PF-05180999
(Synonyms: PF-999) 目录号 : GC30828
A PDE2A inhibitor
Cas No.:1394033-54-5
Sample solution is provided at 25 µL, 10mM.
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PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor (IC50 = 1.6 nM).1 It is greater than 2000-fold selective for PDE2A over a panel of ten additional PDEs. PF-05180999 increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner. In vivo, it inhibits disruption of low frequency cortical δ oscillation induced by the NMDA antagonist MK-801 in rat brain when administered at a dose of 0.03 mg/kg. PF-05180999 (0.1 and 0.32 mg/kg) inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats.
1.Helal, C.J., Arnold, E., Boyden, T., et al.Identification of a potent, highly selective, and brain penetrant phosphodiesterase 2A inhibitor clinical candidateJ. Med. Chem.61(3)1001-1018(2018)
Animal experiment: | Rats[1]Male Sprague-Dawley rats (weighing 250-320 g) under urethane anesthesia at 1.5 g/kg intraperitoneal (ip) are placed in a stereotaxic frame, where craniotomies are performed above the region of the medial prefrontal cortex (mPFC) and ipsilateral (CA)1/subiculum. Body temperature of the rat is maintained at 37°C with an electrical heating pad. The femoral vein is cannulated for administration of test drugs (PF-05180999, etc.). After the conclusion of the experiments animals are euthanized with an iv bolus of urethane[1]. |
References: [1]. Helal CJ, et al. Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. J Med Chem. 2018 Feb 8;61(3):1001-1018. | |
| Cas No. | 1394033-54-5 | SDF | |
| 别名 | PF-999 | ||
| Canonical SMILES | CC1=NC(C2=C(C3=CC=C(C(F)(F)F)C=N3)N(C)N=C2)=C4N1N=CN=C4N5CCC5 | ||
| 分子式 | C19H17F3N8 | 分子量 | 414.39 |
| 溶解度 | DMSO : 50 mg/mL (120.66 mM) | 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 | 2.4132 mL | 12.0659 mL | 24.1319 mL |
| 5 mM | 0.4826 mL | 2.4132 mL | 4.8264 mL |
| 10 mM | 0.2413 mL | 1.2066 mL | 2.4132 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
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet