human cardiac

Mavacamten (MYK-461) 是一种可口服的心肌肌球蛋白 ATP 酶抑制剂，在牛心脏和人心脏中的IC50值分别为 490和711 nM。

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。

Human cardiac troponin (mixture) (cTn) 是一种调节蛋白，位于收缩蛋白的细肌丝上，对肌肉组织的收缩与舒张发挥重要的调控作用。

MIV-247 是一种具有选择性和高效性的 cathepsin S 抑制剂（人、小鼠和野猴 cathepsin S 的 Kis 分别为 2.1、4.2 和 7.5 nM），可减轻临床前神经性疼痛模型中的机械性异常性疼痛，可用于研究心肌损伤。

GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性，并减弱了心脏重塑。它减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。

Neriifolin (17β-Neriifolin) 是一种从 Cerbera manghas 未熟果实中提取的强心苷，是一种 Na+K+-ATPase 抑制剂，具有抗癌活性，通过抑制 HOXA9 依赖性基因表达和诱导人急性髓细胞系 THP-1 细胞凋亡抑制细胞增殖。Neriifolin 诱导人肝癌 HepG2 细胞周期阻滞和凋亡，可用于研究前列腺癌。

Halofantrine hydrochloride(SKF-102886)是一种可口服的抗疟疾药，对耐药的P. falciparum和P. vivax有效。SKF-102886具有心脏毒性，能够抑制hERG和延迟整流钾通道I Kr，导致QTc和PR间期延长。

ALK5-IN-82 是一种激活素受体样激酶 5 (ALK5) 的高选择性抑制剂，其IC50值仅为 9.1 nM。该化合物能够有效抑制转化生长因子-β 在人脐静脉内皮细胞中诱导的 α-平滑肌肌动蛋白 (α-SMA)、胶原蛋白 I 以及金属蛋白酶抑制剂 1 (TIMP-1) 和基质金属蛋白酶 13 (MMP‐13) 的表达。因此，ALK5-IN-82 有潜力应用于心脏纤维化的相关研究。

Pyrocatechol sulfate 是一种在人体血浆中发现的酚类代谢物，与摄入浆果等特定食物及肠道菌群状态有关。该化合物可能用作监测肾功能、透析清除率、全谷物与常规咖啡的摄入量的尿液生物标记。同时，Pyrocatechol sulfate 与其他酚类硫酸盐共同参与调节多种生物学功能，这些功能涉及大脑健康与心肌细胞的节律性跳动。

Adekalant（又名H 345 52）是一种新型抗心律失常化合物，具有低促心律失常活性。该化合物浓度依赖性地阻断HERG携带的电流，其半抑制浓度（IC50）为230 nM。Adekalant优先与开放状态的通道结合，并显示出异常快的动力学特性，通道关闭时被捕获。在方波脉冲和动作电位夹持协议期间观察到Adekalant的电压独立行为。研究提出，通过阻断I(Kr)来延迟人类心肌的复极是Adekalant发挥作用的主要机制。Adekalant高效阻断I(Kr)，相对较低效地阻断I(Ca)，且能延迟心室复极，而不会显著增加时间或空间的离散度，也不诱发早期后除极或TdP。

Uridine triphosphate (UTP) 是一种潜在用于治疗肺癌的嘌呤核苷酸P2U受体激动剂。它通过激活P2Y2受体增加人类癌变胰管上皮细胞的增殖。此外，Uridine triphosphate (UTP) 通过激活P2Y2受体，在心脏成纤维细胞中诱导纤维化反应。同时，UTP通过P2Y2嘌呤受体延长豚鼠乳头肌的动作电位时长。

KY02111 是典型的 WNT 信号抑制剂，能够促进人多潜能干细胞向心肌细胞分化，可用于研究人类心肌细胞再生。

Urotensin-II receptor antagonist-1 (compound 1) 是一种选择性拮抗人类Urotensin II受体的化合物，具低口服生物利用度 (F=0-3%，大鼠)，在表达人重组 UT 受体的 HEK293 细胞中测试Ki为16 nM。Urotensin-II receptor antagonist-1 能抑制细胞色素 P450 (IC50=0.75 μM，CYP2D6；1.4 μM，CYP3A4)，还能够抑制 κ 阿片受体 (EC50=3.2 μM)，并以Ki=2.5 μM对心脏钠通道产生作用。

Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。

Epothilone F is a derivative or analogue of Epothilone D. Epothilone F is also an active metabolite of Epothilone D. In molecule of Epothilone F, a hydroxymethyl group is on the thiazole ring. Like taxanes, Epothilone F prevents cancer cells from dividing

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 cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3’,5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3’-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

(R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC 50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..

TM5441 是口服生物可利用的纤溶酶原激活物抑制剂-1 抑制剂，抑制多个癌症细胞系的 IC50值在 13.9 到 51.1 μM。它诱导几种人类癌症细胞的内在调亡，减弱 Nω-硝基-1-精氨酸甲酯诱导的心脏高血压和血管衰老。

(Rac)-Indoximod (1-Methyl-DL-tryptophan) is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO). Combined treatment with IFN-γ and (Rac)-Indoximod significantly suppresses the activity of α-SMA-expressing human cardiac myofibroblasts (hCMs) and promotes apoptosis by up-regulating the genes IRF-1, Fas, and FasL. Moreover, this co-treatment effectively improves cardiac fibrosis[1].

JB062是一种针对非肌肉肌球蛋白(nonmusclemyosin)的抑制剂，其IC50值对骨骼肌肌球蛋白为1.6μM、心肌肌球蛋白为5.4μM，而对平滑肌肌球蛋白II大于100μM。此化合物对人类癌细胞显示出细胞毒性，对正常细胞则无此作用。JB062在肌肉痉挛、慢性肌肉骨骼疼痛及肥厚型心肌病研究中有潜在应用价值。

Angiotensin II 是一种主要的生物活性血管收缩肽，通过与AT1R和AT2R受体结合，调节血压，刺激交感神经，促进醛固酮合成和肾脏功能。它还能诱导血管平滑肌细胞增生、胶原合成增加，导致血管和心肌增厚及纤维化，同时促进细胞凋亡和内皮细胞毛细血管形成。Angiotensin II常用于诱导高血压和心脏肥大动物模型。

Eleclazine(GS-6615)是一种新型和选择性的电压门控钠离子通道抑制剂，具有抗心律失常的作用，减少对人诱导多能干细胞来源的心肌细胞记录的峰值钠电流。

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg ml. Gliclazide (5 mg kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).