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29

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T0389 Dabigatran etexilate

达比加群酯,BIBR 1048

Thrombin Proteases/Proteasome
Dabigatran etexilate (BIBR 1048) 是一种 Dabigatran 前药,具有口服活性。它具有抗凝作用,能够预防心房颤动引起的静脉血栓栓塞和中风。
T5133 Dabigatran Etexilate Mesylate

甲磺酸达比加群酯,BIBR 1048MS,Dabigatran etexilate methanesulfonate

Thrombin Proteases/Proteasome
Dabigatran Etexilate Mesylate (BIBR 1048MS) 是一种口服具有活性的 Dabigatran 前药,具有抗凝作用,能够预防心房颤动引起的静脉血栓栓塞和中风。
T30520 BMS-394136

BMS394136,BMS 394136,BMS394136;UNII-M694U7167K

Potassium Channel Membrane transporter/Ion channel
BMS-394136 (BMS 394136) 是一种 KV1.5 拮抗剂,可用于治疗心律失常、心房颤动等心血管疾病。
T26689 AVE-0118

AVE 0118,AVE0118

Potassium Channel Membrane transporter/Ion channel
AVE-0118 是一种钾通道阻滞剂,可抑制持续性心房颤动。
T30544 BMS-919373

BMS919373,BMS 919373

Potassium Channel Membrane transporter/Ion channel
BMS-919373是的钾通道Kv1.5(KCNA5)抑制剂,可用于心房颤动和急性冠状动脉综合征。
T68038 Celivarone

Potassium Channel Membrane transporter/Ion channel
Celivarone 是一种钾离子通道阻滞剂,可用于研究心律失常、心房扑动和心房颤动。
T28748 Selodenoson

RG14202,DTI0009,DTI-0009,RG-14202,DT-009,DT009

Adenosine Receptor GPCR/G Protein; Neuroscience
Selodenoson (RG-14202) 是一种选择性腺苷 A1 受体激动剂,可用于减慢心房颤动患者的心率,治疗心律失常。
T1073 Dronedarone hydrochloride

Dronedarone HCl,SR33589,决奈达隆盐酸盐,盐酸决奈达隆

Potassium Channel; Calcium Channel; Sodium Channel; Adrenergic Receptor; Autophagy Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience
Dronedarone hydrochloride (SR33589) 是一种胺碘酮类似物,可抑制 Na+,K+andCa2+的电流,有可能治疗心房颤动。
T68730 AVE1231

Potassium Channel Membrane transporter/Ion channel
AVE1231 是一种 TASK-1 通道阻滞剂,抑制 TASK-1 ,可用于研究心房颤动。
T13021 Sulamserod

RS-100302

5-HT Receptor GPCR/G Protein; Neuroscience
Sulamserod(RS 100302) 是一种有效的 5-HT4 receptor 拮抗剂,具有抗心律失常活性,可用于研究心房颤动和心血管相关疾病。
T61913 Cavutilide

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Cavutilide具有抗心律失常活性,抑制 hERG K(+)通道,可用于研究心力衰竭和持续性心房颤动。
T6476 Dofetilide

UK 68789,UK-68798,Tikosyn,多非利特

Potassium Channel Membrane transporter/Ion channel
Dofetilide (UK 68789) 是一种具有口服活性、有效的且特异性的IKr 阻滞剂,作为 III 类抗心律失常药物。Dofetilide 可用于心血管疾病研究。
T6295 Dabigatran

BIBR 953,BIBR 953ZW,达比加群

Thrombin Proteases/Proteasome
Dabigatran (BIBR 953ZW) 是一种口服抗凝剂,是一种可逆的,竞争性的直接凝血酶 (thrombin) 抑制剂,Ki=4.5 nM。它也抑制凝血酶诱导的血小板聚集 (IC50=10 nM)。
T83979 Sulcardine 2HCl

Sulcardine 2HCl(343935-60-4 Free base),HBI-3000 2HCl

HER; Sodium Channel Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors
Sulcardine 2HCl 是一种多离子通道阻滞剂,具有抗心律失常作用,可阻断 hERG 和hNav1.5通道的特性,可用于研究心房颤动和室性心律失常。
T21373 Aprindine hydrochloride

Fiboran,Amidonal,Aprinidine,Aprindin,Aprindine HCl,Aprindina,Fibocil

Aprindine HCl is a Class 1b antiarrhythmic agent used to manage ventricular and supraventricular arrhythmias. In one study, it delayed atrial fibrillation more than digoxin did. It has shown effectiveness when given orally.
T30678 C1-resveratrol

