目录号 | 产品详情 | 靶点 | |
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T69419 | |||
Vestipitant mesylate is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia. | |||
T60430 | |||
Protriptyline 是有效的抗抑郁剂,抑制AChE 活性(IC50 =.06 mM),并可抑制 Aβ 自组装。Protriptyline 具有用于抑郁症和阿尔茨海默病的研究潜力。 | |||
T2579 | Norepinephrine | ||
Reboxetine (Norebox) 是一种抗抑郁药,用于治疗临床抑郁症、恐慌症和 ADD/ADHD。它有两个手性中心,但它仅作为两种对映体存在,(R, R)-(-)- 和 (S, S)-(+)-Reboxetine。 | |||
T79056 | |||
Orexin receptormodulator-1 是一款针对食欲素受体的调节剂,主要应用于物质成瘾、惊恐障碍、焦虑、创伤后应激障碍 (PTSD)、疼痛、抑郁、季节性情感障碍、进食障碍及高血压的科研领域。 | |||
T73530 | |||
2-PAT 是一种 Rasagiline 和 Selegiline 的类似物,也是可逆的 MAO-A 抑制剂,IC50为 0.721 µM。2-PAT 是 MAO-B 的灭活剂,IC50为 14.6 µM。2-PAT 具有用于帕金森病和抑郁症研究的潜力。 | |||
T76311 | |||
PE 22-28为TREK-1抑制剂,具有0.12 nM的IC50值。该化合物也是包含7个氨基酸的肽,作为通过化学修饰与氨基酸替换来制备类似物的关键序列。PE 22-28可用于抑郁症研究。 | |||
T29183 | |||
YM-430 is a β1 adrenergic receptor antagonist and a calcium channel antagonist. YM430 could be both an antianginal and antihypertensive agent. YM430 (10(-8)-10(-6) M) inhibited 3,4-diaminopyridine-induced rhythmic contractions with an IC50 value of 59.2 n | |||
T74582 | |||
Trimipramine N-oxide 为三环抗抑郁药trimipramine的活性代谢物,其对人去甲肾上腺素单胺转运体(hNAT)、血清素(hSERT)、多巴胺(hDAT)以及人体有机阳离子转运蛋白(hOCT1与hOCT2)的IC50值分别为11.7、3.59、9.4、9.35及27.4 nM。因此,Trimipramine N-oxide在忧郁和焦虑研究中有应用价值。 | |||
TN1194 | HIV Protease | ||
16beta,17-Dihydroxy-ent-kaurane-19-oic acid as an anti-HIV principle, it showed significant activity against HIV replication in H9 lymphocyte cells with an EC50 value of 0.8 microgram/mL. It also possesses the activities of decompression and blood viscosi | |||
T37212 | |||
5-hydroxy-Nω-methyl Tryptamine is a metabolite of serotonin in humans that has also been found in plants. It is an agonist of the 5-HT receptor subtype 5-HT7 (IC50 = 23 pM in a radioligand binding assay). 5-hydroxy-Nω-methyl Tryptamine increases intracellular cyclic AMP production in HEK293 cells expressing 5-HT7 (EC50 = 22 nM). It inhibits serotonin uptake in HEK293 cells expressing human serotonin transporters (IC50 = 490 nM). Elevated levels of urinary 5-hydroxy-Nω-methyl tryptamine have been found in patients with schizophrenia, depression, and epilepsy. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-05510 | BDNF Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
BDNF is a member of thenerve growth factorfamily. It is highly expressed in hippocampus, amygdala, cerebral cortex and cerebellum. It also can be detected in heart, lung, skeletal muscle, testis, prostate and placenta. BDNF is induced by cortical neurons, and is necessary for survival of striatal neurons in the brain. During development, BDNF promotes the survival and differentiation of selected neuronal populations of the peripheral and central nervous systems. It participates in axonal growth, pathfinding and in the modulation of dendritic growth and morphology. It functions as the major regulator of synaptic transmission and plasticity at adult synapses in many regions of the CNS. The versatility of BDNF is emphasized by its contribution to a range of adaptive neuronal responses including long-term potentiation (LTP), long-term depression (LTD), certain forms of short-term synaptic plasticity, as well as homeostatic regulation of intrinsic neuronal excitability.
