Lu-135252,达卢生坦 |
Endothelin Receptor | GPCR/G Protein |
Darusentan (Lu-135252) 是内皮素受体 A (ET-A) 受体选择性拮抗剂,能够作用于 ET-A 受体(Ki:1.4 nM)及ET-B 受体(Ki:184 nM),对 ETA 受体的选择性大于 ETB 受体的100以上。它在大鼠主动脉血管平滑肌细胞膜中竞争结合放射性标记的内皮素(Ki:13 nM)。 | |||
T63349 |
Treprostinil diethanolamine
UT-15C |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Treprostinil diethanolamine (UT-15C) 是EP2、DP1和IP 的有效激动剂,对EP2、DP1、IP、EP1、EP4、EP3 和 FPKi 的值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil diethanolamine 能够促使 cAMP 的上调,进而维持血管系统内的稳态,并造成人肺动脉的血管扩张。 | |||
T24799 |
SKA-111
SKA 111,SKA111 |
Potassium Channel | Membrane transporter/Ion channel |
SKA-111 是一种选择性钙离子激活的钾离子通道 (potassium phannel ) KCa3.1 激活剂,可引起猪内皮细胞膜超极化。SKA-111结合在CaM N-瓣和S4-S5接头之间的界面中,能够改善 Bradykinin 诱导的离体大鼠心脏的冠状动脉扩张,可用于研究心血管疾病。 | |||
T31615 |
Elsibucol
AGI-1096,UNII-O7T92N1Y8T,AGI 1096 |
Antioxidant | oxidation-reduction |
Elsibucol (AGI 1096) 是一种VCAM1抑制剂,可用于研究器官移植排斥。Elsibucol 是一种代谢稳定的丙醇衍生物,具有抗氧化、抗炎和抗增殖的特性。它能降低血液中的胆固醇水平,减少受伤动脉中的氧化应激和炎症反应,从而抑制动脉粥样硬化,保护动脉损伤后的内皮愈合。 | |||
T0957 |
Isradipine
PN 200-110,伊拉地平 |
Calcium Channel; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism |
Isradipine (PN 200-110) 是一种二氢吡啶类钙通道阻滞剂,具有抗高血压和血管扩张活性。它是一种具有口服活性的 L 型钙通道阻滞剂,也是一种潜在可行的帕金森病神经保护剂。 | |||
T1092 |
Zolmitriptan
佐米曲普坦,311C90,BW-311C90 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Zolmitriptan (311C90) 是一种5-HT1B/1D 受体部分激动剂,可用于偏头痛的研究,对 5-HT1B、5-HT1D、5-HT1F 受体的Ki 分别为 5.01、0.63 和 63.09 nM。 | |||
T1215 |
Nicardipine hydrochloride
盐酸尼卡地平,RS-69216,Nicardipine HCl,YC-93 Hydrochloride |
Calcium Channel; Adrenergic Receptor; AChR; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Nicardipine hydrochloride (YC-93 Hydrochloride) 是一种钙通道阻滞剂,IC50为 1 μM。它可阻断某些细胞壁中的钙离子并抑制冠状动脉和外周动脉的收缩,从而降低对氧气的需求心肌和减少动脉收缩和痉挛。它在临床上用作脑和冠状血管扩张剂。 | |||
T1146 |
Nifedipine
BAY-a-1040,Procardia XL,Procardia,硝苯地平,Adalat |
CaMK; Potassium Channel; Calcium Channel; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Nifedipine (Procardia) 是一种二氢吡啶类钙通道阻滞剂,可抑制细胞外钙离子跨膜流入心肌和血管平滑肌细胞,导致主要冠状动脉和全身动脉扩张,降低心肌收缩力。它常用于心肌功能不全的相关研究。 | |||
T9857 |
Vasopressin
antidiuretic hormone (ADH),argipressin,arginine vasopressin (AVP) |
Endogenous Metabolite | Metabolism |
Vasopressin (argipressin) 是一种由下丘脑神经元合成的环状九肽,是肽原激素合成中的一种激素。Vasopressin 参与下丘脑-垂体-肾上腺轴调节过程,增加无溶质水从肾小管的滤液中重新吸收回循环中的量,收缩小动脉提高压强,增强促肾上腺皮质激素释放因子的刺激作用调节垂体促肾上腺皮质激素分泌。Vasopressin 在神经传导过程中可作为神经递质,与特定的 G 蛋白偶联受体结合发挥作用。 | |||
T5391L |
Bepridil free base
CERM1978,CERM 1978,Bepadin,CERM-1978,Angopril |
||
Bepridil is a class IV anti-arrhythmic agent and calcium antagonist. Bepridil hydrochloride blocks calcium entry through membranous calcium channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arter | |||
T38697 |
[Tyr(P)4] Angiotensin II
|
||
[Tyr(P)4] Angiotensin II is a peptide that exerts a multitude of effects on vascular smooth muscle. These effects include the contraction of normal arteries, as well as the induction of hypertrophy or hyperplasia in cultured cells or diseased vessels. | |||
T24701 |
RA-2
RA2 |
||
RA-2 is a pan-negative-gating modulator of KCa2/3 channels that acts by inhibiting EDH-type relaxation in coronary arteries. | |||
T25087 |
Angiopeptin
血管抑肽,D-Nal-cys-tyr-trp-lys-val-cys-thr-NH2,Bim 23014 C |
||
Angiopeptin is a synthetic octapeptide analog of somatostatin; suppresses accelerated transplant atherosclerosis in rabbit heart arteries. | |||
T28977 |
Tilisolol HCl
Tilisolol, trade name Selecal,N 696,N-696,N696 |
||
Tilisolol is a nonselective blocker of beta-adrenergic. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs. | |||
T14036 |
3',4'-Dihydroxyflavonol
DiOHF |
Others | Others |
