Oxolamine
Oxolamine (SKF-9976) is an orally active antitussive. Oxolamine can inhibit CYP2B1/2. Oxolamine has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine can be used in respiratory disease research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 959-14-8
- 分子式: C14H19N3O
- 分子量:245.32
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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CYP2B1 |
CYP2B2 |
体外実験
Oxolamine (SKF-9976 citrate) 是一种具有口服活性止咳剂。Oxolamine 可以抑制 CYP2B1/2。Oxolamine 对豚鼠呼吸器官具有抗炎作用。Oxolamine 增加 Warfarin (HY-B0687) 的 AUC 并延长其终末半衰期。Oxolamine 可用于呼吸道疾病研究[1][2][3][4]。
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
Oxolamine (80 mg/kg body weight initially, then 53.3 mg/kg; i.p.; 11 times at 3, 6, 9, 24, 28, 32, 48, 52, 56, 72 and 76 h) shows a distinct anti-inflammatory action on the respiratory organs of guinea pigs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs + non-bacterial inflammation of the respiratory tract model induced by inhalation of acrolein aerosol[4]
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Dosage:80 mg/kg body weight initially, then 53.3 mg/kg
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Administration:Intraperitoneal injection, 11 times at 3, 6, 9, 24, 28, 32, 48, 52, 56, 72 and 76 h
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Result:Reduced relative lung weight.
Significantly reduced inflammation levels.
Protected the pulmonary parenchyma from emphysema.
Showed anti-inflammatory effect superior to that of Phenylbutyrone.
化学情報
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CAS 番号 959-14-8
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分子量 245.32
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分子式 C14H19N3O
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SMILES
CCN(CC)CCC1=NC(C2=CC=CC=C2)=NO1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
純度とドキュメンテーション
参考文献
[1]. Kirilmaz L, et, al. Sustained-release dosage form of oxolamine citrate: preparation and release kinetics. J Microencapsul. Apr-Jun 1992;9(2):167-72. [Content Brief]
[2]. GIUDICI G, et, al. [On the anti-inflammatory action of oxolamine citrate]. Minerva Med. 1961 Oct 31;52:3752-5. [Content Brief]
[3]. Zhu X, et al. Gender difference in the pharmacokinetic interaction between oral warfarin and oxolamine in rats: inhibition of CYP2B1 by oxolamine in male rats. Biopharm Drug Dispos. 2007 Apr;28(3):125-33. [Content Brief]
[4]. Dahlgren S, et al. The effect of oxolamine citrate on experimentally produced inflammation in the respiratory organs. Acta Pharmacol Toxicol (Copenh). 1966;24(2):286-96. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)