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17

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T7845 BTZO-1

Apoptosis Apoptosis
BTZO-1 是一种具有心脏保护活性的抗氧化反应元件激活剂。它可以结合巨噬细胞迁移抑制因子,结合的Kd 值为 68.6 nM,并且其结合需要 N 末端 Pro1。
T16104 ML-9

Myosin; Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
ML-9 是 Akt 激酶的一种选择性强效抑制剂,可抑制肌球蛋白轻链激酶 (MLCK) 和基质相互作用分子1(STIM1) 活性。它通过刺激自噬小体的形成并抑制其降解来诱导自噬。它抑制 MLCK,PKA 和 PKC 活性,Ki 值分别为 4、32 和 54 μM。
T2052 KY02111

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
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。
T8786 VUT-MK142

Others Others
VUT-MK142 是强效心肌合成剂,能够诱导心脏前中胚层向心肌细胞分化,促进干细胞向心肌细胞分化进行的心脏修复。
TP1035 Cyclic somatostatin

SRIF-14,合成生长抑素,环状生长激素抑制素,Somatostatin-14

Others Others
Cyclic somatostatin (SRIF-14) 是生长激素释放抑制因子,可用于研究胃十二指肠溃疡出血。
T3597 Cutamesine dihydrochloride

AGY94806 dihydrochloride,库他美新二盐酸盐,SA4503 (dihydrochloride),SA4503 dihydrochloride

Sigma receptor GPCR/G Protein
Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种选择性 σ1 受体激动剂,IC50值为 17.4 nM。
T5483 DMX-5804

DMX-5084

MAPK MAPK
DMX-5804 是一种口服有活性的MAP4K4选择性抑制剂,其对人 MAP4K4 的IC50=3 nM,pIC50=8.55。对 MINK1/MAP4K6 (pIC50=8.18) 和 TNIK/MAP4K7 (pIC50=7.96) 的作用相对较弱。它可以提高心肌细胞存活率,降低小鼠的缺血再灌注损伤。
TP2158 TRV-120027 TFA

TRV-120027 TFA (1234510-46-3 free base)

RAAS; Arrestin Endocrinology/Hormones; GPCR/G Protein
TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂,可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂,可与 ß-arrestins 结合,同时阻断 G 蛋白信号传导。 它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌,并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。
T35832 Brain Natriuretic Peptide (1-32), rat acetate

Brain Natriuretic Peptide (1-32), rat acetate (BNP (1-32), rat acetate) is a 32 amino acid polypeptide hormone synthesized by ventricular cardiomyocytes as a result of myocardial cell stretching (cardiomyocyte distension)[1].
TP2158L TRV-120027

Others Others
TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility.
T35875 CCG258208 hydrochloride

GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1]. [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):305...
T62986 CCG-271423

CCG-271423 是一种有效的、选择性的 GRK5 抑制剂,作用于 GRK5 (IC50: 0.0021 μM) 和 GRK2 (IC50: 44 μM)。CCG-271423 能够降低 Ca2+瞬态,抑制心肌细胞收缩能力。
T76252L WLSEAGPVVTVRALRGTGSW TFA

WLSEAGPVVTVTVRALGTGSW TFA 为心肌细胞特异性肽。该化合物通过表达外泌体,提高心肌细胞的特定摄取能力,降低心肌细胞凋亡率,并在体内心肌内注射后提升心脏潴留能力。
T60825 FC9402

FC9402 是硫化物醌氧化还原酶 (SQOR) 的高效选择性抑制剂。FC9402 可调节心血管,减轻 TAC 诱导的心肌细胞肥大和左心室 (LV) 纤维化。
T80130 SDF-1α (human)

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
SDF-1α (human) 是一种能够与CXCR4受体相结合的单核细胞趋化剂,它在心肌梗死模型中的干细胞归巢、维持、生存、增殖、心肌细胞修复、血管形成以及心室重构过程扮演关键角色。SDF-1α (human) 常用于心血管病研究。
T35541 Lipoxygenin

Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin...
T36215 17R(18S)-EpETE

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases ...

化合物

BTZO-1
Cat.No: T7845
Synonym:
Target: Apoptosis
ML-9
Cat.No: T16104
Synonym:
Target: Myosin, Akt
KY02111
Cat.No: T2052
Synonym:
Target: Wnt/beta-catenin
VUT-MK142
Cat.No: T8786
Synonym:
Target: Others
Cyclic somatostatin
Cat.No: TP1035
Synonym: SRIF-14,合成生长抑素,环状生长激素抑制素,Somatostatin-14
Target: Others
Cutamesine dihydrochloride
Cat.No: T3597
Synonym: AGY94806 dihydrochloride,库他美新二盐酸盐,SA4503 (dihydrochloride),SA4503 dihydrochloride
Target: Sigma receptor
DMX-5804
Cat.No: T5483
Synonym: DMX-5084
Target: MAPK
TRV-120027 TFA
Cat.No: TP2158
Synonym: TRV-120027 TFA (1234510-46-3 free base)
Target: RAAS, Arrestin
Brain Natriuretic Peptide (1-32), rat acetate
Cat.No: T35832
Synonym:
Target:
TRV-120027
Cat.No: TP2158L
Synonym:
Target: Others
CCG258208 hydrochloride
Cat.No: T35875
Synonym:
Target:
CCG-271423
Cat.No: T62986
Synonym:
Target:
WLSEAGPVVTVRALRGTGSW TFA
Cat.No: T76252L
Synonym:
Target:
FC9402
Cat.No: T60825
Synonym:
Target:
SDF-1α (human)
Cat.No: T80130
Synonym:
Target: CXCR
Lipoxygenin
Cat.No: T35541
Synonym:
Target:
17R(18S)-EpETE
Cat.No: T36215
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN4892 Randialic acid B

Others Others
Randialic acid B shows significant cell-protective effects against H2O2-induced H9c2 cardiomyocyte injury.
T36667 2'-Deoxyadenosine-5'-triphosphate

dATP,Deoxyadenosine 5-triphosphate

DNA/RNA Synthesis; Endogenous Metabolite Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
2'-Deoxyadenosine-5'-triphosphate (Deoxyadenosine 5-triphosphate) (dATP) 是一种天然存在的小分子核苷酸,在细胞中用于DNA合成或复制。2'-Deoxyadenosine-5'-triphosphate (dATP) 是 DNA 聚合酶的底物。2'-Deoxyadenosine-5'-triphosphate 通过无活性的 α4beta4 四级结构抑制RNA。2'-Deoxyadenosine-5'-triphosphate 与心肌细胞生长有关。

天然产物

Randialic acid B
Cat.No: TN4892
Synonym:
Target: Others
2'-Deoxyadenosine-5'-triphosphate
Cat.No: T36667
Synonym: dATP,Deoxyadenosine 5-triphosphate
Target: DNA/RNA Synthesis, Endogenous Metabolite
TargetMol Loading
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