|
T7530
|
PD146176
NSC168807
|
Ferroptosis;
Lipoxygenase;
Autophagy |
Apoptosis;
Autophagy;
Metabolism |
|
PD146176 (NSC-168807) 是一种 15-脂氧合酶(15-LO)抑制剂，抑制兔网织红细胞 15-LO，Ki 为 197 nM，IC50 为 0.54 μM。 它通过刺激老年三重转基因小鼠的自噬来逆转认知障碍、脑淀粉样变性和 tau 病理学。 |
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T60086
|
TTBK1-IN-2
N-[4-(4-chlorophenoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
|
Microtubule Associated |
Cytoskeletal Signaling |
|
TTBK1-IN-2 (N-[4-(4-chlorophenoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine) 是 Tau-Tubulin 激酶 (TTBK1) 的抑制剂，IC50 为 0.24 和 4.22 µM。 TTBK1-IN-2 降低细胞培养物和转基因 TDP-43 小鼠脊髓中的 TDP-43 磷酸化。 |
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T9253
|
CPFX4158
|
Antibacterial |
Microbiology/Virology |
|
CPFX4158 是一种甘露糖衍生物和抗菌剂，可用于转基因人源化 CEACAM6 小鼠。 |
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T11016
|
DGAT-1 inhibitor 2
|
Transferase |
Metabolism |
|
DGAT-1 inhibitor 2是有效的DGAT-1抑制剂，具有减肥功效。 |
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T77342
|
GSK-3 inhibitor 3
|
GSK-3;
Microtubule Associated |
Cytoskeletal Signaling;
PI3K/Akt/mTOR signaling;
Stem Cells |
|
GSK-3 inhibitor 3 是一种具有选择性、具有口服活性和脑渗透性的 GSK-3 抑制剂，对 GSK-3α 和 GSK-3β 具有抑制作用， IC50s 分别为 0.35 nM 和 0.25 nM。GSK-3 inhibitor 3 在三重转基因小鼠阿尔茨海默病模型中降低 Tau 蛋白 (tau protein) S396 磷酸化水平，IC50为 10 nM。GSK-3 inhibitor 3 可用于研究神经系统疾病。 |
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T9518
|
Inarigivir ammonium
ORI-9020 ammonium,SB-9200 ammonium,Inarigivir铵
|
HBV |
Microbiology/Virology |
|
Inarigivir ammonium (SB-9200 ammonium) 是一种二核苷酸抗病毒化合物，可显着降低表达乙型肝炎病毒的转基因小鼠的 HBV DNA。它是一种激活细胞内先天免疫的视黄酸诱导基因-I 激动剂。 |
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TP1541L
|
BDC2.5 mimotope 1040-31 acetate
BDC2.5 mimotope 1040-31 acetate(329696-49-3 free base)
|
Others |
Others |
|
BDC2.5 mimotope 1040-31 acetate(329696-49-3 free base) 一种用于致糖尿病 T 细胞克隆 BDC2.5 的有效激动肽 (mimotope)。它可以刺激 BDC2.5 细胞，使细胞对这种模拟表位表现出良好的反应。 1040-31 肽对 BDC2.5 TCR Tg+（转基因）T 细胞具有特异性。该肽也称为 p31。 |
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T9901A-001
|
Relatlimab
BMS-986016
|
Others |
Others |
|
Relatlimab(BMS-986016) 是一种靶向人抗 LAG-3 的单克隆抗体，由携带重组 LAG-3 蛋白的人免疫球蛋白的转基因小鼠免疫生成。Relatlimb 有阻断作用，可阻断 LAG-3/MHC II 的相互作用（IC50 ： 0.67 nM），阻断了 LAG-3/FGL1 的相互作用（ IC50：0.019 nM）。Relatlimab 常与 Nivoluma 一起用来治疗晚期黑色素瘤。 |
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T32276
|
JAY2-22-33
JAY-2-22-33,JAY 2 22 33
|
Others |
Others |
|
JAY2-22-33, as a neuroprotective agent, can act by significantly reducing Aβ toxicity by delaying paralysis and improving cognitive performances in a transgenic mouse model of AD. |
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T35689
|
MTP 131 acetate
|
Others |
Others |
|
MTP 131 acetate 是一种小的线粒体靶向四肽。 |
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T32330
|
JWB1-84-1 3HCl
JWB1 84 1 3HCl,JWB1 84 1 trihydrochloride,JWB1-84-1 trihydrochloride,JWB1841 trihydrochloride
|
Others |
Others |
|
JWB1-84-1 3HCl, as a neuroprotective agent, can act by improving cognitive performances in a transgenic mouse model of AD. |
|
T70059
|
ALT-946 HCl
|
Others |
Others |
|
ALT-946 HCl is an inhibitor of advanced glycation that has been shown to improve severe nephropathy in the diabetic transgenic (mREN-2)27 rat. |
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T68794
