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30

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T60080 TMPH

2,2,6,6-Tetramethylpiperidin-4-yl heptanoate

AChR Neuroscience
TMPH 是一种 nAChR 抑制剂,可抑制缺乏 α5、α6 或 β3 亚基的 nAChR。 TMPH 可用于关于 nAChR 功能障碍或神经系统疾病的研究。
T12492 Pivagabine

CXB-722,匹伐加宾

GABA Receptor Membrane transporter/Ion channel; Neuroscience
Pivagabine (CXB-722) 是疏水性 4-氨基丁酸的衍生物,具有神经调节活性。它可穿透大鼠的血脑屏障,拮抗足部休克对大鼠脑中 GABAA 受体功能和促肾上腺皮质激素释放因子 (CRF) 浓度的影响。
T50047 1-(3,4-dihydroxyphenyl)-2-(dimethylamino)ethan-1-one hydrochloride

Others Others
1-(3,4-dihydroxyphenyl)-2-(dimethylamino)ethan-1-one hydrochloride 是一种胆碱能制剂,抑制胆碱代谢,从而导致大脑中乙酰胆碱水平的增加,进而增强认知功能和记忆。
T9232 Mitochondrial fusion promoter M1

Mitochondrial Metabolism Metabolism
Mitochondrial fusion promoter M1 是一种线粒体动态调节剂,能够保持线粒体功能并促进细胞呼吸,减轻心肌缺血/再灌注大鼠的心脏损伤和大脑损伤。
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。
T6961 PX-478

PX-478 2HCl

HIF/HIF Prolyl-Hydroxylase; HIF; Autophagy Angiogenesis; Autophagy; Chromatin/Epigenetic; Metabolism
PX-478 是一种 HIF-1α 抑制剂,具有选择性、口服活性和血脑屏障渗透性。PX-478 具有抗肿瘤活性,还可以保护糖尿病中的胰腺 β 细胞功能,用于 2 型糖尿病的研究。
T50064 2-(4-methoxyphenyl)-2-oxoethyl 2-hydroxy-5-methylbenzoate

KLF MAPK
2-(4-methoxyphenyl)-2-oxoethyl 2-hydroxy-5-methylbenzoate 是一种用于增强认知功能的促神经药物,通过增加大脑中乙酰胆碱的合成和释放以及通过抑制乙酰胆碱酯酶对乙酰胆碱的分解而发挥作用。
T0869 Atomoxetine hydrochloride

Tomoxetine hydrochloride,(R)-Tomoxetine hydrochloride,盐酸托莫西汀,LY 139603,Atomoxetine HCl,LY 139603 HCl

Dopamine Receptor; 5-HT Receptor; Norepinephrine GPCR/G Protein; Neuroscience
Atomoxetine hydrochloride (LY 139603) 是苯氧基-3-丙胺衍生物和选择性非兴奋剂,是去甲肾上腺素再摄取抑制剂,具有认知增强活性。 与人 NET,SERT 和 DAT 的放射性配体结合的 Ki 分别为5,77和1451 nM。
T38063 N-Acetyl lysyltyrosylcysteine amide

Glutathione Peroxidase Metabolism
N-Acetyl lysyltyrosylcysteine amide 是一种无毒的髓过氧化物酶 (MPO) 三肽抑制剂,具有有效性,可逆性和特异性。N-Acetyl lysyltyrosylcysteine amide 在体内可有效抑制 MPO 产生。N-Acetyl lysyltyrosylcysteine amide 减轻中风后大脑的神经元损伤,并保留脑组织和神经功能。N-Acetyl lysyltyrosylcysteine amide 抑制MPO依赖性次氯酸 (HOCl) 的生成,蛋白质硝化和 LDL 氧化。N-Acetyl lysyltyrosylcysteine amide 可用于研究支气管发育不良。
T12946 SNT-207858

Others Others
SNT-207858 is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
T12945 SNT-207858 free base

Others Others
SNT-207858 free base is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor(IC50 of 22 nM (binding) and 11 nM (function), on the MC-4 receptor).
T74045 H-Lys-Tyr-OH TFA

H-Lys-Tyr-OH TFA (Lysyltyrosine TFA)为L-赖氨酸与L-酪氨酸构成的二肽。该化合物通过促进去甲肾上腺素与酪氨酸在大脑中的释放,用于预防神经系统疾病或提升大脑功能。
T68257 Hydromethylthionine HBr

Hydromethylthionine, also known as LMTM and Leucomethylene Blue, is a apotent tau aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. Hydromethylthionine showed pharmacological activity on brain structure and function as both monotherapy and as an add-on to symptomatic treatment in certain patients with Alzheimer’s disease.
T77995 NNZ 2591

NNZ 2591为环状甘氨酸脯氨酸(cGP)小肽的合成类似物,具有口服活性,能穿过血脑屏障。在缺血性脑损伤模型中展现出神经保护作用,并改善帕金森病大鼠模型的运动功能,有望用于研究缺血性脑损伤和天使综合征。
T60344 L-Cytidine

