目录号 | 产品详情 | 靶点 | |
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TN4064 | Phosphatase IL Receptor TNF NOS NF-κB COX Nrf2 Prostaglandin Receptor Autophagy | ||
Flavoglaucin exhibits significant inhibitory effects on PTP1B, the IC50 value of 13.4, micrometer; it also shows good binding affinity for human opioid or cannabinoid receptors. Flavoglaucin appears to be an antitumor promoter, it also has anti-inflammato | |||
T75895 | |||
UFP-101 TFA 是一种强效、选择性和竞争性的 NOP 受体拮抗剂,pKi 为 10.24。UFP-101 TFA 对 δ、μ 和 κ 类阿片受体的选择性大于 3000 倍。UFP-101 TFA 具有抗抑郁药样作用。 | |||
T78779 | Dopamine Receptor | ||
D3R/MOR antagonist 2(Compound 121)为一种D3R/MOR拮抗剂,其Ki值分别为46.5 nM及691 nM。该化合物通过MOR部分激动作用可产生镇痛效果,并通过D3R拮抗减少阿片类药物的潜在滥用风险。 | |||
T83676 | |||
Tianeptine metabolite MC5是一种来自非典型抗抑郁化合物tianeptine的活性代谢物,通过β-氧化形成。此代谢物在使用表达人类μ-阿片受体(MOR)而非人类δ-阿片受体(DOR;EC50s = 0.454和 >100 µM, 分别)的HEK293T细胞进行的生物发光共振能量转移(BRET)试验中,特异性诱导G蛋白激活。在野生型小鼠上,30 mg/kg剂量的Tianeptine metabolite MC5可减少强迫游泳测试中的静止时间,但在MOR敲除小鼠中则不会,表明其具有MOR依赖的抗抑郁样活性。 | |||
T80421 | Opioid Receptor | ||
CSD-CH2(1,8)-NH2 是一种针对KOR的选择性且竞争性拮抗剂,具有较低的Ki值(6.8 nM),能够抑制DRG神经元内的钙动员,并能拮抗U50,488的抗伤害效应,常用于神经精神疾病研究领域。 | |||
T75896 | |||
[Arg14,Lys15]Nociceptin TFA 是一种高效、选择性的 NOP (ORL1; OP4)受体激动剂,EC50为 1 nM。[Arg14,Lys15]Nociceptin TFA 对阿片受体具有较高的选择性,对 NOP、μ、δ 和 κ 受体的 IC50值分别为 0.32、280、>10000 和 1500 nM。 | |||
T71955 | |||
C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mechanical allodynia and inflammation. C3001a represents a lead compound which could advance the rational design of peripherally acting analgesics targeting K2P channels without opioid-like adverse effects. | |||
T79547 | Opioid Receptor | ||
MOR agonist-2 (Compound 46) 为D3R拮抗剂及MOR激动剂,其Ki值分别为7.26 nM和564 nM。MOR agonist-2潜在以MOR部分激动机制实现镇痛效果,并通过D3R拮抗降低阿片类药物的滥用风险。 | |||
T76420 | |||
Nocistatin 是一种神经肽,是孤儿类阿片受体的内源性配体。 Nocistatin 还是神经肽伤害感受肽或孤啡肽 FQ (Noc/OFQ) 的功能性拮抗剂。Nocistatin 通过 Gi/o 蛋白介导途径抑制 5-HT 释放。Nocistatin 阻断 Nociceptin 诱导的异常性疼痛和痛觉过敏。 | |||
T16507 | Casein Kinase | ||
PF-5006739 is an effective and selective inhibitor of CK1δ/ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selecti |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-04733 | OPCML Protein, Rat, Recombinant (hFc) | Rat | HEK293 Cells | ||
OPCML Protein, Rat, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 59 kDa and the accession number is P32736-1.
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TMPY-00893 | OPCML Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
OPCML Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 34 kDa and the accession number is A8K0Y0.
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TMPY-03818 | OPCML Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
OPCML Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 32.7 kDa and the accession number is Q6DFY2.
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TMPJ-00737 | PDYN Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Proenkephalin-B(PDYN), belongs to the opioid neuropeptide precursor family. The N-terminal domain contains 6 conserved cysteines thought to be involved in disulfide bonding and/or processing. Leu-enkephalins, which is a type of Proenkephalin-B, compete with and mimic the effects of opiate drugs. They play a role in a number of physiologic functions, including pain perception and responses to stress. Dynorphin peptides differentially regulate the kappa opioid receptor. Dynorphin A has a typical opiod activity, it is 700 times more potent than Leu-enkephalin.
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TMPH-02020 | RGS17 Protein, Human, Recombinant (GST) | Human | E. coli | ||
Regulates G protein-coupled receptor signaling cascades, including signaling via muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2. Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits, thereby driving them into their inactive GDP-bound form. Binds selectively to GNAZ and GNAI2 subunits, accelerates their GTPase activity and regulates their signaling activities. Negatively regulates mu-opioid receptor-mediated activation of the G-proteins. RGS17 Protein, Human, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 51.4 kDa and the accession number is Q9UGC6.
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TMPJ-00513 | LTF Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Lactotransferrin is a member of the transferrin family that transfer iron to the cells and control the level of free iron in the blood and external secretions. Lactotransferrin is a secreted protein and contains two transferrin-like domains. Lactotransferrin can be cleaved into the following four chains: Kaliocin-1, Lactoferroxin-A, Lactoferroxin-B, and Lactoferroxin-C. Lactoferroxin A, Lactoferroxin B, and Lactoferroxin C have opioid antagonist activity. Lactoferroxin A shows preference for mu-receptors, while Lactoferroxin B and Lactoferroxin C have somewhat higher degrees of preference for kappa-receptors than for mu-receptors. LTF has antimicrobial activity (bacteriocide, fungicide) and is part of the innate defense, mainly at mucoses.
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TMPY-04121 | NAGA Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
NAGA (Alpha-N-Acetylgalactosaminidase) is a Protein Coding gene. NAGA encodes the lysosomal enzyme alpha-N-acetylgalactosaminidase, which cleaves alpha-N-acetylgalactosaminyl moieties from glycoconjugates. It belongs to the glycosyl hydrolase 27 family. The antinociceptive effect of NAGA may involve the participation of endogenous opioid peptides and endogenous catecholamines. Normal alpha-NAGA is synthesized as a 52 kDa precursor which matures to a 49 kDa species through phosphorylation and carbohydrate trimming. Mutations in gene encoding alpha-NAGA cause a wide range of diseases, characterized by mild to severe clinical features. NAGA is widely expressed in the placenta, appendix, and other tissues. Diseases associated with NAGA include Kanzaki Disease and Schindler Disease, Type I.
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