Description
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 . PPM-18 inhibited NF-κB activation with an IC50 of 5 μM . 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 .
Product information
CAS Number: 65240-86-0
Molecular Weight: 277.27
Formula: C17H11NO3
Chemical Name: N-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzamide
Smiles: O=C1C=C(NC(=O)C2C=CC=CC=2)C(=O)C2=CC=CC=C12
InChiKey: BIVQBWSIGJFXLF-UHFFFAOYSA-N
InChi: InChI=1S/C17H11NO3/c19-15-10-14(16(20)13-9-5-4-8-12(13)15)18-17(21)11-6-2-1-3-7-11/h1-10H,(H,18,21)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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