|
ALT-946 free base
|
Others |
Others |
|
ALT-946 free base is an inhibitor of advanced glycation that has been shown to improve severe nephropathy in the diabetic transgenic (mREN-2)27 rat. |
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T62198
|
AR524
|
Others |
Others |
|
AR524 是一种转基因抑制剂，抑制活性高于已知的转基因抑制剂 kifunensine。AR524 能够抑制低浓度 (10 μM) 的人类恶性细胞球状体的形成。 |
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T69664
|
Umibecestat HCl
|
Others |
Others |
|
Umibecestat, also known as CNP-520, is a beta-secretase inhibitor and is a drug candidate for prevention trials in Alzheimer's disease. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. CNP520 reduced brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice. CNP520 reduces Aβ load and neuroinflammation in APP‐transgenic mice |
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T14690
|
BMS 433796
BMS-289948,BMS-299897
|
Beta Amyloid |
Neuroscience |
|
BMS 433796 是一种在阿尔茨海默病转基因小鼠模型中具有Aβ降低活性的γ分泌酶抑制剂，可有效抑制 Aβ 的产生。 |
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T38279
|
C2-8
C2-8
|
Others |
Others |
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s = 25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2... |
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T69524
|
MI-09
|
Others |
Others |
|
MI-09 is a SARS-CoV-2 Protease inhibitor (IC50 = 15.2 nM). In a transgenic mouse model of SARS-CoV-2 infection, oral or intraperitoneal treatment with MI-09 significantly reduced lung viral loads and lung lesions. |
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T69540
|
MI-30
|
Others |
Others |
|
MI-30 is a SARS-CoV-2 Protease inhibitor (IC50 = 17.2 nM). In a transgenic mouse model of SARS-CoV-2 infection, oral or intraperitoneal treatment, MI-30 significantly reduced lung viral loads and lung lesions. |
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TP1954
|
PHM-27 (human)
|
|
|
|
Endogenous peptide product of human prepro-VIP and analog of porcine PHI-27; potent agonist for the human calcitonin receptor (EC50 = 11 nM). Transgenic mice expressing the human VIP/PHM 27 gene in pancreatic β-islets display enhanced glucose-induced insu |
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T70151
|
MeTC7
|
Others |
Others |
|
MeTC7 is a VDR antagonist, which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo. |
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T78807
|
YIAD-0205
|
Others |
Others |
|
YIAD-0205为口服有效的Aβ(1-42)聚集抑制剂，在5XFAD AD转基因小鼠模型中展现体内效力。 |
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T40059
|
Nicotinamide riboside tartrate
|
Others |
Others |
|
Nicotinamide riboside tartrate (NRT) is an oral NAD+ precursor that raises NAD+ levels, activates SIRT1 and SIRT3, and serves as a vitamin B3 (niacin) source. NRT also improves oxidative metabolism and protects against metabolic abnormalities induced by a high-fat diet. Furthermore, NRT mitigates cognitive decline in a transgenic mouse model of Alzheimer's disease. |
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T82908
|
BDC2.5 mimotope 1040-31 TFA
|
|
|
|
BDC2.5 mimotope 1040-31 TFA，一种针对糖尿病T细胞克隆BDC2.5的强活性激动肽，具备对BDC2.5 TCR Tg+T细胞的高度特异性。 |
|
TP1855
|
Moth Cytochrome C (MCC) (88-103)
Moth Cytochrome C (MCC) 88-103
|
|
|
|
