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16

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16873	SERCA2a activator 1	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	SERCA2a activator 1 是一种肌肉/内质网 Ca2+ 依赖性 ATPase 2a 激活剂。 SERCA2a activator 1 降低受磷蛋白抑制并增强心脏的收缩和舒张功能。
T30615	Bupicomide
	Bupicomide is a vasodilator that significantly reduces systolic, diastolic, and means arterial pressure, as well as peripheral vascular resistance.
T7143	Alagebrium chloride 4,5-二甲基-3-(2-氧代-2-苯基乙基)噻唑氯化物,ALT711,阿拉氯胺	Others; Endogenous Metabolite	Metabolism; Others
	Alagebrium chloride (ALT711) 是晚期糖基化终产物(AGE) 抑制剂。
T2535	Ivabradine hydrochloride 盐酸伊伐布雷定,S 16257-2,Ivabradine HCl	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Ivabradine hydrochloride (S 16257-2) 是一种可口服的，超极化激活的环核苷酸门控离子通道通道阻滞剂。
T0866	Propafenone Rythmol,普罗帕酮,Propafenonum	Potassium Channel; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel
	Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。
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.
T61215	Alinidine hydrobromide
	Alinidine hydrobromide, a specific bradycardic agent, diminishes the slope of the diastolic depolarization in sinoatrial tissue and Purkinje fibers [1].
T26452	A 80b A80b,A-80b
	A-80b is a synthesized pyridazino[4,5-b]indole derivate with potent and long-lasting antihypertensive activity. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. A-8
T36230	C2 Ceramide (d14:1/2:0) C2 Ceramide (d14:1/2:0)
	C2 Ceramide (d14:1/2:0) is a bioactive sphingolipid. Dietary administration of C2 ceramide (d14:1/2:0) (100 μM) induces lipotoxic cardiomyopathy via increasing diastolic and systolic diameter as well as reducing fractional shortening and the number of normal cardiac contractile events in Drosophila.
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。
T68397	Xamoterol fumarate
	Xamoterol fumarate is a selective beta-1-adrenergic partial agonist. Because it is a partial agonist, it acts as an agonist when sympathetic activity is low and as an antagonist when sympathetic activity is high. It reduces myocardial ischemia and improves ventricular function in patients with mild to moderate heart failure. In patients with severe heart failure it has been shown to produce benefits in systolic and diastolic function.
T68788	Ellipticine quinone
	Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.). Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mi...
T36547	Quazinone
	Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties.1,2 It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM).1 Quazinone (10-300 μg/kg) increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner, as well as decreases systolic and diastolic blood pressure.2 It also inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smoot...
T37794	Rec 15/2615 (hydrochloride)
	Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50...
T83768	Zofenoprilat Zofenopril-SH,SQ 26,333
	Zofenoprilat是一种血管紧张素转换酶(ACE; IC50 = 8 nM for the rabbit lung enzyme)的抑制剂，同时也是前体药zofenopril的活性代谢产物。它能够抑制分离的豚鼠小肠中由血管紧张素I或缓激肽诱导的收缩(EC50s = 3 and 1 nM, respectively)。在人类脐静脉内皮细胞(HUVECs)中，Zofenoprilat (10 nM)降低基础内皮素-1分泌和一氧化氮(NO)生成，并阻止TNF-α诱导的活性氧种(ROS)增加以及谷胱甘肽(GSH)水平降低。Zofenoprilat (10 µM)保护初级人类心脏微血管内皮细胞免受多柔比星诱导的细胞毒性。此外，Zofenoprilat (10 µM)还能增加HUVECs中的硫化氢(H2S)生成，以及细胞的黏着、迁移和增殖。在以400 µM浓度使用时，它可以减少Langendorff分离的大鼠心脏灌流缺血再灌注损伤模型中的舒张末压和乳酸脱氢酶(LDH)释放。
T36729	Urotensin II (goby) (trifluoroacetate salt)
	Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across ...

化合物

SERCA2a activator 1

Cat.No: T16873

Target: Calcium Channel

Cat.No: T30615

Alagebrium chloride

Cat.No: T7143

Synonym: 4,5-二甲基-3-(2-氧代-2-苯基乙基)噻唑氯化物,ALT711,阿拉氯胺

Target: Others, Endogenous Metabolite

Ivabradine hydrochloride

Cat.No: T2535

Synonym: 盐酸伊伐布雷定,S 16257-2,Ivabradine HCl

Target: Adrenergic Receptor

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Cat.No: T16769

Target: Adrenergic Receptor

Alinidine hydrobromide

Cat.No: T61215

Cat.No: T26452

Synonym: A80b,A-80b

C2 Ceramide (d14:1/2:0)

Cat.No: T36230

Synonym: C2 Ceramide (d14:1/2:0)

Ro 363 hydrochloride

Cat.No: T61918

Xamoterol fumarate

Cat.No: T68397

Ellipticine quinone

Cat.No: T68788

Cat.No: T36547

Rec 15/2615 (hydrochloride)

Cat.No: T37794

Cat.No: T83768

Synonym: Zofenopril-SH,SQ 26,333

Urotensin II (goby) (trifluoroacetate salt)

Cat.No: T36729

Cat. No.	Product Name	Target	Signaling Pathways
TN5073	Strophanthidin 毒毛旋花子甙元,Strophanthidine,葡萄球菌素	ATPase; Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Strophanthidin (Strophanthidine) 是黄花夹竹桃中的一种类固醇，可增加舒张期和收缩期胞内 Ca2+浓度。它在 0.1 和 1 nmol/L 增加Na+/K+-ATPase 活性，1到100 μ mol/L 抑制Na+/K+-ATPase 活性，10 和 100 nmol/L 对Na+/K+-ATPase 活性无影响。
TN3904	Dysolenticin J	Others	Others
	Dysolenticin J shows significant vasodilative effects on intact rat aortic rings with a diastolic degree of 87.4% at 10 ug/mL.
T16332	NKH477 Colforsin dapropate hydrochloride	NMDAR	Neuroscience
	NKH477 is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 shows an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute
TN2001	Oblongine	Others	Others
	Oblongine chloride may have potential haemodynamic effects, it can cause a dose-dependent reduction of systolic and diastolic blood pressure, and that these effects are not mediated by α²-adrenergic receptor stimulation.

天然产物

Cat.No: TN5073

Synonym: 毒毛旋花子甙元,Strophanthidine,葡萄球菌素

Target: ATPase, Calcium Channel

Cat.No: TN3904

Target: Others

Cat.No: T16332

Synonym: Colforsin dapropate hydrochloride

Target: NMDAR

Cat.No: TN2001

Target: Others

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