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Search Results for " primary neurons "

29

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8779	HBT1	GluR	Neuroscience
	HBT1 是一种 AMPA 受体增强剂，可诱导脑源性神经营养因子 (BDNF) 的产生，并且在原代神经元中几乎没有激动作用。 HBT1 以谷氨酸依赖的方式与 AMPA-R 的配体结合结构域结合。
T3106	C-DIM12	Apoptosis; Others	Apoptosis; Others
	C-DIM12是一种人工合成的Nurr1激活剂，可诱导Nurr1和DA 基因表达。
TP1559L	Ziconotide Acetate (107452-89-1 free base) 醋酸齐考诺肽,Prialt,Ziconotide Acetate	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Ziconotide Acetate (107452-89-1 free base) (Prialt) 是一种镇痛剂，已用于治疗神经性和非神经性疼痛。 Ziconotide 通过与位于伤害感受通路初级传入神经元末端部分的 N 型钙通道结合起作用，因此通过有效的镇痛作用减少突触传递。
T37089	Iclepertin
	Iclepertin (BI-425809) is a highly effective, selective, and orally bioavailable inhibitor of glycine transporter 1 (GlyT1). It exhibits no activity against GlyT2. Consequently, Iclepertin holds promise for advancing research on Alzheimer's disease and schizophrenia [1].
T16155	MSN-125	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	MSN-125 effectively inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond
T36141	Boscalid	Mitochondrial Metabolism	Metabolism
	Boscalid 是一种广谱羧酰胺类杀菌剂，通过与线粒体复合物 II/琥珀酸脱氢酶的泛醌位点结合来抑制真菌呼吸。
T71246	DD04107
	DD04107 is a novel inhibitor of α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons, selectively interacting with Synaptotagmin 1.
TP1471	Ziconotide TFA (107452-89-1 free base) Ziconotide TFA
	Ziconotide TEA acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
T37162	8-hydroxy Efavirenz
	8-hydroxy Efavirenz is a major oxidative metabolite of the non-nucleoside reverse transcriptase inhibitor efavirenz . 8-hydroxy Efavirenz is formed when efavirenz is metabolized by the cytochrome P450 (CYP) isoform CYP2B6. It induces apoptosis in rat primary hippocampal neurons and loss of dendritic spines in rat primary hippocampal neuronal cultures when used at a concentration of 0.01 μM.
T71554	ARN 14494
	ARN 14494 is a potent serine palmitoyltransferase inhibitor (SPT; IC50 = 27.3 nM). ARN 14494 inhibits synthesis of long chain ceramides and dihydroceramides in an in vitro model of Alzheimer's diease. The compound prevents the synthesis of proinflammatory cytokines and the oxidative stress-related enzymes iNOS and COX-2 in mouse primary cortical astrocytes. ARN 14494 is neuroprotective against β-amyloid 1-42 induced neurotoxicity in primary cortical neurons co-cultured with astrocytes.
T76539	Insulin-like growth factor II
	Insulin-like growth factor II (IGF-2)为人血清中主要生长激素，对神经突生长具有许可性和直接作用，同时增强交感与感觉神经元的生存能力。
T35551	Gallocyanine
	Gallocyanine is a small molecule blue dye used to stain nuclei. It is known to inhibit Dickkopf-1 (Dkk1), an antagonist of the Wnt pathway. Gallocyanine can disrupt the interaction of Dkk1 with its receptor LRP5/6 (IC50 = 3 μM), thereby activating Wnt/β-catenin signaling. Modulation of the Dkk1-LRP5/6 interaction via gallocyanine has been shown to inhibit prostaglandin J2-induced tau phosphorylation at serine396 in primary cortical neurons in vitro.
T73094	Adhesamine
	Adhesamine 是一种哑铃状的分子，能够激活 MAPK/FAK 通路。Adhesamine 能促进哺乳动物细胞的粘附和生长。Adhesamine 加速原代培养小鼠海马神经元的分化并提高存活率。
T37476	Cyclo(L-Phe-L-Val)
	Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1 that can autoinduce production of antibacterial substances active against S. aureus when co-cultured at a low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro when used at concentrations of 16 and 32 μM. It increases phosphorylation of the PI3K substrate Akt, and neurite outgrowth induced by cyclo(L-Phe-L-Val) can be blocked by the PI3K inhibitor LY294002 . Cyclo(L-...
