Tebipenem Pivoxil (L084)

製品コードS2159 バッチS215902

化学情報

	Synonyms	L-084, ME1211,TBPM-PI,LJC 11036	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₃₁N₃O₆S₂
	分子量	497.63	CAS No.	161715-24-8
Solubility (25°C)*	体外	DMSO	99 mg/mL (198.94 mM)
		Ethanol	87 mg/mL (174.82 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Tebipenem Pivoxil (L-084, ME1211,TBPM-PI,LJC 11036)は、耳鼻咽喉科および呼吸器感染症の治療に使用される経口carbapenem Antibioticsです。
in vitro	Tebipenem Pivoxil has high intestinal apical membrane permeability due to plural intestinal transport routes, including the uptake transporters such as OATP1A2 and OATP2B1 as well as simple diffusion. This compound is quickly converted to tebipenem (TBPM), an active form. It is absorbed quickly, and the bioavailability is 71.4%, 59.1%, 34.8% and 44.9%, respectively, in mouse, rat, dog and monkey. Tebipenem shows the strongest bactericidal activity as early as 2 h after exposure at two times the MIC. It shows higher affinities for PBP 1A and PBP 2B, high-molecular-weight enzymes, and for PBP 3, a low-molecular-weight enzyme, than for PBP 2X. This chemical has a potent activity against Neisseria gonorrhoeae; its activity is comparable to it of cefixime that has most potent activity among oral antibiotics.
in vivo	Tebipenem Pivoxil results in survival rate of 83%, compared with 25% survival for Amoxicillin and 0% survival for controls in animal model of otitis media. This compound exhibits slow tight-binding inhibition at low micromolar concentrations versus the chromogenic substrate nitrocefin. It acyl-enzyme complex remains stable for greater than 90 min and exists as mixture of the covalently bound drug and the bound retro-aldol cleavage product.

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/20735088/
https://pubmed.ncbi.nlm.nih.gov/19882982/
https://pubmed.ncbi.nlm.nih.gov/15728880/

https://pubmed.ncbi.nlm.nih.gov/19673353/
https://pubmed.ncbi.nlm.nih.gov/17055132/
https://pubmed.ncbi.nlm.nih.gov/24846409/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。