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TMPY-02442 | ELK1 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
E twenty-six (ETS)-like transcription factor 1, also known as Elk1 or Member of ETS oncogene family (ELK1), is a member of the ETS oncogene superfamily which is characterized by a common protein domain that regulates DNA binding to target sequences. Elk1 is expressed in the nuclei of non-neuronal cells and function as a transcription activator. It plays important roles in various contexts, including long-term memory formation, drug addiction, Alzheimer's disease, Down syndrome, breast cancer, and depression.
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TMPY-04408 | CAMKII beta/CAMK2B Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Calcium/calmodulin-dependent protein kinase II beta (CAMK2B) is a member of the serine/threonine protein kinase family and to the Ca(2+)/calmodulin-dependent protein kinase subfamily. CaMKII is an important player in prostate cancer cells ability to escape apoptosis under androgen ablation and facilitate the progression of prostate cancer cells to an androgen independent state. As a multifunctional protein kinase, the loss of activity may play a critical role in initiating the changes leading to ischemia-induced cell death. CaMKII are found to be important for the functions of immune cells. CaMKII can be activated by TLR ligands, and in turn promotes both myeloid differentiating factor 88 and Toll/IL-1 receptor domain-containing adaptor protein-inducing IFN-beta-dependent inflammatory responses by directly activating TAK1 and IRF3. CAMKII has four subunit isoforms (alpha, beta, gamma, delta). It is possible that distinct isoforms of this chain have different cellular localizations and interact differently with calmodulin. The alpha- and beta-isoforms have narrow distributions restricted mainly to neuronal tissues, but the gamma- and delta-isoforms are ubiquitously expressed within neuronal and non-neuronal tissues. CAMK2B is important for controlling the direction of plasticity at the parallel fiber-Purkinje cell synapse. CaMK2 is involved in neuronal survival through the reorganization of the neuroarchitecture and that the regulation of this role is controlled at the level of gene expression. Because CaMK2B influences the expression of many neuroreceptors and influences neural outgrowth and pruning, its altered expression in the cerebral cortex in schizophrenia or depression may contribute to schizophrenia and depression.
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TMPY-01856 | MGAT5 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Alpha-1,6-mannosylglycoprotein 6-beta-N-acetylglucosaminyltransferase A, also known as Alpha-mannoside beta-1,6-N-acetylglucosaminyl-transferase, Mannoside acetylglucosaminyltransferase 5, N-acetylglucosaminyl-transferase V, MGAT5, and GGNT5, is a single-pass type II membrane protein that belongs to the glycosyltransferase 18 family. MGAT5 / GGNT5 catalyzes the addition of N-acetylglucosamine in beta 1-6 linkage to the alpha-linked mannose of biantennary N-linked oligosaccharides. It is one of the most important enzymes involved in the regulation of the biosynthesis of glycoprotein oligosaccharides. The central nervous system (CNS) is rich in glycoconjugates, located on the cell surface and in the extracellular matrix. MGAT5 / GGNT5 modification of complex-type N-glycans on CNS glycoproteins is involved in the regulation of depression-like behavior. Inhibitors of MGAT5 / GGNT5 might be useful in the treatment of malignancies by targeting their dependency on focal adhesion signaling for growth and metastasis.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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TMPY-02025 | CPLX2 Protein, Human, Recombinant (His) | Human | E. coli | ||
Complexin-2 (CPLX2), a member of the complexin/synaphin family, is a soluble pre-synaptic protein believed to regulate neurotransmitter release from pre-synaptic terminals. Complexins are soluble proteins that regulate the activity of soluble N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE) complexes necessary for vesicle fusion. Complexins are unable to bind to monomeric SNARE proteins but bind with high affinity to ternary SNARE complexes and with lower affinity to target SNARE complexes. Complexin 1 (CX1) and complexin 2 (CX2) are presynaptic proteins that modulate neurotransmitter release and are used as markers of inhibitory and excitatory synapses, respectively. CPLX2 is localized in pre-synaptic terminals in mature brain. The G71-P89 region of CPLX2 is essential and sufficient for preferential axonal distribution. CPLX2 participates in the Ca(2+)-sensitive regulatory pathway for zymogen granule exocytosis. Complexin-2 is a key player in normal neurological function, and its downregulation could lead to changes in neurotransmitter release sufficient to cause significant behavioural abnormalities such as depression. It is involved in synaptogenesis and the modulation of neurotransmitter release.
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