DQP 1105是一种N-甲基-D-天冬氨酸（NMDA）受体的非竞争性拮抗剂，可抑制含GluN2C和GluN2D亚基受体，IC50值分别为7.0µM和2.7µM。
Cas No.:380560-89-4
Sample solution is provided at 25 µL, 10mM.
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DQP 1105 is a noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptor, which inhibits GluN2C- and GluN2D-containing receptors with IC50 values of 7.0 and 2.7µM [1]. DQP 1105 can reversibly weaken the membrane potential and circadian rhythm of clock gene expression in suprachiasmatic nucleus (SCN) neurons by inhibiting NMDAR2C[2]. DQP 1105 has been widely used for regulating neuronal synaptic responses[3].
In vitro, DQP 1105 treatment (20µM) for 24 hours significantly reduced the levels of Cx43 protein and VIP protein in astrocytes, as well as the level of Clock mRNA[4]. 15µM DQP 1105 treatment for 10 days significantly promoted the growth of pyramidal cells and increased the number of apical dendritic branches of these cells[5]. Treatment with 10µM DQP 1105 for 4 hours can reduce the expression of p-PI3K and p-Akt in CTX-TNA2 cells treated with lipopolysaccharide (LPS) [6].
In vivo, DQP 1105 treatment via a single intraperitoneal injection at a dose of 90mg/kg impaired the motor coordination ability of CD-1 mice within 30 minutes[7]. A single intraperitoneal injection of 28mg/kg dose of DQP 1105 reduced the frequency of epileptic seizures in mice within 2 hours[8].
References:
[1] Acker T M, Yuan H, Hansen K B, et al. Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators[J]. Molecular pharmacology, 2011, 80(5): 782-795.
[2] Brancaccio M, Edwards M D, Patton A P, et al. Cell-autonomous clock of astrocytes drives circadian behavior in mammals[J]. Science, 2019, 363(6423): 187-192.
[3] Mahmoud H, Martin N, Hildebrand M E. Conserved contributions of NMDA receptor subtypes to synaptic responses in lamina II spinal neurons across early postnatal development[J]. Molecular brain, 2020, 13(1): 31.
[4] Xue H, Wu M, Wang Y, et al. The circadian rhythms regulated by Cx43-signaling in the pathogenesis of Neuromyelitis Optica[J]. Frontiers in Immunology, 2023, 13: 1021703.
[5] Köhler I, Rennau L M, Hoffmann L, et al. Activation of GluN2D-containing NMDA receptors promotes development of axons and axon-carrying dendrites of cortical interneurons[J]. Cerebral Cortex, 2025, 35(6): bhaf136.
[6] Gao R, Ali T, Liu Z, et al. NMDAR (2C) deletion in astrocytes relieved LPS-induced neuroinflammation and depression[J]. International Immunopharmacology, 2024, 132: 111964.
[7] Pálfi E, Lévay G, Czurkó A, et al. Acute blockade of NR2C/D subunit‐containing N‐methyl‐D‐aspartate receptors modifies sleep and neural oscillations in mice[J]. Journal of Sleep Research, 2021, 30(4): e13257.
[8] Lozovaya N, Gataullina S, Tsintsadze T, et al. Selective suppression of excessive GluN2C expression rescues early epilepsy in a tuberous sclerosis murine model[J]. Nature communications, 2014, 5(1): 4563.
DQP 1105是一种N-甲基-D-天冬氨酸（NMDA）受体的非竞争性拮抗剂，可抑制含GluN2C和GluN2D亚基受体，IC50值分别为7.0µM和2.7µM[1]。DQP 1105能够通过抑制NMDAR2C而使视交叉上核（SCN）神经元的膜电位和节律基因表达发生可逆性的减弱[2]。DQP 1105已被广泛用于调节神经元突触反应[3]。
在体外，使用20µM的DQP 1105处理星形胶质细胞24小时，显著降低了Cx43蛋白和VIP蛋白的水平，以及Clock mRNA的水平[4]。使用15µM的DQP 1105处理10天，显著促进了锥体细胞的生长，并增加了细胞的顶端树突分支数量[5]。使用10µM的DQP 1105处理经脂多糖（LPS）处理的CTX-TNA2细胞4小时，可降低p-PI3K和p-Akt的表达[6]。
在体内，单次腹腔注射90mg/kg剂量的DQP 1105，在30分钟内损害了CD-1小鼠的运动协调能力[7]。单次腹腔注射28mg/kg剂量的DQP 1105，在2小时内降低了小鼠癫痫发作的频率[8]。
| Cell experiment [1]: | |
Cell lines | Mouse primary astrocytes |
Preparation Method | Mouse primary astrocytes were cultured in high-glucose DMEM medium supplemented with 10% fetal bovine serum (FBS) and 1% Penicillin/Streptomycin at 37℃ in the presence of 5% CO2. The anti-AQP4 IgG (5μg/ml) and human complement C3 (10μg/ml) were added into the culture medium of astrocytes for 24h to induce the neuromyelitis optica phenotype. After treating with 20µM DQP 1105 for 24 hours, the levels of Cx43 protein and VIP protein were analyzed. |
Reaction Conditions | 20µM; 24h |
Applications | DQP 1105 treatment reduced the levels of Cx43 protein and VIP protein in astrocytes. |
| Animal experiment [2]: | |
Animal models | CD-1 mice |
Preparation Method | 3-month-old male CD1 mice (35-48g) were maintained in a temperature and humidity-controlled environment under a 12-12h dark-light cycle (06:00 to 18:00 hours for light) with food and water available ad libitum. A single intraperitoneal injection of 90mg/kg dose of DQP 1105 or ketamine (20mg/kg) as a positive control was administered, and a rotating rod test was conducted within 30 minutes. |
Dosage form | 90mg/kg for once; i.p. |
Applications | DQP 1105 treatment significantly impaired motor coordination in mice. |
References: | |
| Cas No. | 380560-89-4 | SDF | |
| 化学名 | 4-((R)-5-(4-bromophenyl)-3-((R)-6-methyl-2-oxo-4-phenyl-2,3-dihydroquinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid | ||
| Canonical SMILES | BrC1=CC=C(C=C1)[C@@H]2N(C(CCC(O)=O)=O)N=C([C@H]3C(C4=CC=CC=C4)=C(C=C(C)C=C5)C5=NC3=O)C2 | ||
| 分子式 | C29H24BrN3O4 | 分子量 | 558.42 |
| 溶解度 | <55.84mg/ml in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7908 mL | 8.9538 mL | 17.9077 mL |
| 5 mM | 358.2 μL | 1.7908 mL | 3.5815 mL |
| 10 mM | 179.1 μL | 895.4 μL | 1.7908 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00% Appearance: A solid
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