L-Cytidine 是Cytidine 的 L-构型形式。L-Cytidine 是一种嘧啶核苷,是RNA 的组成部分。Cytidine 可控制神经胶质谷氨酸循环,影响脑磷脂代谢,儿茶酚胺的合成和线粒体功能。
T62640 FPR2 agonist 2

FPR2 agonist 2 是一种具有血脑屏障通透性的、有效的 FPR2 激动剂 (EC50: 0.13 nM)。FPR2 agonist 2 对促炎细胞因子的产生和 caspase-3 的活性具有抑制作用,抵消线粒体功能的变化。
T79172 PF-06655075

Oxytocin Receptor Endocrinology/Hormones; GPCR/G Protein
PF-06655075为一新型非脑渗透性OT受体(oxytocin receptor)激动剂,具有显著提高对OT受体(oxytocin receptor)的选择性和药代动力学稳定性。PF-06655075可用作工具化合物,以研究外周OT在行为反应中的功能。
T71174 PBT434 HBr

PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is g...
T37629 IDFP

The endocannabinoids, 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA), are biologically active lipids that regulate diverse neurological and metabolic functions by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) hydrolyze 2-AG and AEA, respectively, thus terminating their biological function. IDFP is an organophosphorus compound that dually inhibits MAGL and F...
T81571 PACAP (1-38) free acid TFA

PACAP (1-38) free acid TFA,一种内源性神经肽,能有效促进胃窦运动,增强体液蛋白分泌,同时抑制胃泌素释放。此外,它刺激血管活性肠肽、胃泌素释放肽和P物质的释放,并通过RACK1增强N-甲基-D-天门冬氨酸受体功能及脑源性神经营养因子表达。
T78954 hNTS1R agonist-1

Neurotensin Receptor GPCR/G Protein
hNTS1R agonist-1 (Compound 10)为能穿透血脑屏障的hNTS1R全激动剂(Ki:6.9 nM)。它能提升帕金森病(PD)模型小鼠的运动能力及记忆。作为一种Neurotensin(8-13)类似物,hNTS1R agonist-1同时具有神经保护作用。
T35892 Q134R

Q134R

Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer’s disease (AD) and aging-related disorders research[1]. Q134R (1-10 μM) suppresses NFAT signaling, without inhibiting calcineurin activity. Q134R partially inhibits NFAT activity in primary rat astrocytes, but does not prevent calcineurin-mediated dephosphorylation of a non-NFAT target, either in vivo...
T81573 Pabinafusp alfa

JR-141

Pabinafusp alfa (JR-141) 是由Iduronate 2-sulfatase和抗人转铁蛋白受体抗体结合而成的转铁蛋白受体靶向抗体。它具备穿透血脑屏障的能力,可防止粘多糖病II型(MPS II)小鼠中枢神经系统中硫酸肝素(HS)的积累。此外,Pabinafusp alfa能够促进小鼠的学习能力,并抑制中枢神经系统神经元的损伤。
T75389 Catechol O-methyltransferase

Catechol O-methyltransferase (COMT) 在镁的作用下,通过将 S-腺苷甲硫氨酸的甲基转移至多巴胺的羟基,生成3-甲氧基酪胺,从而参与调节大脑中肾上腺素、去甲肾上腺素和多巴胺的水平。存在于组织中的Catechol O-methyltransferase有两种形态:可溶性形式(S-COMT)和膜结合形式(MB-COMT)。
T81572 PACAP (1-38) free acid

PACAP (1-38) free acid 是一种具有多重生物功能的内源性神经肽,主要作用包括刺激胃窦运动、增进体液蛋白分泌、抑制胃泌素分泌,以及促进血管活性肠肽、胃泌素释放肽和P 物质的释放。此外,PACAP (1-38) free acid 通过与RACK1互作,可以增强N-甲基-D-天门冬氨酸受体的功能并促进脑源性神经营养因子的表达。
T36499 CuATSM

The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility ...
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。
T74365 Chol-CTPP

Chol-CTPP是针对血脑屏障(BBB)与胶质瘤(glioma)细胞展现双重靶向性的配体,可以与Chol-TPP合成为Lip-CTPP。Lip-CTPP作为一种潜在载体,可用于联合阿霉素(DOX)和氯胺达明(LND)发挥抗胶质瘤(anti-glioma)效果。此载体能够增强对肿瘤细胞的增殖、迁移及侵袭抑制,同时促进细胞凋亡(apoptosis)与坏死(necrosis),并干扰线粒体功能。
T78876 DNL343

DNL343是一种可穿透血脑屏障的eIF2B激活剂,能够有效地抑制异常的整合应激反应(ISR)。该化合物能降低中枢神经系统(CNS)中的ISR活性,逆转神经退行性变化和神经炎症反应。DNL343还能预防带有eIF2B功能丧失(LOF)突变的小鼠模型出现运动障碍和过早死亡现象。此外,DNL343在治疗由eIF2B LOF和慢性ISR激活导致的白质消失病(VWMD)方面显示出明显的治疗潜力。
T64214 NXPZ-2

