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15

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15050	Danicamtiv MYK-491,SAR 440181	Myosin	Cytoskeletal Signaling
	Danicamtiv (MYK-491) 是一种正性肌力药物，也是一种心肌肌球蛋白的选择性变构激活剂，可增加心脏收缩功能并保持机械效率。
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。
T0083	Eplerenone Epoxymexrenone,CGP 30083,依普利酮,SC-66110	Glucocorticoid Receptor	Endocrinology/Hormones
	Eplerenone (CGP 30083) 是一种竞争性的、选择性的、具有口服活性的醛固酮 (aldosterone) 拮抗剂，IC50=138 nM。它对孕酮，雄激素，雌激素和糖皮质激素受体的亲和力低，可用于研究高血压和心肌梗死后的心力衰竭。
T21395	Finerenone BAY948862,BAY-948862,BAY94-8862,非奈利酮,BAY 94-8862,BAY-94-8862,BAY 948862	Glucocorticoid Receptor	Endocrinology/Hormones
	Finerenone (BAY-948862) 是一种选择性、具有口服活性的、非甾体类盐皮质激素受体拮抗剂 (IC50=18 nM)。与糖皮质激素受体、雄激素受体和孕酮受体相比，它表现出良好的选择性 (>500-fold)。它在心肾疾病研究中具有潜在的应用前景，如 2 型糖尿病和慢性肾脏疾病。
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。
T36569	KR-32568	Sodium Channel	Membrane transporter/Ion channel
	KR-32568是一种钠/氢交换器1（NHE-1）抑制剂（IC50：230 nM）。KR-32568具有强大的心脏保护作用。当使用浓度为10μM 时，它能在离体的缺血大鼠心脏模型中恢复心脏收缩功能。KR-32568（0.3mg/kg）在缺血和再灌注损伤的大鼠模型中减少了心肌梗死的大小。
T20094	Adrenochrome Adraxone	Antioxidant	oxidation-reduction
	Adrenochrome (Adraxone) 是一种细胞毒性分子，可用于杀死细菌。Adrenochrome 是 Epinephrine 的氧化产物。Adrenochrome 是一种可作用于大鼠心脏的冠状动脉收缩化合物，与心脏毒性有关，可用于确定超氧化物歧化酶的活性。Adrenochrome 与可用于神经系统疾病研究，是拟精神病的潜在药物。
T35974	5-methyl-2-HOBA (hydrochloride)
	5-methyl-2-HOBA is an isoketal scavenger. It reduces angiotensin II-induced increases in systolic blood pressure in mice.
T60377	CXL-1020
	CXL-1020 是一种硝酰 (HNO) 前体药物。CXL-1020 改善舒张异常大鼠的心肌收缩性/舒张性和 Ca2+循环。CXL-1020 在犬模型中诱导血管舒张并改善心脏功能。CXL-1020 已被用于研究收缩期心力衰竭和稳定期心力衰竭。
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...
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
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.
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.
T35855	AAA
	AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...

化合物

Cat.No: T15050

Synonym: MYK-491,SAR 440181

Target: Myosin

SERCA2a activator 1

Cat.No: T16873

Target: Calcium Channel

Cat.No: T0083

Synonym: Epoxymexrenone,CGP 30083,依普利酮,SC-66110

Target: Glucocorticoid Receptor

Cat.No: T21395

Synonym: BAY948862,BAY-948862,BAY94-8862,非奈利酮,BAY 94-8862,BAY-94-8862,BAY 948862

Target: Glucocorticoid Receptor

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

Cat.No: T36569

Target: Sodium Channel

Cat.No: T20094

Synonym: Adraxone

Target: Antioxidant

5-methyl-2-HOBA (hydrochloride)

Cat.No: T35974

Cat.No: T60377

Cat.No: T36547

Cat.No: T26452

Synonym: A80b,A-80b

Xamoterol fumarate

Cat.No: T68397

C2 Ceramide (d14:1/2:0)

Cat.No: T36230

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

Cat.No: T35855

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。
T5968	DL-Homocysteine thiolactone hydrochloride DL-Homocysteinethiolactone hydrochloride,DL-高半胱氨酸硫内酯盐酸盐	Endogenous Metabolite	Metabolism
	DL-Homocysteine thiolactone hydrochloride (DL-Homocysteinethiolactone hydrochloride) 是具有根生长抑制特性的环状氨基酸衍生物。
T7995	α-Angelica lactone α-当归内酯,当归内酯,Alpha-Angelica Lactone	Others; GST	Others; oxidation-reduction
	α-Angelica lactone 是一种乙烯基亲核试剂，也是一种天然存在的抗癌剂。它可以得到手性的 δ-氨基 γ，γ-二取代丁烯醇内酯羰基衍生物，并在 γ-碳上表现出亲电子俘获。它通过选择性增强谷胱甘肽-S-硫转移酶 (GST) 和 UDP-葡糖苷转移酶 (UGT) 解毒酶发挥强大的化学保护作用。
T3123	Allicin	ERK; IL Receptor; Others; IκB/IKK; p38 MAPK; TNF; ROS; Caspase; Antifection	Apoptosis; Immunology/Inflammation; MAPK; Microbiology/Virology; NF-κB; Others; Proteases/Proteasome
	Allicin 具有抗氧化、杀菌、抗癌、抗炎活性，对肠上皮细胞具有抑制性免疫调节作用。 Allicin 能显着抑制胰岛素诱导的血管平滑肌细胞的增殖和迁移，这可能与抑制 ERK 信号通路的激活有关。 Allicin 有利于降低高胆固醇血症大鼠的血液胆固醇、甘油三酯水平和收缩压，它可能有益于影响动脉粥样硬化的两个危险因素——高脂血症和高血压。
TN4616	N-Methyltaxol C	Others	Others
	N-methyltaxol C and paclitaxel can produce a positive inotropic effect in papillary muscle, without alterations in the action potential. They can induced conduction arrhythmias and reduce coronary flow and left ventricular systolic pressure in the isolate
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

DL-Homocysteine thiolactone hydrochloride

Cat.No: T5968

Synonym: DL-Homocysteinethiolactone hydrochloride,DL-高半胱氨酸硫内酯盐酸盐

Target: Endogenous Metabolite

α-Angelica lactone

Cat.No: T7995

Synonym: α-当归内酯,当归内酯,Alpha-Angelica Lactone

Target: Others, GST

Cat.No: T3123

Target: ERK, IL Receptor, Others, IκB/IKK, p38 MAPK, TNF, ROS, Caspase, Antifection

N-Methyltaxol C

Cat.No: TN4616

Target: Others

Cat.No: TN2001

Target: Others

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