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29

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T9023 Atuliflapon

AZD5718

FLAP Immunology/Inflammation
Atuliflapon (AZD5718) 是可口服的FLAP(5 -脂氧合酶激活蛋白)的抑制剂,IC50值为 2 nM,可用于冠状动脉疾病的研究。
T6033 Zotarolimus

ABT-578,佐他莫司,咗他莫司,A 179578

mTOR PI3K/Akt/mTOR signaling
Zotarolimus (ABT-578) 是一种免疫抑制剂,是雷帕霉素的衍生物,具有抗增殖活性。它被专门开发作为局部输送支架用于预防冠状动脉再狭窄。
T0154 Nebivolol hydrochloride

R 065824 hydrochloride,盐酸奈必洛尔,Nebivolol HCl,R-65824

Apoptosis; Adrenergic Receptor Apoptosis; GPCR/G Protein; Neuroscience
Nebivolol hydrochloride (R 065824 hydrochloride) 是一种β1-肾上腺素受体选择性抑制剂,IC50为0.8 nM。
T8687 diaminohydroxypropanetetraacetic acid

Others Others
diaminohydroxypropanetetraacetic acid 已被研究用于治疗血管疾病、冠状动脉疾病、心肌缺血、冠状动脉再狭窄和冠状动脉疾病等。
T19345 GP2-114

Others Others
GP2-114 是一种儿茶酚胺运动模拟剂 ,可用于研究冠状动脉疾病 (CAD)。
T1986 Atopaxar

E5555,ER-172594-00

Protease-activated Receptor GPCR/G Protein
Atopaxar (E5555) 是一种高效、可口服的,选择性的,可逆的凝血酶受体蛋白酶激活受体-1 (PAR-1) 拮抗剂。它是一种抗血小板剂,能干扰血小板信号,可用于动脉粥样硬化血栓性疾病的研究。
T32155 Indecainide

Ricainide,Ricainid,Decabid,Indecainidum,Indecainida

Others Others
Indecainide (Ricainid) 是一种新型抗心律失常化合物,具有致癌性,可用于研究继发于冠状动脉疾病或心肌病的慢性稳定型室性心律失常。
T0182L2 (±) Clopidogrel hydrogen sulfate

硫酸氢氯吡格雷,Plavix,Clopidogrel hydrogen sulfate,Iscover

P2Y Receptor GPCR/G Protein; Neuroscience
(±) Clopidogrel hydrogen sulfate (Iscover) 是一种在药理学和结构上类似于ticlopidine 的抗血小板药物,用于抑制脑血管疾病、外周血管疾病和冠状动脉疾病等各种疾病中的血栓。
T2480 Apabetalone

RVX-208,RVX000222,阿帕他隆

Epigenetic Reader Domain; HIV Protease Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome
Apabetalone (RVX000222) 是一种 BET 溴结构域抑制剂,用于研究治疗糖尿病、动脉粥样硬化和冠状动脉疾病。
T4179 Probucol disuccinate

LDL Metabolism
Probucol disucinate 是一种 Probucol 的衍生物。其中 Probucol 是脂质调节的化合物,它能降低 LDL-cholesterol 水平。
T61028 Mitiperstat

AZD4831

Glutathione Peroxidase Metabolism
Mitiperstat 是一种强效的骨髓过氧化物酶(MPO)抑制剂。Mitiperstat 对预防如心力衰竭和冠状动脉疾病类的心血管疾病有很好的效果。
T4287 Succinobucol

Probucol monosuccinate,AGI-1067

Antioxidant; Reactive Oxygen Species Immunology/Inflammation; Metabolism; NF-κB; oxidation-reduction
Succinobucol (Probucol monosuccinate) 是酚类抗氧化剂,具有抗炎、抗血小板聚集活性。
T10364 Arbutamine

GP 21213

Adrenergic Receptor GPCR/G Protein; Neuroscience
Arbutamine (GP 21213) 是一种新型非选择性β-肾上腺素受体激动剂,具有α-1-拟交感神经活性。Arbutamine 促进心脏应激,增加心率、心脏收缩力。Arbutamine 可用于研究心脏应激和冠状动脉疾病。
T31992 Granotapide

CETP Metabolism
Granotapide 是一种微粒体甘油三酯转移蛋白(MTP)抑制剂,治疗和而预防动脉硬化,冠状动脉疾病,代谢综合征,肥胖,糖尿病,糖尿病前期和高血压。
T73695 Canakinumab

ACZ 885,Ilaris

IL Receptor Immunology/Inflammation
Canakinumab (ACZ885) 是一种重组人靶向 IL-1β 单克隆抗体。Canakinumab 显示出对人类和绒猴 IL-1β 具有抑制作用, IC50 值为分别为 43.6 和 40.8 pM。Canakinumab 具有抗炎活性,通过中和 IL-1β 信号来抑制与自身免疫性疾病相关的炎症。Canakinumab 可用于治疗痛风和冠状动脉疾病。
T14390L (2R,3S)-Azelaprag

Apelin receptor GPCR/G Protein
(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide 是一种Apelin 受体激动剂,对Apelin 受体的EC50为0.012 µM。(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide 可用于治疗心力衰竭、动脉粥样硬化、肥胖、糖尿病、肌萎缩侧索硬化、冠心病、高血压、中风和心肌梗塞等疾病。
T30255 AZD2716

AZD 2716,AZD-2716

AZD2716 is an effective selective phospholipase A2 inhibitor for the treatment of coronary artery and cardiovascular disease.
T26739 Batifiban

Batifiban, a glycoprotein IIb/IIIa antagonist, is used potentially for the treatment of coronary artery disease.
T69970 AZD5718

AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease.
T1986L Atopaxar Hydrobromide

Protease-activated Receptor GPCR/G Protein
Atopaxar hydrobromide 是可口服的,高效选择性的可逆凝血酶受体蛋白酶激活受体-1 拮抗剂。它是一种抗血小板剂,能干扰血小板信号,用于动脉粥样硬化血栓性疾病的研究。
T68639 Ciprostene (free base)

Ciprostene (free base) is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.
T79239 PCSK9-IN-19

PCSK9-IN-19 (Compound 1)作为一种PCSK9抑制剂,用于研究高LDL胆固醇水平及预防冠状动脉疾病。
T68297 Dilmapimod tosylate

Dilmapimod tosylate is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor. It was investigated for its anti-inflammatory effect in non-head injury trauma patients at risk for developing acute respiratory distress syndrome. IL-1β was identified as a gene regulated by dilmapimod that could influence c-reactive protein levels. Dilmapimod had been in phase III clinical trials by GlaxoSmithKline for the treatment of rheumatoid arthritis, neuropathic pain, coronary artery disease (CAD) and...
T60901 S(-)-Bisoprolol

S(-)-Bisoprolol 是 Bisoprolol 的 S(-)-对映异构体。Bisoprolol 在高血压,冠状动脉疾病和稳定的心室功能不全的研究方面具有潜力。Bisoprolol 是一种有效的选择性的,口服活性的 β1 肾上腺素受体阻滞剂,对 β2 受体几乎没有活性。
T63035 Izilendustat hydrochloride

Izilendustat (hydrochloride) 是一种脯氨酰羟化酶 (prolyl hydroxylase) 的有效抑制剂,能够稳定缺氧诱导因子-1 α (HIF-1α) 和缺氧诱导因子-2 (HIF-2)。Izilendustat (hydrochloride) 具有潜力进行 HIF-1α 相关疾病的研究(包括外周血管疾病(PVD)、心力衰竭、冠状动脉疾病(CAD)、缺血、贫血、结肠炎和其他炎症性肠病)。
T17231 Vicagrel

Others Others
Vicagrel 是一种有效的、具有口服活性抗血小板化合物,通过不可逆地抑制 P2Y12 受体,降低代谢失活,增强了阿司匹林对啮齿类动物血小板聚集和血栓形成起抑制作用。Viagrel 可用于治疗冠状动脉疾病、外周血管疾病和脑血管疾病中血栓。
T74156 S(-)-Bisoprolol fumarate

S(-)-Bisoprolol fumarate 是 Bisoprolol fumarate 的 S(-)-对映异构体,这种化合物是一种有效的、选择性的,并具有口服活性的 β1 肾上腺素受体 (β1-adrenergic receptor) 阻滞剂,对 β2 受体的活性较低。它主要用于研究高血压、冠状动脉疾病和稳定的心室功能障碍。
T21485 Perindopril