T69806	EGIS-8332
	EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimenta...
T36516	RC574 RC574
	RC574 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It inhibits glutamate-induced cell death in HT22 cells (IC50= 276.2 nM) and mouse primary cortical neurons when used at a concentration of 3 μM. RC574 (3 μM) increases glutathione peroxidase 1 (GPX1) levels and GPX activity, as well as inhibits glutamate-induced mitochondrial superoxide anion production, in HT22 cells. It completely inhibits ferroptosis induced by the GPX4 inhibitor ...
T38389	Prostaglandin D2 Ethanolamide Prostaglandin D2 Ethanolamide
	Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of minia...
TP1513	Egg Laying Hormone, aplysia
	Egg-laying hormone (ELH) is a neuropeptide synthesized by the bag cell neurons, Egg-laying hormone (ELH) induces egg laying and its correlated behavior in Aplysia californica. Egg-laying hormone (ELH) has been purified to homogeneity and Egg-laying hormon
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....
T83739	Myr-Tat-CBD3 TFA Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3
	Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下，该化合物能够约81%地抑制Cav2.2-CRMP2相互作用，并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入（IC50约为2.8 µM）。在20 µM的浓度下，Myr-Tat-CBD3能抑制钙电流，但不影响钠电流，在初级DRG神经元中表现出这种特性。经过脊髓内给药，myr-Tat-CBD3（20 µg/5 µl）能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外，Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。
T72227	PI3K/Akt/CREB activator 1
	PI3K/Akt/CREB activator 1 是一种口服有效的PI3K/Akt/CREB 的激活剂。PI3K/Akt/CREB activator 1 通过 PI3K/Akt/CREB 通路上调脑源性神经营养因子，促进神经元增殖，诱导 Neuro-2a 细胞分化成神经元样形态，加速海马原代神经元轴突-树突极化的建立。PI3K/Akt/CREB activator 1 可用于血管性痴呆 (VaD) 的研究。
T83731	Tat-CBD3 TFA
	Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中，Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%，并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流，并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...
T37605	D-DOPA
	D-DOPA is an enantiomer of the dopamine precursor L-DOPA . It can be converted to L-DOPAviasequential oxidation and transamination, which are mediated by D-amino acid oxidase (DAAO) and DOPA transaminase, respectively, in rat kidney homogenates.1It reduces the number of dopaminergic neurons in primary rat embryonic mesencephalic cultures in a concentration-dependent manner.2Intraventricular administration of D-DOPA (200 μg/animal) increases striatal dopamine levels in rats.3D-DOPA (20 mg/kg, i.p...
T83764	Sulfane Sulfur Probe 4 SSP4
	Sulfane sulfur probe 4 (SSP4) 是用于检测含硫化氢衍生的多硫化物、过硫化物和硫化物的荧光探针。在含硫磺物种存在下，SSP4 经核苷酸攻击反应生成荧光素，其激发/发射峰值分别为494/515 nm，以及两分子的1,2-苯并二硫杂环-3-酮。SSP4 已应用于确定H2S3在原代小鼠神经元中的定位，并检测L. japonicus 幼苗根部的多硫化物。
T70538	PD-85639
	PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membr...
T83727	Tat-NTS Peptide TFA Tat-Nuclear Translocation Signal Peptide
	Tat-NTS肽是一种能穿透细胞的肽，由HIV-1 Tat蛋白的转导域与对应于脂联素A1重复III域残基228-237的10个氨基酸肽链接而成，扮演核转运信号（NTS）的角色。它通过阻断脂联素A1与进口素β之间的蛋白质-蛋白质相互作用，阻止脂联素A1在初级鼠海马神经元中的核内转运。Tat-NTS抑制初级鼠海马神经元在葡萄糖-氧剥夺及再灌注诱导的细胞凋亡。在体内，Tat-NTS（10 mg/kg）有效减少了由中脑动脉闭塞（MCAO）引起的缺血-再灌注损伤模型小鼠的梗塞体积和神经元凋亡，并缩短了在Morris水迷宫测试中达到平台的时间。
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...
T83825	Trofinetide acetate NNZ-2566
	Trofinetide是一种衍生自具有神经保护作用的三肽Gly-Pro-Glu的化合物，后者是胰岛素样生长因子-1（IGF-1）的N-端序列。在10 nM的浓度下使用时，它能减少由蛋白磷酸酶抑制剂奥卡达酸在原代大鼠胚胎纹状体神经元中引起的细胞死亡。Trofinetide在一种由穿透性弹道样脑损伤引起的大鼠神经炎症模型中减少了编码IL-1β、TNF-α、IL-6和E-selectin的mRNA的脑表达。在通过中脑动脉闭塞（MCAO）引起的大鼠脑损伤模型中，以30和60 mg/kg的剂量给药时，它减少了皮层和纹状体梗塞区域。Trofinetide（每天100 mg/kg）减少了树突棘的数量，并逆转了在fmr1-/-敲除小鼠脆性X综合征模型中的社交识别和情景恐惧条件反射的缺陷，同时也减少了睾丸重量的增加。含有Trofinetide的制剂已被用于治疗Rett综合征。

