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14
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Cat. No. | Product Name | ||
---|---|---|---|
L9840 | 抗阿尔茨海默症化合物库 | 986 compounds | |
986 种阿尔茨海默症相关的化合物集合,可用于高通量和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7100 |
PLX5622
PLX-5622 |
c-Fms; CSF-1R | Tyrosine Kinase/Adaptors |
PLX5622 是一种选择性的、高效的、能透过血脑屏障的、口服具有活性的 CSF1R 抑制剂 (IC50= 0.016 µM;Ki= 5.9 nM),具有较好的药理学特性,可用于病程发展前和过程中,扩大的和特异性的小胶质细胞的消除。 | |||
T15199 |
Edicotinib
JNJ-527,JNJ-40346527 |
c-Fms; FLT; CSF-1R; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Edicotinib (JNJ-527) 是能够透过血脑屏障的、口服具有活性的、选择性的CSF-1R 抑制剂 (IC50:3.2 nM)。它对 KIT (IC50:20 nM) 和 FLT3 (IC50:190 nM) 的抑制作用较小。它抑制小胶质细胞的扩张,减弱小胶质细胞的增殖和神经退行性变。它可用于研究阿尔茨海默病和类风湿性关节炎。 | |||
T8811 |
Tuftsin 3TFA
|
Endogenous Metabolite | Metabolism |
Tuftsin 3TFA 是一种四肽。它是一种巨噬细胞/小胶质细胞激活剂。 | |||
T14384 |
AZD8797
KAN-0440567,KAND567 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂,对 CX3CR1 和 CXCR2 具有抑制作用,对SARS-CoV-2诱导的神经元损伤有潜在的保护作用,可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。 | |||
T60932 |
MAO-B-IN-8
|
MAO | Metabolism; Neuroscience |
MAO-B-IN-8是一种高效且可逆的单胺氧化酶-B(MAO-B)抑制剂,同时也能抑制微胶质细胞产生的神经炎症介质。该化合物专为神经退行性疾病相关研究而设计[1]。 | |||
TP1786L |
Amyloid β-Protein 10-20 acetate
Amyloid β-Protein 10-20 acetate(152286-31-2 free base) |
Beta Amyloid | Neuroscience |
Amyloid β-Protein 10-20 acetate (Amyloid β-Protein 10-20 acetate (152286-31-2 free base)) 是 Amyloid-β 肽的片段,可能用于神经系统疾病的研究。Amyloid β 蛋白片段含有 α-分泌酶加工位点(Lys16-Leu17 键)。它还包含负责与小胶质细胞结合的 HHQK 结构域(残基 13-16)。 | |||
T10809 |
CHPG
|
Others | Others |
CHPG is a selective agonist of mGluR5. In BV2 microglial cells, it attenuates SO2-induced oxidative stress and inflammation through the TSG-6/NF-κB pathway. | |||
T70367 |
SNU-BP
|
Others | Others |
SNU-BP is an agonist of PPAR-gamma, inhibiting lipopolysaccharide (LPS)-induced NO production and pro-inflammatory cytokines. SNU-BP potentiates interleukin-4-induced arginase-1 expression, and promotes microglial polarization toward an M2 anti-inflammatory phenotype. | |||
T37815 |
PM226
PM 226 |
Others | Others |
Potent and selective CB2 receptor agonist (Ki = 12.8 nM; EC50 = 38.67 nM). Exhibits negligible affinity for the CB1 receptor (Ki > 40,000 nM) and no activity at the GPR55. Suppresses neuroinflammation by reducing microglial activation in a multiple sclerosis mouse model. BBB permeable; anti-inflammatory and neuroprotective. | |||
T79371 |
HDAC-IN-62
|
Autophagy | Autophagy |
HDAC-IN-62(Compound 5),是一款针对HDAC6/8/11的HDAC抑制剂,IC50分别为0.78、1.0、1.2μM。该化合物通过诱导自噬(Autophagy)来抑制微胶质细胞的激活,进而抑制一氧化氮产生,显示出抗炎和抗抑郁的效果。此外,HDAC-IN-62还能抑制实验小鼠大脑中的微胶质细胞活化。 | |||
TP1846 |
Tuftsin diacetate
|
||
