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30

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T7538 Tetraethylammonium chloride

Potassium Channel Membrane transporter/Ion channel
Tetraethylammonium chloride 是非选择性钾通道阻滞剂。它是有机阳离子转运蛋白的良好底物,并具有抗肿瘤特性。
T23516 VU590

Potassium Channel Membrane transporter/Ion channel
VU590 是一种具有高效性和中等选择性的肾外髓质钾 ROMK (Kir1.1) 抑制剂。VU590 抑制 Kir7.1,可调节子宫肌层收缩力和黑皮质素信号传导。
T3465L Vesnarinone HCl

Synonym 2,OPC-8212 HCl,Vesnarinone HCl(81840-15-5 Free base)

Potassium Channel; Calcium Channel; PDE Membrane transporter/Ion channel; Metabolism
Vesnarinone HCl (OPC-8212 HCl) 是一种具有口服活性的 phosphodiesterase 3 (PDE3) 抑制剂。Vesnarinone HCl 可对钙离子和钾离子进行调节, 增加钙通量,减少钾通量。Vesnarinone HCl 是一种新的正性肌力化合物,可增强心肌收缩力,可用于心力衰竭的研究。
T2530 Levosimendan

OR1259,OR1855,左西孟旦

Potassium Channel; PDE; Carbonic Anhydrase; Autophagy Autophagy; Membrane transporter/Ion channel; Metabolism
Levosimendan (OR1259) 是一种钙增敏剂,通过以钙依赖性方式与心肌肌钙蛋白 C 结合,增加肌细胞对钙的敏感性来发挥其作用,可治疗急性失代偿性充血性心力衰竭。
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。
TP2158 TRV-120027 TFA

TRV-120027 TFA (1234510-46-3 free base)

RAAS; Arrestin Endocrinology/Hormones; GPCR/G Protein
TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂,可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂,可与 ß-arrestins 结合,同时阻断 G 蛋白信号传导。 它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌,并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。
T1083L Theophylline monohydrate

Quibron,茶碱一水合物

HDAC; PDE; Adenosine Receptor Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
Theophylline monohydrate (Quibron) 似乎抑制磷酸二酯酶和前列腺素的产生,调节钙通量和细胞内钙分布,并拮抗腺苷。茶碱是黄嘌呤的天然生物碱衍生物,从植物山茶花和小粒咖啡中分离出来。在生理上,该药剂可放松支气管平滑肌,产生血管舒张(脑血管除外),刺激中枢神经系统,刺激心肌,利尿,增加胃酸分泌;它还可以抑制炎症并改善横膈膜的收缩性。
T28778 Silperisone HCl

RGH5002,SILA336,RGH-5002,Silperisone hydrochloride,SILA-336

Silperisone HCl (RGH-5002) 阻断细胞中的钠和钙通道,使肌肉细胞的兴奋度和收缩度降低,降低外周张力,充当肌肉松弛剂和外周血管扩张剂。 Silperisone HCl 可用于治疗脊髓损伤引起的复发性疼痛性肌阵挛、脑血管病引起的异常高肌张力、肌张力症状、锥体紧张综合征、多发性硬化症肌痉挛和脊髓炎。Silperisone 是钠通道蛋白2型α通道阻滞剂。Silperisone 是一种类似于tolperisone 的有机硅化合物,具有中枢作用的肌肉松弛剂特性。
T28268 ORM-3819

ORM-3819 is a potent and selective PDE III inhibitor. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization.
T13806 OR-1855

Others Others
OR-1855 is an active Levosimendan metabolite, has effect on human myometrial contractility.
T30197 ATI-22-107

ATI22-107

ATI-22-107 is a positive cardiac inotropic agent which may affect myocyte calcium cycling and contractility.
T24690 Pyrromecaine HCl

Bumecaine hydrochloride,Pyrromecaine

Pyrromecaine is a local anesthetic used for surface anesthesia. Pyromecaine has a wide spectrum of antiarrhythmic action, exerts a favorable effect on the contractility of the left ventricle, and on the myocardial blood flow following the ligation of the
T15425 GSK1702934A

Others Others
GSK1702934A is a selective TRPC3 agonist. It modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
T16769 Ro 363

Adrenergic Receptor GPCR/G Protein; Neuroscience
RO 363 is an effective inotropic stimulant and is a cardiovascular modulator that decreases diastolic blood pressure and pronounces increases in myocardial contractility. Ro 363 is an effective and highly selective β1-adrenoceptor agonist.
T28321 PD 122860

PD-122860,PD122860

PD 122860 is a dihydropyridine with calcium channel blocking and sodium channel stimulating properties. In the rat heart, PD 122860 increased left ventricular contractility, decreased coronary resistance and altered the shape of the electrocardiogram T-wa
T76629 (Phe2,Orn8)-Oxytocin

