PD 169316
(Synonyms: 4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶) 目录号 : GC17737
A specific p38 MAPK inhibitor
Cas No.:152121-53-4
Sample solution is provided at 25 µL, 10mM.
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IC50: A potent, selective and cell-permeable suppressor of p38 MAP kinase, with the IC50 value of 89 nM.
PD169316, a specific p38 MAPK inhibitor, blocks signal transduction mediated by both TGF-β and Activin A, but not bone morphogenetic protein (BMP) 4. Suppression on TGF-β signaling in a dose-dependent manner may then reduce Smad2 and Smad3 phosphorylation, block nuclear translocation and increase the expression of TGF-β target gene. [1]
In vitro: It was reported that pretreatment of CaOV3 cells with 10 M PD169316 caused a significant decrease in Smad2 and Smad3 phosphorylation which was mediated by TGF-β. The inhibitory effect of PD 169316 was proved to act in a dose-dependent manner. Study also demonstrated that PD169316 at 5 M or higher dose directly suppressed TGF-β signaling activity. [1]
In vivo: Based on an amyloid β (Aβ) rat model of Alzheimer's disease, the effect of PD 169316 on apoptosis induced by amyloid beta was examined. It was demonstrated that caspase-3 and Bax/Bcl-2 ratio, two marks of apoptosis, were significantly decreased in the rats pre-treated with PD169316 intracerebroventricularly. This study suggested the potential neuroprotective role of PD 169316 against the neuronal toxicity induced by Aβ. [2]
Clinical trial: So far, no clinical trial has been conducted.
References:
[1]Fu YX, O’Connor LM, Shepherd TG and Nachtigal MW. The p38 MAPK inhibitor, PD169316, inhibits transforming growth factor β-induced Smad signaling in human ovarian cancer cells. Biochem Bioph Res Co. 2003. 310: 3917.
[2]Ashabi G, Alamdary SZ, Ramin M and Khodagholi F. Reduction of hippocampal apoptosis by intracerebroventricular administration of extracellular signal-regulated protein kinase and/or P38 inhibitors in amyloid beta rat model of Alzheimer’s disease: involvement of nuclear-related factor-2 and nuclear factor-κb. Basic Clin. Pharmacol. Toxicol. 2013 Aug. 112: 145–55.
| Cas No. | 152121-53-4 | SDF | |
| 别名 | 4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶 | ||
| 化学名 | 4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine | ||
| Canonical SMILES | C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)[N+](=O)[O-] | ||
| 分子式 | C20H13FN4O2 | 分子量 | 360.34 |
| 溶解度 | ≥ 15.3mg/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 | 2.7752 mL | 13.8758 mL | 27.7516 mL |
| 5 mM | 0.555 mL | 2.7752 mL | 5.5503 mL |
| 10 mM | 0.2775 mL | 1.3876 mL | 2.7752 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet