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26

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T22012 7BIO

FLT; DYRK; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
7BIO 是靛玉红的衍生物,抑制细胞周期蛋白依赖性激酶5 和糖原合酶激酶-3β。它抑制 Aβ 寡聚体诱导的神经炎症、突触损伤、tau 过度磷酸化、星形胶质细胞和小胶质细胞的活化,并减轻 Aβ 寡聚体诱导的小鼠认知障碍。
T6493 Escitalopram Oxalate

草酸右旋西酞普兰,依他普仑草酸盐,Cipralex,(S)-(+)Citalopram oxalate

Others; 5-HT Receptor; Serotonin Transporter GPCR/G Protein; Neuroscience; Others
Escitalopram Oxalate ((S)-(+)Citalopram oxalate) 是一种外消旋 Citalopram 的 S-对映体,是一种选择性 5-羟色胺再摄取抑制剂,Ki=0.89 nM,比 R(-)-enantiomer 结合亲和力高 30 倍。它对多巴胺转运体和去甲肾上腺素转运体均有选择性,是一种研究抑郁症的抗抑郁药。
T7114 GALANTHAMINONE

(-)-Narwedine,氢溴酸加兰他敏,Narwedin

AChE Neuroscience
Galanthaminone ((-)-Narwedine) 是一种竞争性的、可逆的胆碱酯酶抑制剂,可作用于多种记忆障碍疾病的研究。
T16518 PH-002

Others Others
PH-002 是一种抑制载脂蛋白 E4 神经内分子相互作用的抑制剂(IC50:116 nM)。
T1128 Oxiracetam

奥拉西坦,ISF2522

GABA Receptor Membrane transporter/Ion channel; Neuroscience
Oxiracetam (ISF2522) 是一种 γ-氨基丁酸 (GABA) 的环状衍生物,可用于治疗认知障碍。
T14507 Bay 60-7550

BAY 607550

PDE Metabolism
Bay 60-7550 是一种具有选择性和高效性的 PDE2 抑制剂(Ki:3.8 nM),通过增加 PKA 介导的磷酸化来发挥大鼠心脏的正性肌力作用,可用于改善认知障碍和记忆障碍。
T7165 Basmisanil

RG1662,RO5186582,巴米沙尼

GABA Receptor Membrane transporter/Ion channel; Neuroscience
Basmisanil (RG1662) 是高度选择性GABAAα5负调节剂,用于治疗与唐氏综合症相关的认知障碍。
T14782 Brilaroxazine

RP5063

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
Brilaroxazine (RP5063) 是一种有效的多模式多巴胺/5-HT 调节剂。 Brilaroxazine 是多巴胺 D2、D3 和 D4 受体、5-HT1A (Ki = 1.5 nM) 和 5-HT2A (Ki = 2.5 nM) 的部分激动剂,具有拮抗活性 5-HT2B 和 5-HT7 受体,Ki 分别为 0.19 nM 和 2.7 nM。 Brilaroxazine 可用于研究神经精神和神经系统疾病的认知障碍。
T26646 AQW051

AQ W051,VQW-765,AQW-051

AChR Neuroscience
AQW051 (VQW-765)是一种口服活性alpha -7烟碱乙酰胆碱受体(α7-nAChR)特异性激活剂,与重组人alpha7-nAChR 表达相互作用(pKD 值7.56)。alpha7-nAChR 被认为是治疗与神经障碍相关的认知障碍的一个有吸引力的靶点,因此VQW-051经常用于焦虑障碍和急性焦虑的研究
T25005 AF267

(±)AF 267,(±) AF 267,(±)-AF 267,AF 267,AF-267

AF267 is a M1 muscarinic agonist that works by restoring cognitive impairments.
T68377 GRL-8234

GRL-8234 is a small-molecule BACE1 inhibitor that reverses memory impairments and age-related cognitive decline.
T61258 HFI-419

HFI-419 is a potent inhibitor of insulin-regulated aminopeptidase (IRAP) with a K i value of 0.48 μM. It is utilized in research pertaining to cognitive and memory impairments, including Alzheimer's disease, brain trauma, and stroke [1].
T70075 KDS2010 mesylate

KDS2010 is a potent, highly selective, and reversible MAO-B inhibitor which shows 12,500-fold selectivity over MAO-A. KDS2010 overcomes the disadvantages of the irreversible MAO-B inhibitor and significantly attenuates increased astrocytic GABA levels and astrogliosis, thereby enhancing synaptic transmission, and rescuing learning and memory impairments in APP/PS1 mice.
T61669 BChE-IN-4

BChE-IN-4 is a highly potent inhibitor of the enzyme butyrylcholinesterase, capable of crossing the blood-brain barrier. It effectively reduces learning and memory impairments resulting from a deficiency in cholinergic activity in a mouse model. BChE-IN-4 holds promise for further investigation in the field of Alzheimer's disease research [1].
T61342 BChE-IN-13

BChE-IN-13 (Compound 17c) is an orally active, potent, and selective inhibitor of Butyrylcholinesterase (BChE). It exhibits IC50 values of 0.22 μM and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 demonstrates the capability to enhance memory and cognitive impairments, making it valuable for Alzheimer's disease (AD) research [1].
T39421 DSR-141562

DSR-141562 is a new compound that can be taken orally and has a specific ability to inhibit phosphodiesterase 1 (PDE1) in the brain. This compound exhibits a preference for inhibiting human PDE1B, with an IC50 value of 43.9 nM. It also shows moderate inhibition of human PDE1A (IC50 = 97.6 nM) and PDE1C (IC50 = 431.8 nM). DSR-141562 is particularly useful in the study of positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia.
T78817 AChE-IN-39

AChE-IN-39(化合物7c)为一种高效AChE抑制剂,其IC50值为0.058 μM。该化合物展现出明显的DPPH清除活性,且能显著改善AlCl3诱导的遗忘症动物模型中的认知功能障碍,适用于阿尔茨海默病相关研究。
T78171 QR-0217

QR-0217是一种有效的Aβ1-40聚集抑制剂,具有7.5 µM的IC50值,阻断α-突触核蛋白的聚集,并可减轻Aβ神经毒性导致的记忆障碍。
T79684 5-HT6R antagonist 1

5-HT Receptor GPCR/G Protein; Neuroscience
5-HT6R antagonist 1(Compound 8)是一款具有突出代谢稳定性的5-HT6R拮抗剂(Ki: 5 nM),能有效抑制血小板聚集,并可逆转由MK-801引起的大鼠记忆障碍。此化合物在阿尔茨海默病(AD)的研究中有潜在应用价值。
T33766 OAB-14

OAB 14,OAB14

OAB-14 是一种 Bexarotene 衍生物,通过清除 APP/PS1 转基因小鼠的 β-淀粉样蛋白,改善其阿尔茨海默病相关的病理学和认知障碍。OAB-14 可有效改善 APP/PS1 转基因小鼠内体自噬溶酶体(EAL)途径的功能障碍。
T36720 Deacetylforskolin

Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor...
T37516 [(3R)-3-Hydroxydodecanoyl]-L-carnitine

[(3R)-3-Hydroxydodecanoyl]-L-carnitine is an endogenous metabolite[1]. [1]. Hunter WG, et al. Metabolomic Profiling Identifies Novel Circulating Biomarkers of Mitochondrial Dysfunction Differentially Elevated in Heart Failure With Preserved Versus Reduced Ejection Fraction: Evidence for Shared Metabolic Impairments in Clinical Heart Failure. J Am Heart Assoc. 2016;5(8):e003190. Published 2016 Jul 29.
T78842 α-Synuclein inhibitor 9

α-Synuclein inhibitor9 (Compound 20C) 是一种针对 α-Synuclein 的抑制剂,通过与成熟 α-Synuclein 原纤维内的空腔结合,减少了 β-折叠构型,并有效阻止 A53T α-Syn 的聚集。由于其神经保护性质,该化合物能够改善大脑功能性连接并缓解运动障碍,适用于帕金森病 (PD) 的相关研究。
T75137 BAY-747

BAY-747 (BAY 1165747) 为一种通过口服生效且具有脑渗透性的sGC刺激剂。它能可逆地逆转L-NAME所诱导的记忆障碍并在大鼠中增强认知功能。BAY-747还可在有意识状态下降低正常血压及自发性高血压大鼠(SHR)的血压。此外,BAY-747在mdx/mTRG2小鼠模型中改善了与Duchenne肌营养不良症(DMD)相关的骨骼肌功能。
T37370 Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)