3',4'-Dihydroxyflavonol (DiOHF) is an efficient antioxidant that diminishes superoxide levels and enhances nitric oxide (NO) functionality in the mesenteric arteries of diabetic rats[1]. | |||
TP1661 |
Angiotensin II (1-4), human TFA
|
||
Angiotensin II is a potent direct vasoconstrictor, causing arteries and veins to constrict, so leading to an increase in blood pressure. | |||
T0112L |
Diltiazem
Diltiazem free base,Dilticard,地尔硫卓,CRD-401,CRD401,Dilzen,CRD 401 |
||
Diltiazem is a non-dihydropyridine (non-DHP) calcium channel blocker that relaxes the smooth muscle in arterial walls, thus opening (dilating) arteries, allowing easier blood flow, and lowering blood pressure, and is used to treat hypertension, angina pec | |||
T40563 |
Sandaracopimaric acid
|
||
Sandaracopimaric acid is an anti-inflammatory diterpenoid compound that effectively reduces the contraction of phenylephrine-induced pulmonary arteries. With an EC50 of 43.93 μM, it exhibits noteworthy anti-inflammatory properties. | |||
TP1224 |
[Sar1, Ile8]-Angiotensin II TFA
Angiotensin 2 TFA,AngiotensinII TFA |
||
[Sar1, Ile8]-Angiotensin II (TFA) is a peptide compound that exerts various effects on vascular smooth muscle. These effects include the contraction of normal arteries as well as the hypertrophy or hyperplasia of cultured cells or diseased vessels. | |||
T36063 |
N-desmethyl Zolmitriptan
|
||
N-desmethyl Zolmitriptan (DZT) is an active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist zolmitriptan . DZT is an agonist of 5-HT1B receptors that induces contraction of isolated human cerebral arteries (EC50 = 100 nM). | |||
T38764 |
Amylin (8-37), human
|
||
Amylin (8-37), human, derived from human Amylin, possesses direct vasodilator effects in isolated mesenteric resistance arteries of rats. Human Amylin is a small pancreatic β-cell hormone that forms aggregates in the absence of insulin and is a key pathological feature of type II diabetes mellitus. | |||
T69303 |
Isoxsuprine Free Base
|
||
Isoxsuprine Free Base is a beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. | |||
TP1609 |
Angiotensin II (1-4), human
|
||
Angiotensin II is a potent direct vasoconstrictor, causing arteries and veins to constrict, so leading to an increase in blood pressure. Angiotensin also potentiates the release of norepinephrine by a direct action on postganglionic sympathetic fibers. | |||
T36562 |
(5Z,11Z,15R)-15-Hydroxyeicosa-5,11-dien-13-ynoic Acid
|
||
(5Z,11Z,15R)-15-Hydroxyeicosa-5,11-dien-13-ynoic acid is a stable isomer of 15(S)-HETE , a major arachidonic acid metabolite from the 15-lipoxygenase pathway. (5Z,11Z,15R)-15-Hydroxyeicosa-5,11-dien-13-ynoic acid elicits concentration-dependent contraction of isolated pulmonary arteries from rabbits and inhibits the proliferation and migration of hormone-independent prostate carcinoma PC-3 cells. | |||
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. | |||
T36544 |
Prostaglandin D1
Prostaglandin D1 |
||
Prostaglandin D1 是对离体人动脉具有收缩和舒张作用的一种前列腺素,能抑制 ADP 诱导的血小板聚集( IC50=320 ng/ml)。Prostaglandin D1 可用于代谢研究。 | |||
T39281 |
AM404
|
||
AM404 is a chemical compound that functions as an inhibitor of endocannabinoid reuptake. It effectively blocks the transport of anandamide, with IC50 values measured in the low micromolar range. Moreover, AM404 exhibits the ability to induce relaxation in rat isolated hepatic arteries contracted with Phenylephrine. This relaxation effect is quantified by a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 μM). Additionally, AM404 possesses a neuroprotective effect. | |||
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。 | |||
T83869 |
(±)16,17-EDT