Moth Cytochrome C (MCC) (88-103), derived from the carboxyl terminus of moth cytochrome c, induces positive selection of TCR transgenic thymocytes.This peptide is derived from the carboxyl terminus of moth cytochrome c. Thymic positive and negative select |
|
TP1541
|
BDC2.5 mimotope 1040-31
|
|
|
|
This is a effectively agonistic peptide (mimotope) for diabetogenic T cell clone BDC2.5. It can stimulate BDC2.5 cells with cells showing good response to this mimotope. 1040-31 peptide is specific for BDC2.5 TCR Tg+ (transgenic) T cells. This peptide is |
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T40132
|
Insulin β Chain Peptide (15-23)
|
|
|
|
Insulin β Chain Peptide (15-23), also referred to as INS, is an insulin-derived peptide that is specifically recognized by islet-associated T cells. The tetramer of Insulin β Chain Peptide (15-23) effectively stained the INS-reactive CTL clone G9C8; however, neither this tetramer nor the negative control tetramer (TUM) exhibited staining on the splenic CD8+ T cells obtained from NOD or 8.3-TCRαβ transgenic NOD mice. |
|
T78426
|
MCAAD-3
|
|
|
|
MCAAD-3为一种近红外Aβ成像探针，能穿透血脑屏障。其对Aβ聚合体拥有高亲和力（Ki >106 nM），能够在转基因小鼠大脑中标记Aβ斑块。 |
|
T74065
|
Nifurpirinol
|
Others |
Others |
|
Nifurpirinol (P-7138)，一种硝基芳香型抗生素(antibiotic)，作为细菌硝基还原酶(NTR)的底物。相较于甲硝唑，其作为一种prodrug，在表达硝基还原酶的转基因模型中引发细胞消融的效能更高。 |
|
T37367
|
Amyloid-β (1-42) Peptide (trifluoroacetate salt)
|
Others |
Others |
|
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... |
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T33766
|
OAB-14
OAB 14,OAB14
|
Others |
Others |
|
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。 |
|
T71174
|
PBT434 HBr
|
Others |
Others |
|
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... |
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T36234
|
5(Z),11(Z),14(Z)-Eicosatrienoic Acid
|
Others |
Others |
|
5(Z),11(Z),14(Z)-Eicosatrienoic acid is a polyunsaturated fatty acid found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. 5(Z),11(Z),14(Z)-Eicosatrienoic acid methyl ester, when topically applied, reduces inflammatory processes, pot... |
|
TP1752
|
GP(33-41)
|
|
|
|
GP(33-41), a 9-aa-long peptide, is the optimal sequence of the GP1 epitope of lymphocytic choriomeningitis virus, and can upregulate H-2Db molecules at the RMA-S (Db Kb) cell surface with a SC50 of 344 nM. GP33-41 Epitopeis a strong agonist of CD8 T cells |
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T36639
|
Donecopride (fumarate hydrate)
|
Others |
Others |
|
Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value... |
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T35632
|
Pinolenic Acid
|
Others |
Others |
|
Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro.[1] Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an increase in the sa... |
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T63902
|
XP-524
|
Others |
Others |
|
XP-524 是 BET 和 EP300 的有效抑制剂。 XP-524 在体内具有显著的杀肿瘤作用，能够阻止 KRAS 诱导的体内肿瘤转化，并延长两种侵袭性 PDAC 转基因小鼠模型的存活时间。XP-524 也提高了自身肽的表达及将肿瘤细胞向细胞毒性 T 淋巴细胞的募集。XP-524 对胰腺导管腺癌（PDAC）表现出研究潜力。 |
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T35813
|
CAY10592
|
Others |
Others |
|
Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) ... |
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T82907
|
BDC2.5 Mimotope 1040-63
|
|
|
|