化合物

Cat.No: T8779

Target: GluR

Cat.No: T3106

Target: Apoptosis, Others

Ziconotide Acetate (107452-89-1 free base)

Cat.No: TP1559L

Synonym: 醋酸齐考诺肽,Prialt,Ziconotide Acetate

Target: Calcium Channel

Cat.No: T37089

Cat.No: T16155

Target: Akt

Cat.No: T36141

Target: Mitochondrial Metabolism

Cat.No: T71246

Ziconotide TFA (107452-89-1 free base)

Cat.No: TP1471

Synonym: Ziconotide TFA

8-hydroxy Efavirenz

Cat.No: T37162

Cat.No: T71554

Insulin-like growth factor II

Cat.No: T76539

Cat.No: T35551

Cat.No: T73094

Cyclo(L-Phe-L-Val)

Cat.No: T37476

Cat.No: T69806

Cat.No: T36516

Synonym: RC574

Prostaglandin D2 Ethanolamide

Cat.No: T38389

Synonym: Prostaglandin D2 Ethanolamide

Egg Laying Hormone, aplysia

Cat.No: TP1513

Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)

Cat.No: T37370

Myr-Tat-CBD3 TFA

Cat.No: T83739

Synonym: Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3

PI3K/Akt/CREB activator 1

Cat.No: T72227

Cat.No: T83731

Cat.No: T70063

Cat.No: T37605

Sulfane Sulfur Probe 4

Cat.No: T83764

Synonym: SSP4

Cat.No: T70538

Tat-NTS Peptide TFA

Cat.No: T83727

Synonym: Tat-Nuclear Translocation Signal Peptide

Cat.No: T36570

Trofinetide acetate

Cat.No: T83825

Synonym: NNZ-2566

Cat. No.	Product Name	Target	Signaling Pathways
T5S2129	Sciadopitysin	TNF; NF-κB	Apoptosis; NF-κB
	Sciadopitysin 是一种双黄酮类化合物，来自银杏叶片中。它通过抑制NF-κB 活化并降低c-Fos 和NFATc1的表达来抑制 RANKL 诱导的破骨细胞生成和骨丢失。
T5287	N-Acetyl-L-aspartic acid AC-ASP-OH,N-Acetylaspartic acid,N-乙酰-L-天门冬氨酸	Others; Endogenous Metabolite	Metabolism; Others
	N-Acetyl-L-aspartic acid (AC-ASP-OH) 是天冬氨酸的衍生物，是由氨基酸天冬氨酸和乙酰辅酶 A 在神经元中合成的。
TN3473	Axillarin
	Axillarin has antioxidant activity, it shows xanthine oxidase inhibitory activity ( IC(50) :36.0 uM). Axillarin can strongly protect primary cultured neurons against glutamate-induced oxidative stress.
TN4286	Isodunnianol	NOS; NF-κB; ROS; AChR	Immunology/Inflammation; Neuroscience; NF-κB
	Isodunnianol exhibits anti-AChE activity with an IC50 value of 13.0 uM; it also exhibits neurite outgrowth-promoting activity at the concentration ranging from 0.1 to 10 uM in the primary cultured rat cortical neurons. Isodunnianol, dunnianol, and Macrant

天然产物

Cat.No: T5S2129

Target: TNF, NF-κB

N-Acetyl-L-aspartic acid

Cat.No: T5287

Synonym: AC-ASP-OH,N-Acetylaspartic acid,N-乙酰-L-天门冬氨酸

Target: Others, Endogenous Metabolite

Cat.No: TN3473

Cat.No: TN4286

Target: NOS, NF-κB, ROS, AChR

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