(±)16,17-Epoxydocosatrienoic Acid,(±)-Dihomo-16,17-EET,(±)16,17-EpDoTrE |
||
(±)16,17-EDT,一种经由细胞色素P450 (CYP) 途径形成的腺苷酸代谢物和氧脂肪酸,能够诱导分离的猪小动脉舒张(EC50 = 11 pM)。此外,(±)16,17-EDT 亦能促进以TP受体激动剂U-46619 预收缩的分离牛冠状动脉的松弛。 | |||
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... | |||
T71211 |
Rizatriptan-d6 benzoate salt
|
||
Rizatriptan-d6 is intended for use as an internal standard for the quantification of rizatriptan by GC- or LC-MS. Rizatriptan is an agonist of the serotonin receptor subtypes 5-HT1B and 5-HT1D. It is selective for 5-HT1B and 5-HT1D receptors over 5-HT1A receptors. Rizatriptan induces vasoconstriction in isolated human middle meningeal arteries. In vivo, rizatriptan reduces head grooming, the number of oculotemporal strokes, eye blinking, and one-eye closures in a Cacna1a mutant transgenic mou... | |||
T78096 |
BQ-3020 ammonium
|
Endothelin Receptor | GPCR/G Protein |
BQ-3020 ammonium 是一种内皮素受体(endothelin receptor)(ETB receptor) 激动剂。它在阻断[125I]ET-1与猪小脑ETB受体的结合实验中显示出IC50值为0.2 nM。此外,BQ-3020 ammonium能够引致兔肺动脉血管收缩以及猪膀胱颈的松弛,因此可作为心血管疾病研究的工具。 | |||
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... | |||
T36557 |
(±)8(9)-EE-14(Z)-E
|
||
(±)14(15)-EE-8(Z)-E is a potent vasodilator in bovine coronary arteries. The synthesis of this analog involves the formation of the epoxide at the 14,15-double bond, however, epoxidation can also occur at the 8,9-double bond. (±)8(9)-EE-14(Z)-E is a minor product from the synthesis of (±)14(15)-EE-8(Z)-E. This compound has not been reported in the literature, and its biological activity is not known. It may serve as a tool to verify that the parent compound, (±)14(15)-EE-8(Z)-E, is pure and does... | |||
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-... | |||
T36531 |
PAR2 (1-6) (mouse, rat)
PAR2 (1-6) (mouse, rat) |
||
PAR2 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth i... | |||
T83868 |
(±)13,14-EDT
(±)13,14-Epoxydocosatrienoic Acid,(±)13,14-EpDoTrE,(±)-Dihomo-13,14-EET |
||
(±)13,14-EDT是一种氧脂和腎上腺酸的代谢产物,通过细胞色素P450(CYP)途径形成。在50 nM的浓度下,它能激活分离的大鼠冠状小动脉平滑肌细胞中的大导电钙激活钾通道(KCa1.1/BK),并导致分离的猪小动脉扩张(EC50 = 12 pM)。(±)13,14-EDT还能使用TP受体激动剂U-46619预收缩的分离牛冠状动脉放松。 | |||
T83840 |
Uridine-5'-O-(3-thiotriphosphate) sodium
UTP-γ-S |
||
Uridine-5'-O-(3-thiotriphosphate) (UTP-γ-S) 是UTP的一种抗水解衍生物,是嘌呤P2Y2受体的激动剂。在表达人类P2Y2受体的1321N1星形胶质瘤细胞中,其可诱导肌醇磷酸盐的形成(EC50 = 240 nM),并且在来自囊性纤维化患者的原代鼻上皮细胞中以浓度依赖的方式诱导氯离子分泌。UTP-γ-S在分离的人类冠状动脉中诱导血管收缩(EC50 = 25.1 µM)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2946 |
Tanshinone IIA sulfonate sodium
丹参酮IIA磺酸盐,丹参酮IIA-磺酸钠,Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium |
CaMK; P450; Calcium Channel | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) 是从丹参中提取的丹参酮IIA 的水溶性衍生物,是SOCE 抑制剂,用于心血管疾病的研究。 | |||
T5074 |
Cholesteryl palmitate
|
Others; Endogenous Metabolite | Metabolism; Others |
Cholesteryl palmitate 是一种慢性间质性肺炎的有用预后生物标志物。 | |||
T6535 |
Histamine Phosphate
组胺磷酸盐,Histamine diphosphate,二磷酸组胺,Histamine acid phosphate |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Histamine Phosphate (Histamine acid phosphate) 是组胺受体的强激活剂和血管扩张神经剂,可激活一氧化氮合成酶。 | |||
T38250 | L-Sepiapterin | ||
L-Sepiapterin, also known as Sepiapterin, is a precursor compound crucial for the production of tetrahydrobiopterin (BH4), which serves as a coenzyme for endothelial nitric oxide synthase (eNOS). This compound demonstrates its efficacy by improving endothelial dysfunction in small mesenteric arteries from db/db mice and promoting angiogenesis. Moreover, L-Sepiapterin exerts inhibitory effects on cellular proliferation and migration in ovarian cancer cells through the down-regulation of p70S6K-de... |