Perindopril (S-9490) 是一种长效血管紧张素转换酶(ACE)抑制剂,用于治疗高血压、心力衰竭或稳定性冠状动脉疾病。
T81451 PKCd (8-17)

PKCd (8-17) 是源自蛋白激酶 C (PKC)d V1 结构域的生物活性肽。它能抑制由佛波醇 12-肉豆蔻酸酯 13-乙酸酯 (PMA) 诱导的 PKCd 易位和激活。此外,PKCd (8-17) 在降低心脏和脑细胞缺血损伤、促进成纤维细胞增殖、以及抑制小鼠移植冠状动脉疾病方面具有潜在应用。

化合物

Atuliflapon
Cat.No: T9023
Synonym: AZD5718
Target: FLAP
Zotarolimus
Cat.No: T6033
Synonym: ABT-578,佐他莫司,咗他莫司,A 179578
Target: mTOR
Nebivolol hydrochloride
Cat.No: T0154
Synonym: R 065824 hydrochloride,盐酸奈必洛尔,Nebivolol HCl,R-65824
Target: Apoptosis, Adrenergic Receptor
diaminohydroxypropanetetraacetic acid
Cat.No: T8687
Synonym:
Target: Others
GP2-114
Cat.No: T19345
Synonym:
Target: Others
Atopaxar
Cat.No: T1986
Synonym: E5555,ER-172594-00
Target: Protease-activated Receptor
Indecainide
Cat.No: T32155
Synonym: Ricainide,Ricainid,Decabid,Indecainidum,Indecainida
Target: Others
(±) Clopidogrel hydrogen sulfate
Cat.No: T0182L2
Synonym: 硫酸氢氯吡格雷,Plavix,Clopidogrel hydrogen sulfate,Iscover
Target: P2Y Receptor
Apabetalone
Cat.No: T2480
Synonym: RVX-208,RVX000222,阿帕他隆
Target: Epigenetic Reader Domain, HIV Protease
Probucol disuccinate
Cat.No: T4179
Synonym:
Target: LDL
Mitiperstat
Cat.No: T61028
Synonym: AZD4831
Target: Glutathione Peroxidase
Succinobucol
Cat.No: T4287
Synonym: Probucol monosuccinate,AGI-1067
Target: Antioxidant, Reactive Oxygen Species
Arbutamine
Cat.No: T10364
Synonym: GP 21213
Target: Adrenergic Receptor
Granotapide
Cat.No: T31992
Synonym:
Target: CETP
Canakinumab
Cat.No: T73695
Synonym: ACZ 885,Ilaris
Target: IL Receptor
(2R,3S)-Azelaprag
Cat.No: T14390L
Synonym:
Target: Apelin receptor
AZD2716
Cat.No: T30255
Synonym: AZD 2716,AZD-2716
Target:
Batifiban
Cat.No: T26739
Synonym:
Target:
AZD5718
Cat.No: T69970
Synonym:
Target:
Atopaxar Hydrobromide
Cat.No: T1986L
Synonym:
Target: Protease-activated Receptor
Ciprostene (free base)
Cat.No: T68639
Synonym:
Target:
PCSK9-IN-19
Cat.No: T79239
Synonym:
Target:
Dilmapimod tosylate
Cat.No: T68297
Synonym:
Target:
S(-)-Bisoprolol
Cat.No: T60901
Synonym:
Target:
Izilendustat hydrochloride
Cat.No: T63035
Synonym:
Target:
Vicagrel
Cat.No: T17231
Synonym:
Target: Others
S(-)-Bisoprolol fumarate
Cat.No: T74156
Synonym:
Target:
Perindopril
Cat.No: T21485
Synonym:
Target:
PKCd (8-17)
Cat.No: T81451
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN6715 7-Ketocholesterol

Others Others
7-Ketocholesterol 是胆固醇的代谢物。
S00015 Tea polyphenol

Apoptosis; Others; Autophagy Apoptosis; Autophagy; Others
Tea polyphenol 也称为绿茶提取物,是茶中天然存在的酚类化合物,具有抗癌、抗氧化、抑制细胞增殖、诱导细胞凋亡、延缓细胞周期和调节致癌物代谢等生物活性。

天然产物

7-Ketocholesterol
Cat.No: TN6715
Synonym:
Target: Others
Tea polyphenol
Cat.No: S00015
Synonym:
Target: Apoptosis, Others, Autophagy
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