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31

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T22118 NQTrp

Microtubule Associated Cytoskeletal Signaling
NQTrp 是芳香萘醌-色氨酸杂交分子,可以抑制 tau 蛋白的聚集,具有抗淀粉样蛋白活性。NQTrp 对六肽 (41GCWMLY46,γD-crystallin 的 N 端)和全长 γD-crystallin 的体外聚集有抑制作用。
T13048 SynuClean-D

SC-D

Others Others
SynuClean-D (SC-D) 是一种 α-突触核蛋白聚集的抑制剂,能够破坏成熟的淀粉样蛋白原纤维,抑制原纤维繁殖,防止帕金森氏病动物模型中多巴胺能神经元的变性。
T35941 DC-Chol hydrochloride

​Cholesteryl 3β-N-(dimethylaminoethyl)carbamate hydrochloride,DC-Chol (hydrochloride),DC-Cholesterol hydrochloride,​Cholesteryl 3β-N-(dimethylaminoethyl)carbamate

Beta Amyloid Neuroscience
DC-Chol hydrochloride(DC-Cholesterol hydrochloride) 在适当的实验条件下能抑制 Aβ40 纤维的形成且以剂量依赖性的方式显著抑制氧化hCT的淀粉样蛋白形成。DC-Chol hydrochloride可诱导改善和平衡的免疫力,能够促进乙型肝炎疫苗的研究。
T68836 ADS-J1

ADS-J1 is an HIV-1 entry inhibitor that potently inhibits seminal amyloid fibrillization and block fibril-mediated enhancement of viral infection. Semen-derived amyloid fibrils, comprising SEVI (semen-derived enhancer of viral infection) fibrils and SEM1 fibrils, may remarkably enhance HIV-1 sexual transmission and are potential targets for the development of an effective microbicide.
T32609 Lawsoniaside

Lawsoniaside can hinder the growth of amyloid-β42 fibrils.
T19730 12-Crown-4

12 C 4,12-Crown-4 ether,12C4,12-C-4

12-Crown-4 disrupts Aβ40 fibrils. 12-Crown-4 can enter into the hydrophobic core region and form competitive, hydrophobic interactions with key hydrophobic residues.
T19837 O4

O 4,O-4

O4 is a novel stabilizer of amyloid- fibrils. O4 used for accelerating the formation of end-stage mature fibrils.
T10530 BF 227

Others Others
BF 227 is a candidate for an amyloid imaging probe for PET (Ki: 4.3 nM for Aβ1-42 fibrils).
T19018 K114

Others Others
K114 binds tightly to amyloid fibrils (EC50: 20-30 nM). K114 is an efficient detector of semen-derived enhancer of virus infection (SEVI).
TP1645 β-Amyloid (1-9)

β-Amyloid 1-9

This is an N-terminal fragment of beta amyloid. It consists of amino acid residues 1 to 9. Truncated beta amyloid peptide (10-40) still forms amyloid fibrils and shows fibril polymorphism.
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....
T83106 Anselamimab

Anselamimab (CAEL-101) 为一种靶向血清淀粉样蛋白 A1 (SAA1) 的人源 IgG1-κ 抗淀粉样蛋白原纤维抗体。
T74158 Aβ Fibrillization modulator 1

Aβ Fibrillization Modulator 1 能够稳定Aβ单体,这有助于防止其聚集形成纤维状结构。
T35627 Amylin (human) (trifluoroacetate salt)

Amylin is a 37-residue peptide hormone secreted from pancreatic β-cells that reduces food intake, decreases glucagon secretion, slows gastric emptying, and increases satiety. It binds to amylin receptors with IC50 values of 2 and 0.2 nM for porcine and guinea pig nucleus accumbens membrane preparations, respectively. Amylin is present in amyloid aggregates derived from the pancreatic islets of humans with type 2 diabetes. Amylin forms fibrils that react to thioflavin T and are organized in a cro...
T39638 Eprodisate

Eprodisate is a novel compound specifically developed to disrupt the interactions between amyloidogenic proteins and glycosaminoglycans, effectively impeding the polymerization of amyloid fibrils and their deposition in tissues. This compound shows potential for delaying the advancement of AA amyloidosis-related renal disease and could apply to various forms of amyloidosis.
T73495 q-FTAA

q-FTAA 与 Aβ1-42 原纤维结合,对 Aβ1-42 原纤维和阿尔茨海默病 PIB 结合复合物 (ADPBC) 的 EC50值分别为 330-630,300-500 nM。q-FTAA 具有研究阿尔茨海默病 (AD) 的潜力。
T37472 TAMRA-Amyloid-β (1-42) Peptide (trifluoroacetate salt)

TAMRA-Amyloid-β (1-42) peptide is a fluorescently labeled peptide. Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-residue protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease. Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers. TAMRA-Amyloid-β (1-42) peptide is a labeled form of Aβ42 containing carboxytetramethyl rhodamine (TAMRA), which displays excitation/emission maxima of 543/572 nm, respectively.
T60335 BTA-1

BTA-1 是一种不带电的硫代黄素-T 衍生物。BTA-1 对 Aβ 原纤维具有高亲和力,并具有良好的脑进入和清除能力。
T31828 AZD4694

Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694

Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am
T80374 HBA(111–142)

HSV Microbiology/Virology
HBA(111-142) 是一种源于 α-血红蛋白 C 端的32-聚体抗菌肽片段,对 ESKAPE 病原体展示出了抗菌效果。它能形成淀粉样原纤维结构,并表现出针对多种病毒,包括麻疹病毒和疱疹病毒(HSV-1、HSV-2、HCMV)的抗病毒活性。
T61087 THK-5105

THK-5105为芳基喹啉衍生物,具备与tau原纤维高度结合的亲和力。它对tau蛋白聚集体及含tau的阿尔茨海默病(AD)脑匀浆显示出显著的结合能力。18F-THK-5105展现出作为tau成像PET探针的潜能。
T37367 Amyloid-β (1-42) Peptide (trifluoroacetate salt)

Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-amino acid protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease.1,2,3Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers.1Aβ42 accumulates in the brain of many transgenic mouse models of Alzheimer's disease and, in many models, the onset of amyloid deposition positively correlates with deficits in spatial learning and memory.4 1.Wolfe, M.S.Therapeutic strategi...
T60907 THK-5117

THK-5117 是一种芳基喹啉衍生物,具有作为 tau 成像 PET 探针的潜力。THK-5117 对 tau 原纤维表现出高结合亲和力,Ki 值为 10.5 nM。THK-5117 还显示出对 tau 蛋白聚集体和富含 tau 的阿尔茨海默病 (AD) 脑匀浆的高结合亲和力。
T75958 β-Amyloid (22-35) (TFA)

β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA是β-淀粉样蛋白22-35残基段,具细胞毒性,能影响无血清培养大鼠海马神经元。在中性缓冲液中,此化合物能形成聚集体与典型淀粉样纤维,模拟β-淀粉样蛋白行为。
T74645 Eplontersen

Eplontersen 是一种三触角的、N-乙酰半乳糖胺 (GalNAc3)-缀合的反义寡核苷酸,能够靶向 甲状腺素运载蛋白 TTR 的 mRNA,抑制变体和野生型 TTR 产生。错误折叠的 TTR 诱导心脏和周围神经的淀粉样原纤维形成,并介导淀粉样 TTR (ATTR) 蛋白变性疾病。
T73912 Maysin

Maysin 是一种具有神经保护作用的 C-糖基黄酮,可以从玉米须中分离得到。Maysin 对 Syn 淀粉样蛋白聚集体-低聚物和原纤维引起的损伤具有保护作用。Maysin 可防止氧化应激和细胞内钙稳态失衡,激活自噬降解过程。Maysin 可用于帕金森病(PD) 的研究。
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。
T80362 Human α-Defensin 6

Human α-Defensin 6,含32个半胱氨酸残基的抗菌肽,能够阻止细菌入侵,促进粘膜免疫。该肽通过自组装形成有序的原纤维和纳米网,能随机结合细菌表面蛋白,进而围绕并缠绕细菌。此外,Human α-Defensin 6抑制C. albicans生物膜的形成。
T82379 FN-A208 fusion peptide

FN-A208 是源自鼠层粘连蛋白 a1 的 A208 与纤连蛋白 (GRGDS) 活性位点和甘氨酸间隔区融合形成的生物活性肽。该肽能形成淀粉样原纤维,并有助于促进肌动蛋白应力纤维的形成,进而介导成纤维细胞附着,显示出其在组织再生和工程生物粘合剂方面的应用潜力。FN-A208 与 IKVAV 受体和整合素发生相互作用,而在 EDTA 存在下,其活性则会被破坏。
T83507 [Asn23] β-Amyloid (1-40), Iowa mutation

[Asn23] β-Amyloid (1-40), Iowa mutation 是一种与重度大脑淀粉样蛋白血管病 (CAA) 相关的生物活性肽。该突变涉及 APP 694 位点的错义突变,Asp 23 位置的天冬酰胺被天冬酰氨酸取代。这种变异的 β-Amyloid 肽倾向于更快聚集,并形成有害的原纤维。
T83726 Tat-βsyn-degron TFA

