PF-04957325
目录号 : GC32701
PF-04957325是一种高效，选择性的PDE8抑制剂，抑制PDE8A和PDE8B的IC50值分别为0.7nM和0.3nM。
Cas No.:1305115-80-3
Sample solution is provided at 25 µL, 10mM.
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PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.
PF-04957325 is over two orders of magnitude less efficient than PICL in suppressing polyclonal Teff cell proliferation, and shows no effect on cytokine gene expression in these cells, despite its robust effect on T cell adhesion[1]. PF-04957325 is a selective PDE8 inhibitor and inhibits breast cancer cell migration[2]. PF-04957325 greatly potentiates steroidogenesis in WT adrenal cells. PF-04957325 shows a reported IC50 of 0.7 nM against PDE8A, 0.2 nM against PDE8B, and > 1.5 μM against all other PDE isoforms[3]. PF-04957325 treatment of WT Leydig cells or MA10 cells increases steroid production but has no effect in PDE8A (-/-)/B(-/-) double-knockout cells, confirming the selectivity of the drug. Moreover, under basal conditions, cotreatment with PF-04957325 plus rolipram, a PDE4-selective inhibitor, synergistically potentiates steroid production[4].
[1]. Vang AG, et al. Differential Expression and Function of PDE8 and PDE4 in Effector T cells: Implications for PDE8 as a Drug Target in Inflammation. Front Pharmacol. 2016 Aug 23;7:259. [2]. Dong H, et al. Inhibition of breast cancer cell migration by activation of cAMP signaling. Breast Cancer Res Treat. 2015 Jul;152(1):17-28. [3]. Tsai LC, et al. Regulation of adrenal steroidogenesis by the high-affinity phosphodiesterase 8 family. Horm Metab Res. 2012 Sep;44(10):790-4. [4]. Shimizu-Albergine M, et al. cAMP-specific phosphodiesterases 8A and 8B, essential regulators of Leydig cell steroidogenesis. Mol Pharmacol. 2012 Apr;81(4):556-66.
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Cell experiment: |
Breast cancer cells are in a total volume of 0.1 mL of fresh medium containing the test reagents or vehicle (PF-04957325). Following incubation at 37°C for 72 h, 20 μL of a combined solution of MTS (2 mg/mL)/PMS (0.92 mg/mL) (20:1, mixed immediately before use) is added to each well, and the plates incubated for an additional 2 h at 37°C, protected from light, following which the absorbency of the formazan product formed is determined at 492 nm using a microtiter plate reader. All reagents tested are dissolved in DMSO and diluted into the cell culture medium[2]. |
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References: [1]. Vang AG, et al. Differential Expression and Function of PDE8 and PDE4 in Effector T cells: Implications for PDE8 as a Drug Target in Inflammation. Front Pharmacol. 2016 Aug 23;7:259. |
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| Cas No. | 1305115-80-3 | SDF | |
| Canonical SMILES | NC1=C(N=NN2C[C@H]3CN(CC4=NC=CS4)CCO3)C2=NC(C(F)(F)F)=N1 | ||
| 分子式 | C14H15F3N8OS | 分子量 | 400.38 |
| 溶解度 | DMSO : 9.9 mg/mL (24.73 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 | 2.4976 mL | 12.4881 mL | 24.9763 mL |
| 5 mM | 0.4995 mL | 2.4976 mL | 4.9953 mL |
| 10 mM | 0.2498 mL | 1.2488 mL | 2.4976 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet