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18

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8674 SR33805

Calcium Channel Membrane transporter/Ion channel; Metabolism
SR33805 是钙通道拮抗剂,在去极化和极化条件下的 EC50值分别为 4.1 和 33 nM。它阻止 L 型 Ca2+通道,可用于研究急性或慢性心脏衰竭。
T12321 ORM-10103

Calcium Channel Membrane transporter/Ion channel; Metabolism
ORM-10103 是一种新型有效且具有选择性的 Na+/Ca2+ 交换体 (NCX) 抑制剂。ORM-10103 对 NCX 电流有抑制作用,在 -80 和 20 mV 下的 IC50 的估算值分别为 55 和 67 nM,可减少犬心脏的早期和延迟后去极化。
T60247 Diethylamine NONOate diethylammonium salt

NOC-18 Diethylamine,DEA NONOate diethylamine

Antibiotic Microbiology/Virology
Diethylamine NONOate diethylammonium salt (DEA NONOate diethylamine) 是一种一氧化氮供体,具有抗菌活性,是铜绿假单胞菌生物膜预形成生物膜的分散剂,可抑制大肠杆菌的生长。Diethylamine NONOate diethylammonium salt 可用于离体大鼠心脏的保存。
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。
T16420 P-1075

Potassium Channel Membrane transporter/Ion channel
P-1075 是磺酰脲受体2相关的 ATP 敏感性的钾通道(SUR2-KIR6)的激活剂,EC50为 45 nM。它在兔子中通过打开线粒体 K (ATP) 通道产生活性氧,产生保护心脏的功效。
T26621 AMP-579

RPR100579,RPR 100579,AMP 579,RPR-100579

AMP-579 is an adenosine A1 receptor agonist. AMP-579 also acts as a A2b-adenosine receptor agonist in human 293 cells and rabbit hearts.
T24145 Hns 32

Hns32,Hns-32

Hns 32 possesses antiarrhythmic properties in dog and guinea pig hearts. It also has vasodilator action.
T13588 Ipramidil

C80-1324,异丙地尔

Others Others
Ipramidil (C80-1324) reveals marked dilator activity in the coronary circulation of isolated working hearts.
T75953 BeKm-1 TFA

BeKm-1 TFA is a potent, selective blocker of the KV11.1 (hERG) channel, demonstrating specificity for KV11.1 over 14 other potassium channels. This compound dose-dependently prolongs the QTc interval in isolated rabbit hearts, affirming its role as a selective inhibitor.
TP1923 Elabela(19-32)

ELA-14 (human)

Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo.
T68878 L-2286

L-2286 is a novel PARP inhibitor. L-2286 exerted significant protective effect against ischemia-reperfusion-induced myocardial injury in both experimental models. More importantly, L-2286 facilitated the ischemia-reperfusion-induced activation of Akt, extracellular signal-regulated kinase, and p38-MAPK in both isolated hearts and in vivo cardiac injury.
T40850 [D-Trp11]-Neurotensin

[D-Trp11]-Neurotensin

[D-Trp11]-Neurotensin is a compound that functions as a selective antagonist of Neurotensin (NT) in perfused rat hearts, while exhibiting full agonist properties in guinea pig atria and rat stomach strips. Additionally, this compound can inhibit hypotension induced by NT.
TP2096 ELA-21 (human)

High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc
T35873 C19 Ceramide (d18:1/19:0)

C19 Ceramide (d18:1/19:0)

C19 Ceramide is a naturally occurring ceramide that has been found in J. juncea extracts as well as rat brain and mouse heart.[1],[2],[3] It is elevated in adult and decreased in juvenile whole rat brain extracts by 114 and 37%, respectively, following chronic ethanol exposure.[2] C19 Ceramide is also increased in mouse hearts following administration of angiotensin II.[3]
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...
T83880 C18 Ceramide-1-phosphate (d18:1/18:0) ammonium

Ceramide-1-phosphate (d18:1/18:0),N-octadecanoyl-D-erythro-Sphingosine-1-phosphate,C18 Ceramide-1-phosphate,C18 C1P,CerP(d18:1/18:0),N-stearoyl-D-erythro-Sphingosine-1-phosphate

C18 Ceramide-1-phosphate (d18:1/18:0) 是一种在鼠皮肤中发现的长链ceramide-1-phosphate。它能在0.5至5 µM的浓度范围内促进分离的小鼠骨髓来源的多能间充质细胞和人脐静脉内皮细胞(HUVECs)的迁移。与胰腺癌干细胞相比,CFPAC-1胰管腺癌细胞中C18 Ceramide-1-phosphate (d18:1/18:0)的水平有所增加。在Langendorff分离的灌流小鼠心脏的离体缺血模型中,心肌中C18 ceramide-1-phosphate (d18:1/18:0)的水平有所增加。
T74988 DIBA-Cy5

DIBA-Cy5 是一种 DIBA 荧光拮抗剂,由 DIBA-炔结合 Cyanine5 荧光团 (Cy5) 和聚乙二醇 (PEG) 生物分子组成。DIBA-Cy5 可以作为荧光配体,适合通过点击化学附着探针。DIBA-Cy5 对 type-2mAChR(M2R) 具有很高的结合亲和力 ( Kd=1.80 nM),可直接染色小鼠窦房结的 M2R 受体。
T83677 Neuropeptide Y (porcine, bovine) TFA

NPY (porcine, bovine)

神经肽Y(Neuropeptide Y, NPY)是一种参与调节食欲、血管收缩、心脏收缩力和肠道分泌的神经肽,同时也是NPY受体Y1、Y2和Y5的激动剂。它在全身范围内表达。NPY能够在表达大鼠Y1或Y2以及表达大鼠Y5的HEK293细胞中选择性抑制由forskolin诱导的cAMP积累,而对表达大鼠Y4受体的L-M(TK-)细胞的影响较小(EC50分别为0.15、2.7、0.66和>1,000 nM)。在分离的豚鼠心脏模型中,NPY能够增加灌注压(EC30 = 1.3 nM)。神经内注射NPY(300 pmol/动物)能够在大鼠中增加食物摄取量。

化合物

SR33805
Cat.No: T8674
Synonym:
Target: Calcium Channel
ORM-10103
Cat.No: T12321
Synonym:
Target: Calcium Channel
Diethylamine NONOate diethylammonium salt
Cat.No: T60247
Synonym: NOC-18 Diethylamine,DEA NONOate diethylamine
Target: Antibiotic
Adrenochrome
Cat.No: T20094
Synonym: Adraxone
Target: Antioxidant
P-1075
Cat.No: T16420
Synonym:
Target: Potassium Channel
AMP-579
Cat.No: T26621
Synonym: RPR100579,RPR 100579,AMP 579,RPR-100579
Target:
Hns 32
Cat.No: T24145
Synonym: Hns32,Hns-32
Target:
Ipramidil
Cat.No: T13588
Synonym: C80-1324,异丙地尔
Target: Others
BeKm-1 TFA
Cat.No: T75953
Synonym:
Target:
Elabela(19-32)
Cat.No: TP1923
Synonym: ELA-14 (human)
Target:
L-2286
Cat.No: T68878
Synonym:
Target:
[D-Trp11]-Neurotensin
Cat.No: T40850
Synonym: [D-Trp11]-Neurotensin
Target:
ELA-21 (human)
Cat.No: TP2096
Synonym:
Target:
C19 Ceramide (d18:1/19:0)
Cat.No: T35873
Synonym: C19 Ceramide (d18:1/19:0)
Target:
(3S)-hydroxy Quinidine
Cat.No: T36561
Synonym:
Target:
C18 Ceramide-1-phosphate (d18:1/18:0) ammonium
Cat.No: T83880
Synonym: Ceramide-1-phosphate (d18:1/18:0),N-octadecanoyl-D-erythro-Sphingosine-1-phosphate,C18 Ceramide-1-phosphate,C18 C1P,CerP(d18:1/18:0),N-stearoyl-D-erythro-Sphingosine-1-phosphate
Target:
DIBA-Cy5
Cat.No: T74988
Synonym:
Target:
Neuropeptide Y (porcine, bovine) TFA
Cat.No: T83677
Synonym: NPY (porcine, bovine)
Target:
Cat. No. Product Name Target Signaling Pathways
T4518 Licochalcone D

ERK; NF-κB MAPK; NF-κB
Licochalcone D 是一种 NF-κB p65的有效抑制剂,是一种存在于 Glycyrrhiza inflate 中的黄酮类化合物,具有抗氧化、抗炎、抗癌等作用。
T2973 Astragaloside IV

AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV

MMP; ERK; Estrogen/progestogen Receptor; JNK Endocrinology/Hormones; MAPK; Proteases/Proteasome
Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷,抑制ERK1/2和JNK 激活,在乳腺癌细胞 MDA-MB-231 中,下调(MMP)-2和(MMP)-9的信号通路。
TN1412 Astringin

trans-Astringin,白皮杉醇葡萄糖苷

IL Receptor; Others Immunology/Inflammation; Others
Astringinin is a potent antiarrhythmic agent with cardioprotective activity in ischemic and ischemic-reperfused rat heart, the beneficial effects of astringinin in the ischemic and ischemic-reperfused hearts may be correlated with its antioxidant activity and upregulation of NO production.
TN3914 Echinatine

ATPase; IL Receptor; TNF Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel
Echinatin exerts a protective effect against ischemia/reperfusion (I/R)-induced myocardial injury on hearts, this effect may be attributed to the antioxidant and anti-inflammatory activities of this compound. Echinatin can inhibit DNP-ATPase activity whil

天然产物

Licochalcone D
Cat.No: T4518
Synonym:
Target: ERK, NF-κB
Astragaloside IV
Cat.No: T2973
Synonym: AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV
Target: MMP, ERK, Estrogen/progestogen Receptor, JNK
Astringin
Cat.No: TN1412
Synonym: trans-Astringin,白皮杉醇葡萄糖苷
Target: IL Receptor, Others
Echinatine
Cat.No: TN3914
Synonym:
Target: ATPase, IL Receptor, TNF
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