PPM-18
(Synonyms: NSC 73233) 目录号 : GC16657
Inhibits activation of NF-κB
Cas No.:65240-86-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PPM-18 is a chemically synthesized naphthoquinone derivative and an anti-inflammatory agent that inhibits the expression of inducible NO synthase (iNOS). NOS catalyzes the oxidation of the amino acid L-arginine to form NO. As an important cellular signaling molecule, NO has been implicated in modulating vascular tone, airway tone, insulinsecretion, and peristalsis. It has also been shown that NO is involved in angiogenesis and neural development and can function as a retrograde neurotransmitter
In vitro: Pretreatment of rat alveolar macrophages with PPM-18 (0.1-10 μM) significantly inhibited nitrite production, iNOS mRNA accumulation and iNOS protein expression. PPM-18 did not affect the enzymic activities of iNOS and other constitutive NOS forms directly. PPM-18 (10 μM) inhibited the LPS-induced increase in nuclear transcription factor κB (NF-κB) p65 and p50 in nucleus.. PPM-18 significantly decreased LPS-induced the production of tumour necrosis factor α [1]. PPM-18 inhibited NF-κB activation with an IC50 of 5 μM [3].
In vivo: In rats, intravenously pretreatment with PPM-18 (15 mg/kg) maintained a significantly higher mean arterial pressure compared with LPS-treated controls. PPM-18 protected mice against LPS-induced lethal toxicity. In mice, PPM-18 (5 or 15 mg/kg) dose-dependently decreased the lethality. In the mouse model of sepsis, PPM-18 exhibited as a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter and exerted a beneficial effect [1].
References:
[1] YU M S, LIN J F W U T L, KUO C S. Inhibition of nitric oxide synthase expression by PPM-18, a novel anti-inflammatory agent, in vitro and in vivo[J]. Biochemical Journal, 1997, 328(2): 363-369.
[2] Beck K F, Eberhardt W, Frank S, et al. Inducible NO synthase: role in cellular signalling[J]. Journal of Experimental Biology, 1999, 202(6): 645-653.
[3] Davis, M. E.,Grumbach, I.M.,Fukai, T., et al. Shear stress regulates endothelial nitric-oxide synthase promoter activity through nuclear factor κB binding.The Journal of Biological Chemisty 279(1), 163-168 (2004).
| Cas No. | 65240-86-0 | SDF | |
| 别名 | NSC 73233 | ||
| 化学名 | N-(1,4-dihydro-1,4-dioxo-2-naphthalenyl)-benzamide | ||
| Canonical SMILES | O=C(NC1=CC(=O)c2ccccc2C1=O)c1ccccc1 | ||
| 分子式 | C17H11NO3 | 分子量 | 277.3 |
| 溶解度 | ≥ 27.7mg/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 | 3.6062 mL | 18.031 mL | 36.062 mL |
| 5 mM | 0.7212 mL | 3.6062 mL | 7.2124 mL |
| 10 mM | 0.3606 mL | 1.8031 mL | 3.6062 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。