Bay 60-7550
(Synonyms: BAY 607550) 目录号 : GC19512
Bay 60-7550是一种高效磷酸二酯酶2(PDE2)抑制剂，对从牛心脏中纯化的PDE2的IC50值为2.0±0.7nM。
Cas No.:439083-90-6
Sample solution is provided at 25 µL, 10mM.
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Bay 60-7550 is a potent inhibitor of Phosphodiesterase 2 (PDE2) purified from bovine heart with an IC50 value of 2.0±0.7nM[1]. Bay 60-7550 increased cGMP and cAMP levels and promoted cGMP signaling[2]. Bay 60-7550 has been widely used in different animal models to improve depression-like behaviors and enhance brain function[3].
In vitro, Bay 60-7550 treatment (1µM) for 24h rescued HT-22 cells from the cytotoxicity induced by 50µM corticosterone and reversed down-regulation of CBP proteins induced by corticosterone[4]. Treatment with 1µM Bay 60-7550 for 48 hours blocked oxidative stress and apoptosis in mouse primary cortical neuronal cells treated with Aβ1-42 oligomers[5].
In vivo, Bay 60-7550 treatment via intraperitoneal injection at a dose of 3mg/kg twice daily for 4 days reduced ethanol preference and intake without affecting locomotor activity in C57BL/6J mice[6]. BAY 60-7550 treatment (p.o.) at a daily dose of 1mg/kg for 21 days alleviated bilateral common carotid artery occlusion (BCCAO)-induced behavioral deficits in mice and enhanced the expression of pCREB and BDNF proteins in the hippocampus of mice[7]. Intraperitoneal injection of BAY 60-7550 at a daily dose of 3mg/kg for 14 days reversed Aβ1-42-induced memory impairment in mice[8].
References:
[1] Boess F G, Hendrix M, van der Staay F J, et al. Inhibition of phosphodiesterase 2 increases neuronal cGMP, synaptic plasticity and memory performance[J]. Neuropharmacology, 2004, 47(7): 1081-1092.
[2] Masood A, Huang Y, Hajjhussein H, et al. Anxiolytic effects of phosphodiesterase-2 inhibitors associated with increased cGMP signaling[J]. The Journal of pharmacology and experimental therapeutics, 2009, 331(2): 690-699.
[3] Huang X, Xiaokaiti Y, Yang J, et al. Inhibition of phosphodiesterase 2 reverses gp91phox oxidase-mediated depression-and anxiety-like behavior[J]. Neuropharmacology, 2018, 143: 176-185.
[4] Xu Y, Pan J, Chen L, et al. Phosphodiesterase-2 inhibitor reverses corticosterone-induced neurotoxicity and related behavioural changes via cGMP/PKG dependent pathway[J]. International Journal of Neuropsychopharmacology, 2013, 16(4): 835-847.
[5] Yan Y, Gao S, Avasthi S, et al. Protective effects of phosphodiesterase 2 inhibitor against Aβ1-42 induced neuronal toxicity[J]. Neuropharmacology, 2022, 213: 109128.
[6] Shi J, Liu H, Pan J, et al. Inhibition of phosphodiesterase 2 by Bay 60-7550 decreases ethanol intake and preference in mice[J]. Psychopharmacology, 2018, 235(8): 2377-2385.
[7] Soares L M, Meyer E, Milani H, et al. The phosphodiesterase type 2 inhibitor BAY 60-7550 reverses functional impairments induced by brain ischemia by decreasing hippocampal neurodegeneration and enhancing hippocampal neuronal plasticity[J]. European Journal of Neuroscience, 2017, 45(4): 510-520.
[8] Ruan L, Du K, Tao M, et al. Phosphodiesterase-2 inhibitor bay 60-7550 ameliorates Aβ-induced cognitive and memory impairment via regulation of the HPA Axis[J]. Frontiers in cellular neuroscience, 2019, 13: 432.
Bay 60-7550是一种高效磷酸二酯酶2(PDE2)抑制剂，对从牛心脏中纯化的PDE2的IC50值为2.0±0.7nM[1]。Bay 60-7550可通过提升细胞内cGMP与cAMP水平增强cGMP信号通路[2]。Bay 60-7550已广泛应用于多种动物模型中以改善抑郁样行为及增强脑功能[3]。
在体外，1µM的Bay 60-7550处理24小时能有效保护HT-22细胞免受50µM皮质酮诱导的细胞毒性，并逆转皮质酮引起的CBP蛋白下调[4]。使用1µM的Bay 60-7550处理小鼠原代皮层神经元细胞48小时，可阻断Aβ1-42寡聚体诱导的氧化应激与细胞凋亡[5]。
在体内，每日两次腹腔注射3mg/kg剂量的Bay 60-7550，连续4天，可降低C57BL/6J小鼠对乙醇的偏好和摄入量，且不影响自主活动[6]。每日口服1mg/kg剂量的Bay 60-7550，连续21天，能缓解双侧颈总动脉结扎(BCCAO)引起的小鼠行为缺陷，并增强海马组织中pCREB与BDNF蛋白表达[7]。每日腹腔注射3mg/kg剂量的Bay 60-7550，连续14天，可逆转Aβ1-42诱导的小鼠记忆功能障碍[8]。
| Cell experiment [1]: | |
Cell lines | HT-22 cells |
Preparation Method | HT-22 cells were cultured in DMEM medium containing 10% FBS at 37°C in 5% CO2. Cells were seeded in 96-well plates at a density of 1×105 cells/well. Cells were divided into three groups: control group, 50µM corticosterone treatment group, and 50µM corticosterone+1µM Bay 60-7550 experimental group. After 24 hours, 10µl MTT solution was added to each well and incubated for an additional 4 hours at 37°C. The medium in each well was then replaced with 200µl DMSO, and the absorbance at 570nm was measured. |
Reaction Conditions | 1µM; 24h |
Applications | Bay 60-7550 treatment significantly rescued HT-22 cells from corticosterone-induced cytotoxicity. |
| Animal experiment [2]: | |
Animal models | Male C57bL/6 mice |
Preparation Method | Male C57bL/6 mice (25-30g; 3 months of age) were housed at a controlled temperature (22±1°C) with a 12h/12h light/dark cycle (lights on at 7:00 am). The mice had ad libitum access to food and water. Transient cerebral ischemia was induced by BCCAO. Vehicle or BAY 60-7550 was administered by oral gavage (p.o.) at a dose of 1mg/kg/day for 21 days, followed by behavioral testing. |
Dosage form | 1mg/kg/day for 21 days; p.o. |
Applications | BAY 60-7550 treatment alleviated BCCAO-induced behavioral disorders and anxiety in mice. |
References: | |
| Cas No. | 439083-90-6 | SDF | |
| 别名 | BAY 607550 | ||
| Canonical SMILES | O=C1N=C(NN2C1=C(N=C2[C@@H](CCCC3=CC=CC=C3)[C@@H](C)O)C)CC4=CC=C(C(OC)=C4)OC | ||
| 分子式 | C₂₇H₃₂N₄O₄ | 分子量 | 476.57 |
| 溶解度 | Acetone: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml | 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 | 2.0983 mL | 10.4916 mL | 20.9833 mL |
| 5 mM | 419.7 μL | 2.0983 mL | 4.1967 mL |
| 10 mM | 209.8 μL | 1.0492 mL | 2.0983 mL |
| 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 | ||||||||||
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet