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15

抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T23310	SB-203186 hydrochloride	5-HT Receptor	GPCR/G Protein; Neuroscience
	SB 203186 hydrochloride 是一种选择性的、竞争性的5-HT4拮抗剂。它拮抗5-HT4受体介导的多巴酚收缩大鼠离体食管弛缓，其在大鼠食管、豚鼠回肠和人类结肠的 pKB 值分别是 10.9、9.5 和 9.0。
T28540	Ripisartan UP 269-6,UP-2696,UP 2696,UP-269-6,UP269-6	RAAS	Endocrinology/Hormones
	Ripisartan (UP-269-6) 是一种强效的特异性血管紧张素 II 受体拮抗剂，对血管紧张素 II 介导的交感神经性心动过速反应有抑制作用。
T10634	Bunaftide Bunaphtide,Meregon,Bunaftine	Others	Others
	Bunaftide（Bunaphtid）具有抗心律失常作用，对乌头碱诱导的室性心动过速有抑制作用。
T1439	Lacidipine SN-305,拉西地平,GX-1048,GR-43659X	Apoptosis; Calcium Channel; Reactive Oxygen Species	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB
	Lacidipine (SN-305) 是一种L 型钙离子通道阻断剂。
T1158	Phenoxybenzamine hydrochloride 苯氧苯札明,NCI-c01661,NSC 37448,盐酸酚苄明,Phenoxybenzamine HCl	CaMK; Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Phenoxybenzamine hydrochloride (NCI-c01661) 是一种选择性的 α-adrenoceptor 和 calmodulin 的抑制剂，是常用的抗高血压药。
T15257	Etripamil MSP-2017,(-)-MSP-2017	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Etripamil (MSP-2017) 是一种短效L 型钙通道拮抗剂，可用于治疗阵发性室上性心动过速的研究。它通过抑制房室结细胞中钙慢通道的钙离子流入，显示房室结传导并延长房室结不应期
T0976	Propoxur 残杀威,Aprocarb,Propoxure,Baygon	AChR; Antifungal	Microbiology/Virology; Neuroscience
	Propoxur (Propoxure) 是一种氨基甲酸酯类杀虫剂，用于控制蟑螂、苍蝇、蚊子以及草坪和草坪昆虫。
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
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
T14153	Aladorian ARM036	Others	Others
	Aladorian (ARM036) is a benzothiazepine derivative and it has anti-arrhythmia effect. Aladorian is used for the research of heart failure and catecholaminergic polymorphic ventricular tachycardia[1][2].
T68639	Ciprostene (free base)
	Ciprostene (free base) is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.
T36732	Ciprostene (calcium salt)
	Ciprostene is the 9β-methyl analog of carbaprostacyclin and a stable analog of PGI2. Ciprostene exhibits biological activity similar to PGI2, but is 30-fold less potent. In patas monkeys, ciprostene induces hypotension and causes tachycardia when administered at a dose of 0.16 μg/kg/min. In addition, ciprostene inhibits ADP-induced platelet aggregation ex vivo and in vitro with ID50 values of 9.1 μg/kg/min and 60 ng/ml, respectively.
T36561	(3S)-hydroxy Quinidine
	(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-depe...
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...
T70077	Fadolmidine HCl
	Fadolmidine, also known as MPV-2426, is a novel and potent alpha2 -adrenoceptor (alpha2) -AR) agonist developed for spinal analgesia. Fadolmidine displayed high affinity and full agonist efficacy at all three human alpha2-adrenoceptor subtypes (A, B and C) in transfected CHO cells with EC50 values (nM) of 0.4, 4.9 and 0.5, respectively. Fadolmidine inhibited also electrically evoked contractions in rat vas deferens demonstrating the activation of rodent presynaptic alpha2D-adrenoceptors with an ...

化合物

SB-203186 hydrochloride

Cat.No: T23310

Target: 5-HT Receptor

Cat.No: T28540

Synonym: UP 269-6,UP-2696,UP 2696,UP-269-6,UP269-6

Target: RAAS

Cat.No: T10634

Synonym: Bunaphtide,Meregon,Bunaftine

Target: Others

Cat.No: T1439

Synonym: SN-305,拉西地平,GX-1048,GR-43659X

Target: Apoptosis, Calcium Channel, Reactive Oxygen Species

Phenoxybenzamine hydrochloride

Cat.No: T1158

Synonym: 苯氧苯札明,NCI-c01661,NSC 37448,盐酸酚苄明,Phenoxybenzamine HCl

Target: CaMK, Adrenergic Receptor

Cat.No: T15257

Synonym: MSP-2017,(-)-MSP-2017

Target: Calcium Channel

Cat.No: T0976

Synonym: 残杀威,Aprocarb,Propoxure,Baygon

Target: AChR, Antifungal

Cat.No: T21391

Synonym: Tambocor,Apocard,Flecainida,Flecainidum

Disopyramide phosphate

Cat.No: T21424

Synonym: SC13957,SC 13957,SC-13957

Cat.No: T14153

Synonym: ARM036

Target: Others

Ciprostene (free base)

Cat.No: T68639

Ciprostene (calcium salt)

Cat.No: T36732

(3S)-hydroxy Quinidine

Cat.No: T36561

Disopyramide HCl

Cat.No: T69119

Fadolmidine HCl

Cat.No: T70077

Cat. No.	Product Name	Target	Signaling Pathways
T4550	Ajmaline Cardiorythmine,Raugalline,阿义吗啉,阿义马林,Tachmalin,(+)-Ajmaline	Sodium Channel	Membrane transporter/Ion channel
	Ajmaline (Cardiorythmine) 是一种钠通道阻断剂，属于1A 类抗心律失常剂。Ajmaline 阻断 HERG 电流，在 HEK 细胞的 IC50为 1 μM，爪蟾卵母细胞的IC50为 42.3 μM。Ajmaline 在室性心动过速方面具有研究价值。

天然产物

Cat.No: T4550

Synonym: Cardiorythmine,Raugalline,阿义吗啉,阿义马林,Tachmalin,(+)-Ajmaline

Target: Sodium Channel

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