PPM-18 (Synonyms: NSC 73233) |
Katalog-Nr.GC16657
One-Click Copy Product Info
|
NF-κB inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 65240-86-0
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Überlieferungen | NSC 73233 | ||
| Chemical Name | N-(1,4-dihydro-1,4-dioxo-2-naphthalenyl)-benzamide | ||
| Canonical SMILES | O=C(NC1=CC(=O)c2ccccc2C1=O)c1ccccc1 | ||
| Formula | C17H11NO3 | M.Wt | 277.3 |
| Löslichkeit | ≥ 27.7mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6062 mL | 18.031 mL | 36.062 mL |
| 5 mM | 721.2 μL | 3.6062 mL | 7.2124 mL |
| 10 mM | 360.6 μL | 1.8031 mL | 3.6062 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)