NXPZ-2 是一种口服具有活力的 Keap1-Nrf2protein–protein interaction(PPI) 抑制剂 (Ki: 95 nM, EC50: 120 and 170 nM)。NXPZ-2 能够上调Nrf2含量,并促进其从细胞质向细胞核的易位,表现出对氧化应激的抑制作用。NXPZ-2 能够剂量依赖性地缓解 Aβ[1-42]诱导的认知紊乱,能够提高神经元数量和功能,增强阿尔茨海默病 (AD) 小鼠脑组织的病理改变情况。NXPZ-2 具有潜力进行 Keap1-Nrf2 PPI 抑制剂和 AD 相关的疾病的研究。

化合物

TMPH
Cat.No: T60080
Synonym: 2,2,6,6-Tetramethylpiperidin-4-yl heptanoate
Target: AChR
Pivagabine
Cat.No: T12492
Synonym: CXB-722,匹伐加宾
Target: GABA Receptor
1-(3,4-dihydroxyphenyl)-2-(dimethylamino)ethan-1-one hydrochloride
Cat.No: T50047
Synonym:
Target: Others
Mitochondrial fusion promoter M1
Cat.No: T9232
Synonym:
Target: Mitochondrial Metabolism
Cutamesine dihydrochloride
Cat.No: T3597
Synonym: AGY94806 dihydrochloride,库他美新二盐酸盐,SA4503 (dihydrochloride),SA4503 dihydrochloride
Target: Sigma receptor
PX-478
Cat.No: T6961
Synonym: PX-478 2HCl
Target: HIF/HIF Prolyl-Hydroxylase, HIF, Autophagy
2-(4-methoxyphenyl)-2-oxoethyl 2-hydroxy-5-methylbenzoate
Cat.No: T50064
Synonym:
Target: KLF
Atomoxetine hydrochloride
Cat.No: T0869
Synonym: Tomoxetine hydrochloride,(R)-Tomoxetine hydrochloride,盐酸托莫西汀,LY 139603,Atomoxetine HCl,LY 139603 HCl
Target: Dopamine Receptor, 5-HT Receptor, Norepinephrine
N-Acetyl lysyltyrosylcysteine amide
Cat.No: T38063
Synonym:
Target: Glutathione Peroxidase
SNT-207858
Cat.No: T12946
Synonym:
Target: Others
SNT-207858 free base
Cat.No: T12945
Synonym:
Target: Others
H-Lys-Tyr-OH TFA
Cat.No: T74045
Synonym:
Target:
Hydromethylthionine HBr
Cat.No: T68257
Synonym:
Target:
NNZ 2591
Cat.No: T77995
Synonym:
Target:
L-Cytidine
Cat.No: T60344
Synonym:
Target:
FPR2 agonist 2
Cat.No: T62640
Synonym:
Target:
PF-06655075
Cat.No: T79172
Synonym:
Target: Oxytocin Receptor
PBT434 HBr
Cat.No: T71174
Synonym:
Target:
IDFP
Cat.No: T37629
Synonym:
Target:
PACAP (1-38) free acid TFA
Cat.No: T81571
Synonym:
Target:
hNTS1R agonist-1
Cat.No: T78954
Synonym:
Target: Neurotensin Receptor
Q134R
Cat.No: T35892
Synonym: Q134R
Target:
Pabinafusp alfa
Cat.No: T81573
Synonym: JR-141
Target:
Catechol O-methyltransferase
Cat.No: T75389
Synonym:
Target:
PACAP (1-38) free acid
Cat.No: T81572
Synonym:
Target:
CuATSM
Cat.No: T36499
Synonym:
Target:
BAY-747
Cat.No: T75137
Synonym:
Target:
Chol-CTPP
Cat.No: T74365
Synonym:
Target:
DNL343
Cat.No: T78876
Synonym:
Target:
NXPZ-2
Cat.No: T64214
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T4947 3-Hydroxybutyric acid

Butanoic acid,3-羟基丁酸

Endogenous Metabolite Metabolism
3-Hydroxybutyric acid (Butanoic acid) 是一种人内源性代谢物,在 I 型糖尿病中升高。它能够调节膜脂的性质。
T3893 Forsythoside B

连翘酯苷 B,连翘脂苷B

TNF; NF-κB Apoptosis; NF-κB
Forsythoside B 是传统中药植物独一味叶子中分离的一种苯乙醇苷。它可抑制 TNF-alpha,IL-6,IκB, 调节 NF-κB。它抑制炎症反应,具有抗氧化和神经保护作用。

天然产物

3-Hydroxybutyric acid
Cat.No: T4947
Synonym: Butanoic acid,3-羟基丁酸
Target: Endogenous Metabolite
Forsythoside B
Cat.No: T3893
Synonym: 连翘酯苷 B,连翘脂苷B
Target: TNF, NF-κB
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