Tat-βsyn-degron是一种降低α-synuclein表达的肽。其结构包括HIV-1 Tat质膜跨导域、与β-synuclein氨基酸36-45相对应的α-synuclein结合域βsyn,以及蛋白酶体定向域degron。在肽-蛋白结合实验中,Tat-βsyn-degron能够与重组α-synuclein结合,并在大鼠初级皮质神经元培养中降低α-synuclein水平,这一效应可以通过蛋白酶体抑制剂MG132阻止。体内研究显示,Tat-βsyn-degron (40 mg/kg)能够在过表达人类A53T突变体α-synuclein的M38转基因小鼠的大脑中降低α-synuclein水平,并且在黑质和脑桥中降低磷酸化α-synuclein水平,以及在通过α-synuclein预成纤维诱导的扩散性α-synuclein病理模型小鼠中减少神经炎症。此外,Tat-βsyn-degron (6 µmol/kg, i.p.)在MPTP诱导的帕金森病小鼠模型中,保护多巴胺能神经元,缓解运动缺陷。

化合物

NQTrp
Cat.No: T22118
Synonym:
Target: Microtubule Associated
SynuClean-D
Cat.No: T13048
Synonym: SC-D
Target: Others
DC-Chol hydrochloride
Cat.No: T35941
Synonym: ​Cholesteryl 3β-N-(dimethylaminoethyl)carbamate hydrochloride,DC-Chol (hydrochloride),DC-Cholesterol hydrochloride,​Cholesteryl 3β-N-(dimethylaminoethyl)carbamate
Target: Beta Amyloid
ADS-J1
Cat.No: T68836
Synonym:
Target:
Lawsoniaside
Cat.No: T32609
Synonym:
Target:
12-Crown-4
Cat.No: T19730
Synonym: 12 C 4,12-Crown-4 ether,12C4,12-C-4
Target:
O4
Cat.No: T19837
Synonym: O 4,O-4
Target:
BF 227
Cat.No: T10530
Synonym:
Target: Others
K114
Cat.No: T19018
Synonym:
Target: Others
β-Amyloid (1-9)
Cat.No: TP1645
Synonym: β-Amyloid 1-9
Target:
Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)
Cat.No: T37370
Synonym:
Target:
Anselamimab
Cat.No: T83106
Synonym:
Target:
Aβ Fibrillization modulator 1
Cat.No: T74158
Synonym:
Target:
Amylin (human) (trifluoroacetate salt)
Cat.No: T35627
Synonym:
Target:
Eprodisate
Cat.No: T39638
Synonym:
Target:
q-FTAA
Cat.No: T73495
Synonym:
Target:
TAMRA-Amyloid-β (1-42) Peptide (trifluoroacetate salt)
Cat.No: T37472
Synonym:
Target:
BTA-1
Cat.No: T60335
Synonym:
Target:
AZD4694
Cat.No: T31828
Synonym: Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694
Target:
HBA(111–142)
Cat.No: T80374
Synonym:
Target: HSV
THK-5105
Cat.No: T61087
Synonym:
Target:
Amyloid-β (1-42) Peptide (trifluoroacetate salt)
Cat.No: T37367
Synonym:
Target:
THK-5117
Cat.No: T60907
Synonym:
Target:
β-Amyloid (22-35) (TFA)
Cat.No: T75958
Synonym:
Target:
Eplontersen
Cat.No: T74645
Synonym:
Target:
Maysin
Cat.No: T73912
Synonym:
Target:
α-Synuclein inhibitor 9
Cat.No: T78842
Synonym:
Target:
Human α-Defensin 6
Cat.No: T80362
Synonym:
Target:
FN-A208 fusion peptide
Cat.No: T82379
Synonym:
Target:
[Asn23] β-Amyloid (1-40), Iowa mutation
Cat.No: T83507
Synonym:
Target:
Tat-βsyn-degron TFA
Cat.No: T83726
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2987 (-)-Epigallocatechin

表没食子儿茶素,(-)-表没食子儿茶素,l-Epigallocatechin,Epigallocatechin,EGC

MMP; Autophagy Autophagy; Proteases/Proteasome
(-)-Epigallocatechin (Epigallocatechin) 是绿茶中含量最丰富的黄酮类天然产物,可与未折叠的天然多肽结合,阻止转化为淀粉样蛋白原纤维。
T40641 Crocin-4

Crocin-4, a carotenoid compound found in saffron, possesses potent antioxidant properties and can penetrate the brain. It effectively inhibits the aggregation and deposition of Aβ fibrils, making it useful for Alzheimer's Disease research. Additionally, Crocin-4 demonstrates antitumor and anti-inflammatory activities.

天然产物

(-)-Epigallocatechin
Cat.No: T2987
Synonym: 表没食子儿茶素,(-)-表没食子儿茶素,l-Epigallocatechin,Epigallocatechin,EGC
Target: MMP, Autophagy
Crocin-4
Cat.No: T40641
Synonym:
Target:
TargetMol Loading
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