Amyloid-β (25-35) (Aβ (25-35)) is an 11-residue fragment of the Aβ protein that retains the physical and biological characteristics of the full length peptide. It forms fibrils that react to thioflavin T and Congo red and are organized in a cross-β arrangement of β-strands similar to Aβ (1-40) and Aβ (1-42) fibrils. Aggregated Aβ (25-35) decreases the viability of rat adrenal PC12 cells. It also decreases the viability of primary rat cortical neurons at concentrations ranging from 1 nM to 30 μM....
T35560 SAR502250

SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2]. SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2]. SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mic...

化合物

7BIO
Cat.No: T22012
Synonym:
Target: FLT, DYRK, Aurora Kinase
Escitalopram Oxalate
Cat.No: T6493
Synonym: 草酸右旋西酞普兰,依他普仑草酸盐,Cipralex,(S)-(+)Citalopram oxalate
Target: Others, 5-HT Receptor, Serotonin Transporter
GALANTHAMINONE
Cat.No: T7114
Synonym: (-)-Narwedine,氢溴酸加兰他敏,Narwedin
Target: AChE
PH-002
Cat.No: T16518
Synonym:
Target: Others
Oxiracetam
Cat.No: T1128
Synonym: 奥拉西坦,ISF2522
Target: GABA Receptor
Bay 60-7550
Cat.No: T14507
Synonym: BAY 607550
Target: PDE
Basmisanil
Cat.No: T7165
Synonym: RG1662,RO5186582,巴米沙尼
Target: GABA Receptor
Brilaroxazine
Cat.No: T14782
Synonym: RP5063
Target: Dopamine Receptor, 5-HT Receptor
AQW051
Cat.No: T26646
Synonym: AQ W051,VQW-765,AQW-051
Target: AChR
AF267
Cat.No: T25005
Synonym: (±)AF 267,(±) AF 267,(±)-AF 267,AF 267,AF-267
Target:
GRL-8234
Cat.No: T68377
Synonym:
Target:
HFI-419
Cat.No: T61258
Synonym:
Target:
KDS2010 mesylate
Cat.No: T70075
Synonym:
Target:
BChE-IN-4
Cat.No: T61669
Synonym:
Target:
BChE-IN-13
Cat.No: T61342
Synonym:
Target:
DSR-141562
Cat.No: T39421
Synonym:
Target:
AChE-IN-39
Cat.No: T78817
Synonym:
Target:
QR-0217
Cat.No: T78171
Synonym:
Target:
5-HT6R antagonist 1
Cat.No: T79684
Synonym:
Target: 5-HT Receptor
OAB-14
Cat.No: T33766
Synonym: OAB 14,OAB14
Target:
Deacetylforskolin
Cat.No: T36720
Synonym:
Target:
[(3R)-3-Hydroxydodecanoyl]-L-carnitine
Cat.No: T37516
Synonym:
Target:
α-Synuclein inhibitor 9
Cat.No: T78842
Synonym:
Target:
BAY-747
Cat.No: T75137
Synonym:
Target:
Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)
Cat.No: T37370
Synonym:
Target:
SAR502250
Cat.No: T35560
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T0185 Escitalopram

Seroplex,依他普仑,S-(+)-Citalopram,艾司西酞普兰,(S)-Citalopram

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Escitalopram (Seroplex) 是一种外消旋 Citalopram 的 S-对映体,是一种选择性 5-羟色胺再摄取抑制剂,Ki=0.89 nM,比 R(-)-enantiomer 结合亲和力高 30 倍。它对多巴胺转运体和去甲肾上腺素转运体均有选择性,是一种研究抑郁症的抗抑郁药。
T82725 Chrysanthellin A

Chrysanthellin A, 主要皂苷化合物,源自Chrysanthellum americanum提取物,适用于研究消化功能障碍。

天然产物

Escitalopram
Cat.No: T0185
Synonym: Seroplex,依他普仑,S-(+)-Citalopram,艾司西酞普兰,(S)-Citalopram
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor
Chrysanthellin A
Cat.No: T82725
Synonym:
Target:
TargetMol Loading
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