RC-3095是一种胃泌素释放肽（GRP）受体拮抗剂。
Cas No.:138147-78-1
Sample solution is provided at 25 µL, 10mM.
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RC-3095 is a gastrin-releasing peptide (GRP) receptor antagonist[1]. GRP affects several systems in mammals, including neuroendocrine regulation, gastrointestinal secretion, and cell proliferation[2]. RC-3095 works by blocking bombesin/GRP receptors and is considered an anticancer drug with clinical application value[3].
In vitro, treatment with RC-3095 for 48h inhibited proliferation at 0.1nM but stimulated proliferation at 100nM in Neuro2a murine neuroblastoma cells[4].
In vivo, RC-3095 treatment (1mg/kg; s.c.; twice daily for 2 or 10 days) significantly reduced neutrophil migration, mechanical hypernociception, and proteoglycan loss in mice with AIA (antigen-induced arthritis)[2]. Administration of RC-3095 (0.3 or 1mg/kg; s.c.; twice daily for 10 days) significantly decreased arthritis clinical scores and reduced disease severity as assessed by histological analysis in mice with CIA (collagen-induced arthritis)[2]. A single intraperitoneal injection of RC-3095 (0.2 or 1.0mg/kg) 30 minutes before behavioral testing impaired short-term and long-term inhibitory avoidance memory in mice, but did not affect their cognitive memory[3].
References:
[1]Qin Y, Halmos G, Cai RZ, Szoke B, Ertl T, Schally AV. Bombesin antagonists inhibit in vitro and in vivo growth of human gastric cancer and binding of bombesin to its receptors. J Cancer Res Clin Oncol. 1994;120(9):519-528.
[2] Oliveira PG, Grespan R, Pinto LG, et al. Protective effect of RC-3095, an antagonist of the gastrin-releasing peptide receptor, in experimental arthritis. Arthritis Rheum. 2011;63(10):2956-2965.
[3] Roesler R, Kopschina MI, Rosa RM, Henriques JA, Souza DO, Schwartsmann G. RC-3095, a bombesin/gastrin-releasing peptide receptor antagonist, impairs aversive but not recognition memory in rats. Eur J Pharmacol. 2004;486(1):35-41.
[4] Abujamra AL, Almeida VR, Brunetto AL, Schwartsmann G, Roesler R. A gastrin-releasing peptide receptor antagonist stimulates Neuro2a neuroblastoma cell growth: prevention by a histone deacetylase inhibitor. Cell Biol Int. 2009;33(8):899-903.
RC-3095是一种胃泌素释放肽（GRP）受体拮抗剂[1]。GRP影响哺乳动物的多个系统，包括神经内分泌调节、胃肠道分泌和细胞增殖[2]。RC-3095通过阻断胃泌素释放肽/GRP受体发挥作用，被认为是一种具有临床应用价值的抗癌药物[3]。
体外实验中，在Neuro2a小鼠神经母细胞瘤细胞中，0.1nM的RC-3095处理48小时可抑制细胞增殖，而100nM的RC-3095则可促进细胞增殖[4]。
体内实验中，皮下注射RC-3095（1mg/kg；每日两次；持续2天或10天）可显著减少抗原诱导关节炎（AIA）小鼠模型中中性粒细胞迁移、机械性痛觉过敏和蛋白聚糖丢失[2]。皮下注射RC-3095（0.3或1mg/kg；每日两次；持续10天）可显著降低胶原诱导关节炎（CIA）小鼠的关节炎临床评分[2]。在行为测试前30分钟，单次腹腔注射RC-3095（0.2或1.0mg/kg）会损害小鼠的短期和长期抑制性回避记忆，但不会影响其识别记忆[3]。
| Cell experiment [1]: | |
Cell lines | Neuro2a neuroblastoma cells |
Preparation Method | Cells were seeded at 5x104 cells/well in 24-well plates and treated 24h later with RC-3095 (0.1, 1, 10, or 100nM). 48 hours later, the medium was removed and the cells were washed twice with HBSS. They were detached with 0.25% trypsin/EDTA and 10mL of cellular suspension was homogenized 1:1 with 0.4% trypan blue solution. Cells were counted immediately in a hemocytometer. |
Reaction Conditions | 0.1, 1, 10, or 100nM; 48h |
Applications | RC-3095, at 0.1nM inhibited, whereas at 100nM stimulated proliferation of Neuro2a murine neuroblastoma cells |
| Animal experiment [2]: | |
Animal models | Male Balb/c wild-type mice with AIA (antigen-induced arthritis) model; Male DBA/1J inbred mice with CIA (collagen-induced arthritis) model |
Preparation Method | AIA studies: The Balb/c mice were injected with RC-3095 (1mg/kg; s.c.) or vehicle (0.9% saline) twice a day for a total of 2 or 10 days, starting on the second day before the induction of arthritis. CIA studies: mice were randomly divided into 4 groups. Group 1 comprised mice that were not manipulated, group 2 comprised immunized mice treated with vehicle, and groups 3 and 4 comprised immunized mice treated with either 0.3mg/kg (group 3) or 1mg/kg (group 4) RC-3095, administered s.c. twice a day for 10 days after the onset of the disease. |
Dosage form | AIA studies: 2mg/kg/d; 2 or 10d; s.c. CIA studies: 0.6 or 2mg/kg/d; 10d; s.c. |
Applications | In mice with AIA, administration of RC-3095 reduced neutrophil migration, mechanical hypernociception, and proteoglycan loss. In the CIA model, treatment with RC-3095 led to a significant reduction in arthritis clinical scores and the severity of disease determined histologically. |
References: | |
| Cas No. | 138147-78-1 | SDF | |
| 分子式 | C56H79N15O9 | 分子量 | 1106.32 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 903.9 μL | 4.5195 mL | 9.039 mL |
| 5 mM | 180.8 μL | 903.9 μL | 1.8078 mL |
| 10 mM | 90.4 μL | 451.9 μL | 903.9 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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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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