C1resveratrol,C1 resveratrol

C1 resveratrol is a novel multifunctional derivative of resveratrol, which is used to treat atrial fibrillation.
T68893 Vanoxerine free base

Vanoxerine, also known as GBR-12909; I-893, is a dopamine ruptake inhibitor potentially for the treatment of atrial fibrillation.
T30607 Budiodarone

ATI2042,ATI-2042,ATI 2042

Budiodarone(ATI-2042)is a chemical analog of an antiarrhythmic drug and amiodarone. Budedalone is promising as an antiarrhythmic agent for the prevention of atrial fibrillation.
T37821 AP 14145 hydrochloride

KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+...
T62207 KVI-020

KVI-020 是一种选择性的、口服具有活力的心房钾通道 Kv1.5 阻滞剂 (IC50: 480 nM)。KVI-020 对 hERG 表现出抑制作用 (IC50: 15100 nM)。 KVI-020 是一种有效的抗心律失常剂 (antiarrhythmic),能够用于研究房颤 (AF)。
T79195 Cav 3.2 inhibitor 4

Calcium Channel Membrane transporter/Ion channel; Metabolism
Cav 3.2 inhibitor 4 (compound 21) 是高效的选择性 T 型钙通道 (Cav3.2) 抑制剂,具有外周限制性,其 IC50 值为 0.6 μM,适用于心房颤动研究。
T62283 DDO-02005

DDO-02005 是一种 Kv1.5 钙离子通道的有效抑制剂 (IC50: 0.72 μM)。DDO-02005 在 CaCl2-ACh 房颤大鼠模型中表现出良好的抗房颤效果,并能有效抵因抗乌头碱引发的心律失常。
T80039 ATX-II

Sodium Channel Membrane transporter/Ion channel
ATX-II为特定Na+通道调节剂,源自海葵(Anemonia sulcata)毒液。该化合物会使细胞培养物对Na+Halothane、Caffeine及Ryanodine敏感,并可诱发肺静脉心律失常及心房颤动。
T21391 Flecainide

Tambocor,Apocard,Flecainida,Flecainidum

Flecainide acetate is a class Ic antiarrhythmic agent, it is used to treat a variety of cardiac arrhythmias including paroxysmal atrial fibrillation, paroxysmal supraventricular tachycardia, and ventricular tachycardia. It works by regulating the flow of
T39963 AP14145 hydrochloride

AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
T30192 Atecegatran metoxil

Atecegatran fexenetil,AZD-0837,AZD 0837,AZD0837

Atecegatran Metoxil (Atecegatran Fexenetil ,AZD0837) is an oral direct thrombin inhibitor,which currently in clinical development for the prevention of stroke and systemic embolic events in patients with atrial fibrillation. AZD0837 is a selective and re
T82936 ATX-II TFA

Sodium Channel Membrane transporter/Ion channel
ATX-II TFA为源自海葵(Anemonia sulcata)毒素的特定Na+通道调节剂,能使细胞培养物对Na+、Halothane、Caffeine和Ryanodine敏感,并可诱发肺静脉心律失常和心房颤动。
T61231 DDO-02005 free base

DDO-02005 (free base) 是一种针对Kv1.5 钙离子通道的高效抑制剂,其IC50 值为0.72 μM。在CaCl2-ACh诱导的房颤大鼠模型中,DDO-02005 (free base) 显示出显著的抗房颤效果,并能有效对抗乌头碱所致的心律失常。
T64099 FXIa-IN-9

FXIa-IN-9 (compound 3f) 是一种具有高选择性的FXIa抑制剂,通过与FXIa结合并形成氢键(human FXIaKi: 0.17 nM, rabbit FXIaKi: 0.5 nM),展现出显著的抗凝活性。该化合物在心房颤动、中风、心肌梗塞、深静脉血栓以及肺栓塞等血栓栓塞性疾病的研究中有潜在应用价值。

