目录号 | 产品详情 | 靶点 | |
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T62805 | |||
SB-612111 hydrochloride 是一种高效的、新型的阿片受体孤儿受体 (ORL-1) 拮抗剂,对 hORL-1 具有较高的亲和力,Ki 值为 0.33 nM。SB-612111 hydrochloride 能够作用于 μ-receptor (Ki: 57.6 nM),κ-receptor (Ki: 160.5 nM) 和 δ-receptor (Ki: 2109 nM)。SB-612111 hydrochloride 能有效拮抗 Nociceptin 在急性疼痛模型中的造成的痛觉作用。 | |||
T73272 | |||
VU6019650 是一种强效、选择性的M5mAChR 正向拮抗剂 (IC50=36 nM),能够用于减轻阿片类药物使用障碍 (OUD) 的研究。VU6019650 具有血脑透过性,可能调节中边缘多巴胺能奖赏回路。VU6019650 能够阻断Oxotremorine M iodide 诱导引起的腹侧被盖区中脑 (VTA) 多巴胺神经元的放电速率的增加。 | |||
T76598 | |||
H-Ser-Tyr-OH是一种由谷氨酸、甘氨酸和组氨酸组成的二肽。它能与铜离子形成的铜(II)配合物生成,表现出较强的自由基清除活性。此外,H-Ser-Tyr-OH还能增加deltorphin这一δ阿片受体配体的细胞内摄取。 | |||
T81763 | |||
MOR Agonist-3 (Compound 84) 是一种双重作用化合物,具有D3R/MOR拮抗活性(Ki值为55.2 nM和382 nM)。该化合物其MOR部分激动性质展现出镇痛潜力,并可能通通过D3R拮抗作用降低阿片类药物的滥用风险。MOR Agonist-3 亦适用于炎症治痈和神经性疼痛的研究领域。 | |||
T76337 | |||
[DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) 是猪脑垂体提取物中发现的阿片肽(dynorphinl-13, DYN)的一个衍生物。该化合物对GPI和MVD的外周阿片受体有高效力,但在体内易被快速分解。与原始肽相比,[DAla2, DArg6] Dynorphin A, (1-13) (porcine) 更具酶解稳定性,能有效抵抗酶的裂解作用。 | |||
T38030 | |||
(R)-AM1241 binds to cannabinoid (CB) receptors and has greater than 100-fold selectivity for the CB2 over the CB1 receptor (Kis = 15 and 5,000 nM, respectively, in a membrane assay using human receptors). (R)-AM1241 acts as an agonist at human CB2 receptors (EC50 = 118 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 315 and 341 nM, respectively). Similar to the racemate AM1241 , (R)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (R)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone . | |||
T73676 | |||
MIF-1 TFA(Melanostatin)是一种内源性脑肽,具有有效调节多巴胺受体变构的作用,并抑制黑色素生成。此外,它通过阻断阿片受体的激活,调控吗啡的镇痛效果及应激诱导的镇痛(SIA)。MIF-1 TFA 能直接穿过血脑屏障(BBB)进入中枢神经系统。 | |||
T83899 | |||
N-didesmethyl Loperamide是loperamide的一个活性代谢产物,属于周围μ1-阿片受体激动剂。它能抑制孤立的豚鼠肠膜丛中由电刺激引起的收缩(IC50 = 370 nM)。N-didesmethyl Loperamide还能增强对氯喹产生抗药性的P. falciparum菌株对氯喹的敏感性(EC50 = 482 nM),同时在A-10血管平滑肌细胞中未引起毒性(IC50 = >10,000 nM)。 | |||
T38147 | |||
(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat and mouse CB2 receptors (EC50 = 785 and 2,000 nM, respectively). Similar to the racemate AM1241 , (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (S)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone . | |||
T83685 | |||
UFP101是一种合成肽类物质,作为nociceptin受体的拮抗剂(Ki为0.06 nM,测试于表达人类受体的CHO细胞中)。它对nociceptin受体的选择性高于κ-opioid受体(Ki为204 nM,测试于表达大鼠受体的CHO细胞中)。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS(EC50为1.86 nM)。通过脑室内给药,UFP101(10 nmol/每只动物)能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中,UFP101(0.003、0.03及0.3 mg/kg)能提高生存率。 |
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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