Tuftsin diacetate, a tetrapeptide, is a macrophage/microglial activator. Tuftsin is a tetrapeptide, Thr-Lys-Pro-Arg, which resides in the Fc-domain of the heavy chain of immunoglobulin G. Tuftsin possesses a broad spectrum of activities related primarily | |||
T80682 |
γ-Fibrinogen 377-395 TFA
|
||
γ-Fibrinogen377-395 TFA 是纤维蛋白原衍生抑制肽,具有纤维蛋白原表位特性。该化合物能在体外抑制小胶质细胞激活、阻断纤维蛋白与Mac-1相互作用,并在小鼠体内抑制实验性自身免疫性脑脊髓炎(EAE)。该肽适用于多发性硬化症(MS)及其他血脑屏障损伤和小胶质细胞激活相关的神经炎症疾病研究。 | |||
T80683 |
γ-Fibrinogen 377-395
|
||
γ-Fibrinogen377-395是一种衍自纤维蛋白原的抑制性肽段,也被认为是纤维蛋白原的表位之一。它能在体外抑制小胶质细胞的激活并阻断纤维蛋白与Mac-1的交互作用;此外,在小鼠体内能够抑制实验性自身免疫性脑脊髓炎(EAE)的发展。因此,γ-Fibrinogen377-395对于多发性硬化症(MS)以及其他与血脑屏障损伤和小胶质细胞活化相关的神经炎症性疾病的研究具有潜在的应用价值。 | |||
T81685 |
NEP(1-40) TFA
|
||
NEP(1-40) TFA 是一种Nogo-66 受体 (NgR) 的肽类拮抗剂,其作用机制为通过抑制髓蛋白所引发的损伤逆转,限制小胶质细胞形态分布的变化。 | |||
T37726 |
MMP-9 Inhibitor I
|
Others | Others |
MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM. | |||
T62612 |
CD33 splicing modulator 1
|
Others | Others |
CD33 splicing modulator 1 (Compound 1) 是一种 CD33 splicing modulator。CD33/Siglec 3 是一种已知可调节小胶质细胞活性的髓系细胞表面受体。CD33 splicing modulator 1 加强了细胞 mRNA 池中外显子 2 的跳跃。CD33 splicing modulator 1 具有潜力进行包括阿尔茨海默病在内的神经退行性疾病的研究。 | |||
T12505 |
PLX5622 hemifumarate
|
c-Fms | Tyrosine Kinase/Adaptors |
PLX5622 hemifumarate 是高度选择性的、能透过血脑屏障的、具有口服活性的 CSF1R 抑制剂,IC50值为 0.016 μM,Ki 值为 5.9 nM,可用于病程发展前和过程中,扩大和特异性的小胶质细胞的消除。PLX5622 hemifumarate 具有较理想的药代动力学特性。 | |||
T35864 |
T-5342126
|
Others | Others |
T-5342126 is a toll-like receptor 4 (TLR4) antagonist.1It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50= 27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-depen... | |||
TP1786 |
β-Amyloid (10-20)
Amyloid β-Protein 10-20 |
||
Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.Amyloid β protein fragment containing the α-secretase processing site (Lys16-Leu17 bond). It also contains the HHQK domain (residues 13-16) re | |||
T79484 |
Nrf2 activator-8
|
Others | Others |
Nrf2 activator-8(化合物 10e)作为一种效能显著的Nrf2激活剂(EC50=37.9 nM),在BV-2微神经胶质细胞中展现出优异的抗氧化及抗炎效应。此外,Nrf2 activator-8可有效逆转脂多糖(LPS)诱导的小鼠神经炎症模型中的空间记忆缺失。 | |||
T83798 |
8-bromo NAD+ sodium
8-bromo Nicotinamide adenine dinucleotide,N(8-bromo-A)D+ |
Others | Others |
8-bromo NAD+ 作为循环ADP-核糖(cADPR)抑制剂8-bromo cADPR的前药形式,通过CD38转化为8-bromo-cADPR。在1 mM浓度下,8-bromo NAD+ 阻止由N-formyl-Met-Leu-Phe (fMLP) 在分离的小鼠骨髓衍生的中性粒细胞内引起的细胞内钙水平增加和趋化作用。同时,在100 µM浓度下使用,减少了小鼠原代小胶质细胞中LPS诱导的亚硝酸盐产生以及TNF-α和IL-2的分泌。 | |||
T75339 |
Methylene blue hydrate
|
Others | Others |
亚甲蓝(Basic Blue 9)水合物,作为鸟苷酸环化酶(sGC)、单胺氧化酶A(MAO-A)及NO合酶(NOS)的抑制剂,常用于医疗作为血管加压剂及染料。该化合物通过影响一氧化氮合成酶/鸟苷酸环化酶信号通路,能够减少脉冲前抑制,同时作为一种氧化还原循环化合物,具有穿透血脑屏障的能力,并作为Tau蛋白聚集的抑制剂,有助于缓解脑水肿、减轻小胶质细胞活化和神经炎症。 | |||
T83777 |
LAU-0901
|
||