化合物

Dabigatran etexilate
Cat.No: T0389
Synonym: 达比加群酯,BIBR 1048
Target: Thrombin
Dabigatran Etexilate Mesylate
Cat.No: T5133
Synonym: 甲磺酸达比加群酯,BIBR 1048MS,Dabigatran etexilate methanesulfonate
Target: Thrombin
BMS-394136
Cat.No: T30520
Synonym: BMS394136,BMS 394136,BMS394136;UNII-M694U7167K
Target: Potassium Channel
AVE-0118
Cat.No: T26689
Synonym: AVE 0118,AVE0118
Target: Potassium Channel
BMS-919373
Cat.No: T30544
Synonym: BMS919373,BMS 919373
Target: Potassium Channel
Celivarone
Cat.No: T68038
Synonym:
Target: Potassium Channel
Selodenoson
Cat.No: T28748
Synonym: RG14202,DTI0009,DTI-0009,RG-14202,DT-009,DT009
Target: Adenosine Receptor
Dronedarone hydrochloride
Cat.No: T1073
Synonym: Dronedarone HCl,SR33589,决奈达隆盐酸盐,盐酸决奈达隆
Target: Potassium Channel, Calcium Channel, Sodium Channel, Adrenergic Receptor, Autophagy
AVE1231
Cat.No: T68730
Synonym:
Target: Potassium Channel
Sulamserod
Cat.No: T13021
Synonym: RS-100302
Target: 5-HT Receptor
Cavutilide
Cat.No: T61913
Synonym:
Target: EGFR
Dofetilide
Cat.No: T6476
Synonym: UK 68789,UK-68798,Tikosyn,多非利特
Target: Potassium Channel
Dabigatran
Cat.No: T6295
Synonym: BIBR 953,BIBR 953ZW,达比加群
Target: Thrombin
Sulcardine 2HCl
Cat.No: T83979
Synonym: Sulcardine 2HCl(343935-60-4 Free base),HBI-3000 2HCl
Target: HER, Sodium Channel
Aprindine hydrochloride
Cat.No: T21373
Synonym: Fiboran,Amidonal,Aprinidine,Aprindin,Aprindine HCl,Aprindina,Fibocil
Target:
C1-resveratrol
Cat.No: T30678
Synonym: C1resveratrol,C1 resveratrol
Target:
Vanoxerine free base
Cat.No: T68893
Synonym:
Target:
Budiodarone
Cat.No: T30607
Synonym: ATI2042,ATI-2042,ATI 2042
Target:
AP 14145 hydrochloride
Cat.No: T37821
Synonym:
Target:
KVI-020
Cat.No: T62207
Synonym:
Target:
Cav 3.2 inhibitor 4
Cat.No: T79195
Synonym:
Target: Calcium Channel
DDO-02005
Cat.No: T62283
Synonym:
Target:
ATX-II
Cat.No: T80039
Synonym:
Target: Sodium Channel
Flecainide
Cat.No: T21391
Synonym: Tambocor,Apocard,Flecainida,Flecainidum
Target:
AP14145 hydrochloride
Cat.No: T39963
Synonym:
Target:
Atecegatran metoxil
Cat.No: T30192
Synonym: Atecegatran fexenetil,AZD-0837,AZD 0837,AZD0837
Target:
ATX-II TFA
Cat.No: T82936
Synonym:
Target: Sodium Channel
DDO-02005 free base
Cat.No: T61231
Synonym:
Target:
FXIa-IN-9
Cat.No: T64099
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T41358 2-Hydroxybenzylamine

Others Others
2-Hydroxybenzylamine 是一种有效的 IsoLG 小分子清除剂,可将活性物质作为惰性加合物螯合。 2-Hydroxybenzylamine 可用于通过减少具有天然生物分子的 IsoLG 加合物来减少心房颤动消融后心房颤动和其他心房心律失常的早期复发。
T3S0081 Oxypeucedanin

(+-)-Oxypeucedanin,氧化前胡素,Oxypeucadanin

Potassium Channel Membrane transporter/Ion channel
Oxypeucedanin ((+-)-Oxypeucedanin) 是呋喃香豆素衍生物,分离自Angelica dahurica。它是选择性开放通道阻滞剂,可抑制hKv1.5通道电流,IC50值为 76 nM。它延长心脏动作电位持续时间,是潜在的抗心律失常试剂。它通过抑制癌细胞迁移来诱导细胞凋亡。
T7056 Dronedarone

决奈达隆,SR 33589

P450; Potassium Channel; Calcium Channel; Sodium Channel; Adrenergic Receptor; AChR; Autophagy Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience
Dronedarone (SR 33589) 是一种胺碘酮类似物,对治疗心房颤动可能有效。它是CYP3A4的底物和中度抑制剂。它是多种离子电流的有效阻滞剂,通过非竞争性结合到肾上腺素能受体显示出抗肾上腺素能的效果。

天然产物

2-Hydroxybenzylamine
Cat.No: T41358
Synonym:
Target: Others
Oxypeucedanin
Cat.No: T3S0081
Synonym: (+-)-Oxypeucedanin,氧化前胡素,Oxypeucadanin
Target: Potassium Channel
Dronedarone
Cat.No: T7056
Synonym: 决奈达隆,SR 33589
Target: P450, Potassium Channel, Calcium Channel, Sodium Channel, Adrenergic Receptor, AChR, Autophagy
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