目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T1445 | Melatonin Receptor 5-HT Receptor | ||
Agomelatine (Valdoxan) 是褪黑激素受体的强效激动剂和 5-羟色胺-2C (5-HT2C) 受体的拮抗剂,在猪和人 5-HT2C 克隆受体中pKi 分别为 6.4 和 6.2。 | |||
T1199 | Apoptosis AChR | ||
Mitotane (NCI-C04933) 是 DDD 的同分异构体和 DDT 的衍生物,可作用于肾上腺皮质癌,有抗癌活性。 | |||
T12632L | 5-HT Receptor | ||
(S)-Mirtazapine ((S)-Org3770) 是 Mirtazapine 的 S(+)-对映体。(S)-Mirtazapine 是一种选择性 5-HT2 受体拮抗剂,具有促痛觉作用,常与Mirtazapine 的 R(-)-对映体混合使用来研究抑郁症。 | |||
T90597 | |||
SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1抑制剂 (hGlyT1,rGlyT1,mGlyT1IC50分别为 18、15 和 38 nM)。SSR504734 在精神分裂症、焦虑症和抑郁症模型中表现出活性。 | |||
T22947 | 5-HT Receptor | ||
LY266097 hydrochloride (LY 266097 hydrochloride) 是 5-HT2 的拮抗剂,对人 5-HT2A、5-HT2B 和 5-HT2C 的 pKis 分别为 7.7、9.8 和 7.6,可用于抑郁症研究。 | |||
T4559 | Monoamine Oxidase | ||
Isocarboxazid 是不可逆的、非选择性的单胺氧化酶 monoamine oxidase 抑制剂,其在大鼠大脑中测得的 IC50值为4.8 μM。 | |||
T16265 | EGFR 5-HT Receptor | ||
Naluzotan(PRX 00023) 是一种新型高效的 5-HT1A 激动剂,IC50 和 Ki 值分别为约 20 nM 和 5.1 nM。Naluzotan 是一种有效的 hERG K+ 通道阻滞剂,IC50 值为 3800 nM。Naluzotan 具有抗焦虑活性,可用于研究抑郁症。 | |||
T0025 | Dopamine Receptor 5-HT Receptor | ||
Haloperidol (Serenace) 是一种安定药,是一种dopamine D2 receptor 拮抗剂。 | |||
TQ0145 | Calcium Channel PPAR | ||
(R)-(+)-Bay-K-8644 是一种 Ca2+ 通道激动剂,是二氢吡啶激动剂,抑制 Ba2+电流 (IBa),诱导猫的中枢性呼吸抑制,通过竞争性拮抗血栓素 A2-前列腺素 H2 受体抑制血小板活化。 | |||
T50061 | Others | ||
[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methanamine 是一种哌嗪衍生物,它是血清素和多巴胺受体的部分激动剂,使其成为治疗抑郁症和精神分裂症等精神疾病的候选药物。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
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.
|
|||||
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.
|
|||||
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.
|
|||||
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
|
|||||
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.
|