LAU-0901是一种血小板活化因子(PAF)受体拮抗剂。在体内,LAU-0901(30、60及90 mg/kg)通过减少梗塞体积和改善大鼠由中脑动脉阻塞(MCAO)引起的脑缺血模型中的神经功能来发挥作用。它还能减少同一模型中的小胶质细胞浸润,并增加星形胶质细胞和神经元的存活率。单独使用LAU-0901(30 mg/kg)或与阿托伐他汀联合使用,能减少U87MG胶质母细胞瘤小鼠原位肿瘤模型中的肿瘤生长。 | |||
T83895 |
NCI 126224
NSC 126224 |
||
NCI 126224 是一种 toll-like receptor 4 (TLR4) 的拮抗剂。它在 RAW 264.7 巨噬细胞中,选择性抑制由 TLR4 激动剂 LPS 引起的一氧化氮 (NO) 产生(IC50 = 0.31 µM),而对 TLR7/8 激动剂 R-848、TLR1/2 激动剂 Pam3CSK4 以及 TLR3 激动剂 poly(I:C) 的影响较小;但对于相同细胞中由 TLR2/6 激动剂 FSL-1 引起的 NO 产生,其抑制作用在 0.6 µM 时亦显现。此外,NCI 126224 在 BV-2 微胶质细胞的报告实验中抑制了 LPS 引起的 NF-κB 活性,并在 RAW 264.7 巨噬细胞中降低了 LPS 引起的 IL-1β 和 TNF-α 水平(IC50s = 5.92, 0.42, 和 1.54 µM,分别)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN6714 |
Geranylgeraniol
FT-0626663,Tetraprenol,CJ24095,CJ 24095,FT0626663,香叶基香叶醇,CJ-24095 |
Apoptosis | Apoptosis |
Geranylgeraniol (FT0626663) 是一种类异戊二烯,存在于水果、蔬菜和谷物中,包括大米。 Geranylgeraniol (FT0626663) 抑制生长并诱导各种肿瘤细胞的凋亡。 Geranylgeraniol (FT0626663) 保护单核细胞免受他汀类药物诱导的细胞毒性并抑制分枝杆菌的生长。 | |||
T3896 |
Shanzhiside methyl ester
三栀子甙甲酯,山芝皂苷甲酯 |
Glucagon Receptor | GPCR/G Protein |
Shanzhiside methyl ester 是一种小分子胰高血糖素样肽 1 受体激动剂,分离自轮状乳杆菌,能够诱导抗异常性痛觉耐受。 | |||
TWS1977 |
Kamebakaurin
尾叶香茶菜丙素,Kamebakaurine |
NF-κB | NF-κB |
Kamebakaurin (Kamebakaurine) 是一种提取自Isodon japonicus 中的天然产物,是一种NF-κB 的抑制剂,能够抑制 p50 的 DNA 结合活性。 | |||
T4S1962 |
beta-Asarone
β-细辛脑,(Z)-1,2,4-三甲氧基-5-丙烯基苯;顺式细辛脑,Cis-Isoasarone,Cis-Asarone,Cis-Isoelemicin |
NF-κB; JNK | MAPK; NF-κB |
beta-Asarone (Cis-Isoelemicin) 是一种石菖蒲中的主要成分,具有免疫抑制、促进安定、中枢神经系统抑制、降温等功能。它可透过血脑屏障,能够预防帕金森病。 | |||
T3824 |
Jaceosidin
|
Apoptosis; BCL; COX; UGT | Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience |
Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物,可激活Bax,下调 Mcl-1 和 c-FLIP 的表达,诱导癌细胞凋亡。它能够降低炎性因子水平,激活 NF-κB,抑制COX-2的表达,具有抗癌和抗炎作用。 | |||
T82211 |
Herpotrichone B
|
||
Herpotrichone B exhibits potent anti-neuroinflammatory activity in BV-2 microglial cells induced by lipopolysaccharide (LPS), with a half-maximal inhibitory concentration (IC50) of 0.11μM. | |||
TN4182 |
Hannokinol
|
Others | Others |
(+)-Hannokinol and MESO-hannokinol can significantly inhibit lipopolysaccharide-induced nitric oxide production in BV2 microglial cells at concentrations ranging from 1 microM to 100 microM. | |||
T83056 |
Anti-inflammatory agent 5
|
||
5 是一种抗炎剂,对由 LPS 诱导的 BV-2 小胶质细胞中 NO 的生成显示出显著的抑制活性。 | |||
T82212 |
Herpotrichone A
|
||
Herpotrichone A在LPS诱导的BV-2小胶质细胞中表现出显著的抗炎活性,IC50值为0.41μM。 | |||
T83553 |
(4S)-10-Nor-calamenen-10-one
|
||
(4S)-10-Nor-calamenen-10-one(Compound 15)促进小胶质细胞通过LPS刺激产生的NO增强。该化合物为桉树倍半萜烯类,可从Alpinia oxyphylla中提取。 | |||
TN5248 |
Voleneol
|
NOS; COX; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