'(Phe2,Orn8)-Oxytocin' 作为选择性 V1 加压素激动剂,具有引发兔附睾持续收缩的功能,其EC50值达280 nM。
T76630 (Phe2,Orn8)-Oxytocin acetate

(Phe2,Orn8)-Oxytocin acetate 是一种选择性 V1 加压素 (V1 vasopressin) 激动剂,能诱导兔附睾持续收缩,其EC50值为 280 nM。
TP2158L TRV-120027

Others Others
TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility.
T61918 Ro 363 hydrochloride

Ro 363 hydrochloride 是一种有效的,高度选择性的 β1 肾上腺素受体 (β1-adrenoceptor) 激动剂。Ro 363 hydrochloride 是有效的正性肌力活化剂。Ro 363 hydrochloride 是心血管调节剂,可降低舒张压,显著增加心肌收缩力。
T21424 Disopyramide phosphate

SC13957,SC 13957,SC-13957

Disopyramide, a sodium channel blocker in the Class of 1a anti-arrhythmic agent, is used in the treatment of Ventricular Tachycardia. Disopyramide has a negative inotropic effect on the ventricular myocardium, resulting in a significant decrease in contra
T35875 CCG258208 hydrochloride

GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1]. [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):305...
T62986 CCG-271423

CCG-271423 是一种有效的、选择性的 GRK5 抑制剂,作用于 GRK5 (IC50: 0.0021 μM) 和 GRK2 (IC50: 44 μM)。CCG-271423 能够降低 Ca2+瞬态,抑制心肌细胞收缩能力。
T60428 Cibenzoline

Cibenzoline 是一种抗心律失常药,通过直接影响成孔 Kir6.2 亚基而不是 SUR1 亚基来抑制 KATP 通道。 Cibenzoline 几乎不具有抗胆碱能活性。 Cibenzoline 显着降低与心肌收缩力下降密切相关的LVPG。 Cibenzoline 具有研究肥厚型梗阻性心肌病的潜力[1][2]。
T63237 Acotiamide hydrochloride

Acotiamide hydrochloride 是选择性的、口服具有活力的、可逆的乙酰胆酶碱酯 (AChE) 抑制剂 (IC50: 1.79 μM),能够提高胃收缩性,加速胃排空延迟,能够用于研究胃动力障碍的功能性消化不良及肠道炎症。
T79179 GLX481304

GLX481304是一种针对Nox-2和-4的特异性抑制剂,具有1.25 μM的半抑制浓度(IC50)。它能减少离体小鼠心肌细胞中活性氧(ROS)的生成,并增强心肌收缩功能。此化合物适用于心脏缺血性损伤研究。
T69119 Disopyramide HCl

Disopyramide HCl is the salt form of Disopyramide, an antiarrhythmic medication used in the treatment of ventricular tachycardia. It is a sodium channel blocker and therefore classified as a Class 1a anti-arrhythmic agent. Disopyramide has a negative inotropic effect on the ventricular myocardium, significantly decreasing the contractility. Disopyramide also has an anticholinergic effect on the heart which accounts for many adverse side effects. Disopyramide is available in both oral and intrave...
T35599 Neuropeptide Y (3-36) (human, rat) (trifluoroacetate salt)

Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1 receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial...
T22230 Acotiamide

Acotiamide 是一种具有口服活性、选择性和可逆性的乙酰胆酶碱酯 (AChE) 抑制剂,IC50值为1.79 μM。Acotiamide 是一种胃促动力剂,可增强胃收缩性并加速胃排空延迟。Acotiamide 可用于胃动力障碍的功能性消化不良及肠道炎症的研究。
T26751 BBR 2160

BBR-2160,BBR2160

BBR 2160 is a dihydropyridine derivative belonging to the group of the so-called tiampidine. BBR 2160 has calcium-antagonistic properties in cardiac tissue. Intracellular microelectrodes have been used to characterize the electrophysiological properties o
T83677 Neuropeptide Y (porcine, bovine) TFA

NPY (porcine, bovine)

神经肽Y(Neuropeptide Y, NPY)是一种参与调节食欲、血管收缩、心脏收缩力和肠道分泌的神经肽,同时也是NPY受体Y1、Y2和Y5的激动剂。它在全身范围内表达。NPY能够在表达大鼠Y1或Y2以及表达大鼠Y5的HEK293细胞中选择性抑制由forskolin诱导的cAMP积累,而对表达大鼠Y4受体的L-M(TK-)细胞的影响较小(EC50分别为0.15、2.7、0.66和>1,000 nM)。在分离的豚鼠心脏模型中,NPY能够增加灌注压(EC30 = 1.3 nM)。神经内注射NPY(300 pmol/动物)能够在大鼠中增加食物摄取量。

化合物

Tetraethylammonium chloride
Cat.No: T7538
Synonym:
Target: Potassium Channel
VU590
Cat.No: T23516
Synonym:
Target: Potassium Channel
Vesnarinone HCl
Cat.No: T3465L
Synonym: Synonym 2,OPC-8212 HCl,Vesnarinone HCl(81840-15-5 Free base)
Target: Potassium Channel, Calcium Channel, PDE
Levosimendan
Cat.No: T2530
Synonym: OR1259,OR1855,左西孟旦
Target: Potassium Channel, PDE, Carbonic Anhydrase, Autophagy
Nifedipine
Cat.No: T1146
Synonym: BAY-a-1040,Procardia XL,Procardia,硝苯地平,Adalat
Target: CaMK, Potassium Channel, Calcium Channel, Autophagy
TRV-120027 TFA
Cat.No: TP2158
Synonym: TRV-120027 TFA (1234510-46-3 free base)
Target: RAAS, Arrestin
Theophylline monohydrate
Cat.No: T1083L
Synonym: Quibron,茶碱一水合物
Target: HDAC, PDE, Adenosine Receptor
Silperisone HCl
Cat.No: T28778
Synonym: RGH5002,SILA336,RGH-5002,Silperisone hydrochloride,SILA-336
Target:
ORM-3819
Cat.No: T28268
Synonym:
Target:
OR-1855
Cat.No: T13806
Synonym:
Target: Others
ATI-22-107
Cat.No: T30197
Synonym: ATI22-107
Target:
Pyrromecaine HCl
Cat.No: T24690
Synonym: Bumecaine hydrochloride,Pyrromecaine
Target:
GSK1702934A
Cat.No: T15425
Synonym:
Target: Others
Ro 363
Cat.No: T16769
Synonym:
Target: Adrenergic Receptor
PD 122860
Cat.No: T28321
Synonym: PD-122860,PD122860
Target:
(Phe2,Orn8)-Oxytocin
Cat.No: T76629
Synonym:
Target:
(Phe2,Orn8)-Oxytocin acetate
Cat.No: T76630
Synonym:
Target:
TRV-120027
Cat.No: TP2158L
Synonym:
Target: Others
Ro 363 hydrochloride
Cat.No: T61918
Synonym:
Target:
Disopyramide phosphate
Cat.No: T21424
Synonym: SC13957,SC 13957,SC-13957
Target:
CCG258208 hydrochloride
Cat.No: T35875
Synonym:
Target:
CCG-271423
Cat.No: T62986
Synonym:
Target:
Cibenzoline
Cat.No: T60428
Synonym:
Target:
Acotiamide hydrochloride
Cat.No: T63237
Synonym:
Target:
GLX481304
Cat.No: T79179
Synonym:
Target:
Disopyramide HCl
Cat.No: T69119
Synonym:
Target:
Neuropeptide Y (3-36) (human, rat) (trifluoroacetate salt)
Cat.No: T35599
Synonym:
Target:
Acotiamide
Cat.No: T22230
Synonym:
Target:
BBR 2160
Cat.No: T26751
Synonym: BBR-2160,BBR2160
Target:
Neuropeptide Y (porcine, bovine) TFA
Cat.No: T83677
Synonym: NPY (porcine, bovine)
Target:
Cat. No. Product Name Target Signaling Pathways
T4S1518 Pseudoginsenoside RT1

拟人参皂苷 RT1,假人参皂苷RT1

Others Others
Pseudoginsenoside RT1 是分离自 Randia siamensis 中,具有鱼毒素作用。它可导致血压下降、心率加快和子宫自发收缩力增加。
T4S1422 Praeruptorin E

白花前胡素 E,白花前胡素E

Others; Calcium Channel Membrane transporter/Ion channel; Metabolism; Others
Praeruptorin E 是白花前胡中的一种主要成分,是钙拮抗剂,pD2′值为 5.2。
T83454 13-Hydroxylupanine hydrochloride

Hydroxylupanine hydrochloride

13-Hydroxylupanine是甜羽扇豆中一种典型的生物碱。它具有阻断神经节传递、降低心肌收缩力以及收缩子宫平滑肌的作用。

天然产物

Pseudoginsenoside RT1
Cat.No: T4S1518
Synonym: 拟人参皂苷 RT1,假人参皂苷RT1
Target: Others
Praeruptorin E
Cat.No: T4S1422
Synonym: 白花前胡素 E,白花前胡素E
Target: Others, Calcium Channel
13-Hydroxylupanine hydrochloride
Cat.No: T83454
Synonym: Hydroxylupanine hydrochloride
Target:
TargetMol Loading
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