BDC2.5 Mimotope 1040-63是具有生物活性的肽，广泛应用于1型糖尿病（T1D）研究中的TCR转基因模型（BDC2.5）模拟表位。T1D是一种涉及自身免疫系统对胰岛β细胞的T细胞介导损害的自身免疫性疾病。BDC2.5模拟表位在研究胰岛素产生细胞遭到自身反应性T细胞破坏的过程中，对支持抗原肽实现向胰岛自身抗原特异性T细胞的抗原呈递具有重要作用。 |
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T36499
|
CuATSM
|
Others |
Others |
|
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 ... |
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T35633
|
Pinolenic Acid ethyl ester
|
Others |
Others |
|
Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an ... |
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T38204
|
GAT229
|
Others |
Others |
|
GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 an... |
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T38218
|
1-Stearoyl-2-docosahexaenoyl-sn-glycero-3-PC
|
Others |
Others |
|
1-Stearoyl-2-docosahexaenoyl-sn-glycero-3-PC 是一种在生物膜中的磷脂，在 sn-1 和 sn-2 位置分别含有硬脂酸和二十二碳六烯酸。它已被用于研究脂膜的组织和动力学。在超氧化物歧化酶 1 突变体转基因小鼠肌萎缩性脊髓侧索硬化症（ALS）模型中1-Stearoyl-2-docosahexaenoyl-sn-glycero-3-PC 的水平在疾病晚期会在 L5 前角下降。1-Stearoyl-2-docosahexaenoyl-sn-glycero-3-PC 可用于研究生物膜。 |
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T35855
|
AAA
|
Others |
Others |
|
AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension... |
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T37791
|
A-971432
|
Others |
Others |
|
A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s ... |
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T36188
|
Ceramide Phosphoethanolamines (bovine)
|
|
|
|
Ceramide phosphoethanolamine (CPE) is an analog of sphingomyelin that contains ethanolamine rather than choline as the head group. It is the principal membrane phospholipid in invertebrates such as Drosophila, which lacks sphingomyelin. It is only produced in small amounts in mammalian cells, accounting for approximately 0.02 mol% of total phospholipids in mouse testis and brain. In Drosophila, CPE is biosynthesized by CPE synthase from ceramide and cytidine diphosphate-ethanolamine in the Golgi... |
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T83955
|
MOMBA
|
Others |
Others |
|
MOMBA是一种针对人类自由脂肪酸2(hFFA2)工程化受体和设计药物激活的设计受体(DREADD)的选择性正交激动剂，对野生型hFFA2、hFFA3和小鼠FFA2无活性。MOMBA能够在表达hFFA2-DREADD受体的细胞中抑制forskolin刺激的cAMP水平，其功效改善且与山梨酸的效力相当。在hFFA2-DREADD转基因小鼠中，MOMBA治疗显著降低肠道传输速度，并促进依赖浓度的结肠隐窝GLP-1释放。该化合物具有口服生物利用度。 |
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T36521
|
Alaproclate (hydrochloride)
|
Others |
Others |
|
Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio... |
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T36911
|
Pramlintide (acetate hydrate)
|
Others |
Others |
|
Pramlintide is a non-amyloidogenic analog of the antidiabetic peptide hormone amylin that contains proline residues substituted at positions 25, 28, and 29. It stimulates cAMP production in HEK293 cells expressing human amylin receptor 1a (AMY1a), AMY2a, and AMY3a (EC50s = 0.35, 22.9, and 0.89 nM, respectively). Pramlintide inhibits human islet amyloid polypeptide fibrilization in a concentration-dependent manner. In vivo, pramlintide (200 pg/kg) reduces brain levels of amyloid-β (1-40) and incr... |
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T35560
|
SAR502250
|
Others |
Others |
|
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... |
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