1β,6α-Dihydroxyeudesm-4(15)-ene (Voleneol,DE) can attenuate the lipopolysaccharide (LPS)-induced inflammation in BV2 microglial cells, it also can dose-dependently suppress the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenas | |||
TN2641 | 15-Methoxypinusolidic acid | ERK; IL Receptor; p38 MAPK; Calcium Channel; NOS; NF-κB; COX; JNK; NMDAR; PPAR | DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB |
15-Methoxypinusolidic acid has anti-inflammatory effects, it inhibits LPS-induced iNOS expression and NO production, independent on MAPK and NF-kappaB. 15-Methoxypinusolidic acid suppresses adipocyte differentiation through the inhibition of PPARgamma-dep | |||
T36417 |
Nargenicin
Antibiotic 47444 |
Others | Others |
Nargenicin is a macrolide antibiotic that selectively inhibits the growth of S. aureus, methicilin resistant S. aureus (MRSA), and M. luteus (MICs = 0.6, 0.3, and 2.5 μg/ml, respectively) over a panel of 11 Gram-positive and Gram-negative bacteria (MICs = >80 μg/ml). [1] It dose-dependently inhibits S. aureus DnaE in the presence of DNase I-activated DNA and E. coli DnaE when used at concentrations of 0.00001-0.1 and 0.01-100 μg/mL, respectively. [2] In murine BV-2 microglial cells, nargenicin (... | |||
TN5011 |
Shizukaol B
|
ERK; IL Receptor; p38 MAPK; TNF; NOS; NF-κB; COX; HIV Protease; DNA/RNA Synthesis; Prostaglandin Receptor; JNK | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; Microbiology/Virology; Neuroscience; NF-κB; Proteases/Proteasome |
Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimul |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPK-00735 |
CXCL13/BCA-1 Protein, Mouse, Recombinant (His)
ANGIE,BLR1L,ANGIE2,BLC,SCYB13,BCA1,BCA-1 |
Mouse | HEK293 Cells |
Recent studies have implicated chemokines in microglial activation and pathogenesis of neuropathic pain. C-X-C motif chemokine 13 (CXCL13) is a B lymphocyte chemoattractant that activates CXCR5. Using the spinal nerve ligation (SNL) model of neuropathic pain, CXCL13 was persistently upregulated in spinal cord neurons after SNL, resulting in spinal astrocyte activation via CXCR5 in mice. CXCL13/BCA-1 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with N-His tag. The pred... | |||
TMPK-00734 |
CXCL13/BCA-1 Protein, Mouse, Recombinant (hFc)
ANGIE,ANGIE2,BCA-1,BLR1L,BLC,BCA1,SCYB13 |
Mouse | HEK293 Cells |
Recent studies have implicated chemokines in microglial activation and pathogenesis of neuropathic pain. C-X-C motif chemokine 13 (CXCL13) is a B lymphocyte chemoattractant that activates CXCR5. Using the spinal nerve ligation (SNL) model of neuropathic pain, CXCL13 was persistently upregulated in spinal cord neurons after SNL, resulting in spinal astrocyte activation via CXCR5 in mice. CXCL13/BCA-1 Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with N-hFc tag. The pred... | |||
