セスロマイシン

セスロマイシン 価格

メーカー	製品番号	製品説明	CAS番号	包装	価格	更新時間	購入

セスロマイシン 化学特性,用途語,生産方法

効能

抗生物質, タンパク質合成阻害薬

説明

Cethromycin (formerly ABT-773) is a ketolide antibiotic originally developed by Abbott in the late 1990s, but abandoned in 2002. Since 2004, Advanced Life Sciences has promoted current development of cethromycin. The ketolides are structurally derived from erythromycin A and are designed to overcome resistance to macrolides. One of the main features is the lack of the neutral sugar L-cladinose at position 3 of the erythonolide ring, which is replaced by a keto group (thus giving rise to the class name). Lack of the L-cladinose moiety results in better drug absorption and less gastric irritation through improved acid stability.

物理的性質

Cethromycin is a 6-O-ketolide, meaning that, compared with 11-Nketolides such as telithromycin, linkage with the macrolactone ring is in the 6-O-position, with an O-propylallyl linkage replacing the aminopropyl linkage of telithromycin. Cethromycin presents as a white crystalline powder. As yet, cethromycin has been used only in clinical trials and is not available for clinical use. Development is primarily directed at upper and lower respiratory tract infections.

使用

Antibacterial.

生物活性

Oral bioavailability of cethromycin has been poorly studied in humans. Animal studies report values ranging from approximately 36% to 50%. Absorption of cethromycin appears to be dose dependent with time to Cmax increasing from 0.9 to 5.1 hours with increasing dosage. Food does not appear to exert meaningful effects on the pharmacokinetics of cethromycin, but this aspect deserves additional study. In a study on the effects of drug co-administration on the pharmacokinetics of cethromycin, ranitidine was found to significantly reduce cethromycin Cmax concentrations, by 25.7%. Conversely, sucralfate had no effect on cethromycin concentrations. The degree of serum protein binding is considered to approach 90%.

作用機序

The mechanism of action is similar to macrolides and is based on interaction with the peptidyl transferase site of the 50S ribosomal subunit, thus inhibiting the translation of rRNAs and preventing the elongation step of protein synthesis. In addition, cethromycin also interferes at an earlier stage of protein synthesis by disrupting the assembling of 50S subunit precursors to block the formation of a functional 50S subunit. Ketolides in general (including cethromycin) inhibit protein synthesis by binding to the 50S ribosomal subunit, close to the peptidyl transferase site at the entrance of the ribosomal exit tunnel. The presence of a 3-keto group in place of the L-cladinose moiety, common to all ketolides, allows cethromycin to bind to the ribosomal target in the 23S rRNA domain V without causing expression of ribosomal mutations. The additional flexible side chain (in the 6-O position for cethromycin) attached to the macrocyclic ring allows binding to an additional ribosomal site. This dual binding affinity increases the binding affinity of cethromycin several-fold compared with that of erythromycin. It is probably also responsible for overcoming resistance mediated by both the ribosomal mutations (erm) and efflux pump (mef) mechanisms. This leads to an enhanced activity against S. pneumoniae, including most of the macrolide-resistant strains. Conversely, the methoxy group at position C-6 provides greater acid stability than that of other macrolides, and is related to greater gastrointestinal stability.

薬物相互作用

Ketolides and macrolides are substrates and inhibitors of the cytochrome P450 (CYP450) 3A4 system. So far, data available specifically for cethromycin are very limited and mainly exist in abstract form. It is expected that interactions are similar to other drugs that are involved in this pathway. This is exemplified by ketoconazole, a potent CYP3A4 inhibitor that caused a 5-fold increase in cethromycin AUC and a 2.5-fold increase in drug Cmax, although cethromycin’s main metabolite showed a decreased Cmax but no effect on its AUC. Similarly, rifampicin (600 mg) significantly affected the pharmacokinetics of cethromycin (300 mg), with a 95% reduction in the ketolide’s AUC and its metabolite N-desmethyl cethromycin.

セスロマイシン 上流と下流の製品情報

原材料

準備製品

セスロマイシン 生産企業

名前	電話番号	電子メール	国籍	製品カタログ	優位度
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Shanghai Acmec Biochemical Technology Co., Ltd.	+undefined18621343501	product@acmec-e.com	China	33349	58
Shaanxi Cuikang Pharmaceutical Technology Co., Ltd	+86-19164747840 +86-13119157289	13119157289@163.com	China	2971	58
Shanghai Boyle Chemical Co., Ltd.	021-50182298 021-50180596	sales@boylechem.com	China	2210	55
ShangHai Caerulum Pharma Discovery Co., Ltd.	18149758185	sales-cpd@caerulumpharma.com	China	3419	58
Fan De(Beijing) Biotechnology Co., Ltd.	15911056312	liming@bio-fount.com	China	9730	58
Nanjing Shizhou Biology Technology Co.,Ltd	025-85560043 15850508050	rose.shi@synzest.com	China	9287	58
Zhejiang Huida Biotech Co., LTD	0571-89903882 13626641628	jiangnan@huidabiotech.com	China	3661	58
Zhejiang Huida Biotech Co., LTD	0571-0571-89903882 15990081639	sunshixuan@huidabiotech.com	China	3705	58

205110-48-1(セスロマイシン)キーワード:

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• 205110-48-1
• CETHROMYCIN(ABT-773)
• 11-Amino-11-deoxy-3-oxo-5-o-desosaminyl-6-o-[1'-(3'-quinolyl-2'-propenyl)] erythronolide A 11,12-cyclic carbamate
• ABT-773
• CETHROMYCIN
• A-195773
• Abbott-195773
• 2H-Oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetrone, 4-ethyloctahydro-3a,7,9,11,13,15-hexamethyl-11-[[3-(3-quinolinyl)-2-propenyl]oxy]-10-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, (3aS,4R,7R,9R,10R,11R,13R,15R,15aR)-
• quinerythromycin
• セスロマイシン
• ABT-773
• 5-O-[3,4,6-トリデオキシ-3-(ジメチルアミノ)-β-D-xylo-ヘキソピラノシル]-6-O-[3-(キノリン-3-イル)-2-プロペニル]-3,11,12-トリデオキシ-3,23-ジオキソ-12,11-(エポキシメタノイミノ)エリスロノリドA
• セトロマイシン
• 3,11,12-トリデオキシ-3,23-ジオキソ-6-O-[3-(キノリン-3-イル)-2-プロペニル]-5-O-[3-(ジメチルアミノ)-3,4,6-トリデオキシ-β-D-xylo-ヘキソピラノシル]-12,11-(エポキシメタノイミノ)エリスロノリドA
• 11,12-(イミノカルボニルオキシ)-11,12-ジデオキシ-3-オキソ-3-デス(2,6-ジデオキシ-3-C-メチル-3-O-メチル-α-L-ribo-ヘキソピラノシルオキシ)-6-O-[3-(3-キノリル)アリル]エリスロマイシン
• (3aS,4R,7R,9R,10R,11R,13R,15R,15aR)-10-{[(2S,3R,4S,6R)-4-(ジメチルアミノ)-3-ヒドロキシ-6-メチルオキサン-2-イル]オキシ}-4-エチル-3a,7,9,11,13,15-ヘキサメチル-11-{[3-(キノリン-3-イル)プロパ-2-エン-1-イル]オキシ}-テトラデカヒドロ-1H-オキサシクロテトラデカ[4,3-d][1,3]オキサゾール-2,6,8,14-テトラオン