TMPK-00018 |
CXCL13/BCA-1 Protein, Human, Recombinant (His & Sumo)
BLC,SCYB13,ANGIE,ANGIE2,BCA-1,BLR1L,BCA1 |
Human | E. coli |
Recent studies have implicated chemokines in microglial activation and pathogenesis of neuropathic pain. C-X-C motif chemokine 13 (CXCL13) is a B lymphocyte chemoattractant that activates CXCR5. Using the spinal nerve ligation (SNL) model of neuropathic pain, CXCL13 was persistently upregulated in spinal cord neurons after SNL, resulting in spinal astrocyte activation via CXCR5 in mice. CXCL13/BCA-1 Protein, Human, Recombinant (His & Sumo) is expressed in E. coli expression system with N-His-Sum... | |||
TMPK-00017 |
CXCL13/BCA-1 Protein, Human, Recombinant (hFc)
BCA1,BLR1L,BLC,SCYB13,ANGIE2,BCA-1,ANGIE |
Human | HEK293 Cells |
Recent studies have implicated chemokines in microglial activation and pathogenesis of neuropathic pain. C-X-C motif chemokine 13 (CXCL13) is a B lymphocyte chemoattractant that activates CXCR5. Using the spinal nerve ligation (SNL) model of neuropathic pain, CXCL13 was persistently upregulated in spinal cord neurons after SNL, resulting in spinal astrocyte activation via CXCR5 in mice. CXCL13/BCA-1 Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with N-hFc tag. The pred... | |||
TMPK-00188 |
JAM-A Protein, Mouse, Recombinant (His)
F11R,JCAM1,PAM-1,PAM-1KAT,JAM-1,JAM,JCAM,JAM-A,KAT,F11 recep... |
Mouse | HEK293 Cells |
junctional adhesion molecule A (JAM-A), a cell adhesion molecule, is highly elevated in human GBM cancer stem cells and predicts poor patient prognosis. While JAM-A is also highly expressed in other cells in the tumor microenvironment, specifically microglia and macrophages,JAM-A functions to suppress pathogenic microglial activation in the female tumor microenvironment, highlighting an emerging role for sex differences in the GBM microenvironment and suggesting that sex differences extend beyon... | |||
TMPH-02803 |
NRROS Protein, Mouse, Recombinant (His)
Negative regulator of reactive oxygen species,Transforming g... |
Mouse | E. coli |
Key regulator of transforming growth factor beta-1 (TGFB1) specifically required for microglia function in the nervous system. Required for activation of latent TGF-beta-1 in macrophages and microglia: associates specifically via disulfide bonds with the Latency-associated peptide (LAP), which is the regulatory chain of TGFB1, and regulates integrin-dependent activation of TGF-beta-1. TGF-beta-1 activation mediated by LRRC33/NRROS is highly localized: there is little spreading of TGF-beta-1 acti... |