レタパムリン
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- CAS番号.
- 224452-66-8
- 化学名:
- レタパムリン
- 别名:
- レタパムリン;[[(1R,5S)-8-メチル-8-アザビシクロ[3.2.1]オクタン-3β-イル]チオ]酢酸(3aS,4R,5S,6S,8R,9R,9aR,10R)-6-エテニルデカヒドロ-5-ヒドロキシ-4,6,9,10-テトラメチル-1-オキソ-3a,9-プロパノ-3aH-シクロペンタシクロオクテン-8-イル;(1S,2R,3S,4S,6R,7R,8R,14R)-4-エテニル-3-ヒドロキシ-2,4,7,14-テトラメチル-9-オキソトリシクロ[5.4.3.01,8]テトラデカン-6-イル 2-{[(1R,5S)-8-メチル-8-アザビシクロ[3.2.1]オクタン-3-イル]スルファニル}アセタート
- 英語名:
- RETAPAMULIN
- 英語别名:
- CS-329;Retamole;SB-275833;Rebapamulin;RETAPAMULIN;tetapaMulin;Rui he Maureen;RetapaMulin API;Retapamulin, >=98%;RetapaMulin (SB-275833)
- CBNumber:
- CB32455623
- 化学式:
- C30H47NO4S
- 分子量:
- 517.76
- MOL File:
- 224452-66-8.mol
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レタパムリン 物理性質
- 沸点 :
- 594.9±50.0 °C(Predicted)
- 比重(密度) :
- 1.16±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- 2-8°C
- 溶解性:
- insoluble in H2O; ≥114.8 mg/mL in EtOH; ≥16.15 mg/mL in DMSO
- 外見 :
- solid
- 酸解離定数(Pka):
- 14.65±0.70(Predicted)
- 色:
- White to off-white
- InChIKey:
- STZYTFJPGGDRJD-IFPFAXJDNA-N
- CAS データベース:
- 224452-66-8(CAS DataBase Reference)
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
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| 注意喚起語 |
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| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H412 |
長期的影響により水生生物に有害 |
水生環境有害性、慢性毒性 |
3 |
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P273, P501 |
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| 注意書き |
| P273 |
環境への放出を避けること。 |
| P501 |
内容物/容器を．．．に廃棄すること。 |
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| 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 |
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富士フイルム和光純薬株式会社(wako)
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W01COBQB-7392 |
レタパムリン
Retapamulin |
224452-66-8 |
1g |
￥42500 |
2024-03-01 |
購入 |
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富士フイルム和光純薬株式会社(wako)
|
W01COBQB-7392 |
レタパムリン
Retapamulin |
224452-66-8 |
250mg |
￥34200 |
2021-03-23 |
購入 |
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富士フイルム和光純薬株式会社(wako)
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W01COBQB-7392 |
レタパムリン
Retapamulin |
224452-66-8 |
5g |
￥135000 |
2024-03-01 |
購入 |
レタパムリン 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
Antibacterial retapamulin is a derivative of the natural
product pleuromutilin and was developed by Glaxo and approved
in the US in 2007 for the treatment of skin infections. It has a unique mechanism of action, inhibiting bacterial
protein synthesis by inhibiting the larger subunit of the ribosome,
and thus has no cross resistance to other antibacterial
agents.
Pleuromutilin is a tricyclic diterpenoid that was first isolated in 1951 from the edible mushroom Pleurotus mutilus. The first semisynthetic analogs tiamulin and valnemulin, developed for veterinary use, have been shown to interact uniquely with bacterial ribosomes by high affinity binding to a site on the 50S subunit. Binding to this site interferes with ribosomal peptidyl transferase activity, blocks P-site interactions, and prevents the evolution of active 50S ribosomal subunits. Retapamulin, the first pleuromutilin approved for human use, behaves similarly to selectively inhibit bacterial protein synthesis. This novel mechanism of action has been implicated in the lack of in vitro target-specific cross-resistance with other classes of antibiotics.
使用
Retapamulin is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM
応用例（製薬）
A semisynthetic pleuromutilin formulated as a 1% ointment
for topical use. It is active against staphylococci
(MIC 0.12 mg/L), including methicillin-resistant strains, and
against streptococci (MIC 0.03–0.25 mg/L), including Str.
pyogenes and Str. pneumoniae. Most enterococci and Gramnegative
bacilli are resistant. Propionibacteria are susceptible,
suggesting that it might be useful in acne. Early indications
suggest that resistance does not emerge readily, but experience
with veterinary pleuromutilins indicates that chromosomal
resistance may develop with extended use.
It is metabolized in the liver and rapidly excreted, precluding
use in systemic infection. Systemic exposure is said to be
low following topical application and it appears safe, but there
are few data on absorption through broken and unbroken skin.
Principal side effects noted include local irritation and occasional
allergic reactions. Licensed use is presently restricted to
the treatment of impetigo and uncomplicated skin infections.
Possible value in methicillin-resistant Staph. aureus (MRSA)
infection or carriage has not yet been established.
副作用
The most frequent adverse event was application site irritation, but other side effects, occurring in o2% of patients, included headache, diarrhea, nausea, and nasopharyngitis. While there are no contraindications, it is recommended that pregnant women only use retapamulin when the potential benefits outweigh the potential risks since animal reproductive studies are not always predictive of human response. Likewise, nursing mothers are cautioned about the unknown possibility of retapamulin excretion in breast milk.
レタパムリン 上流と下流の製品情報
原材料
8-Azabicyclo[3.2.1]octane-3-thiol, 8-Methyl-, (3-exo)-
2-[(Methylsulfonyl)oxy]acetic acid (3aS,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester
Tropine-3-mesylate
チアムリン関連化合物A (TOSYL PLEUROMUTIトシルプレウロムチリン
トロピン
準備製品
レタパムリン 生産企業
Global( 225)Suppliers
224452-66-8(レタパムリン)キーワード:
- 224452-66-8
- RETAPAMULIN
- RetapaMulin (SB-275833)
- (3aS,4R,5S,6S,8R,9R,9aR,10R)-2-(exo-8-Methyl-8-azabicyclo[3.2.1]octan-3-ylsulfanyl)acetic acid 5-hydroxy-4,6,9,10-tetraMethyl-1-oxo-6-vinylperhydro-3a,9-propanocyclopentacycloocten-8-yl ester
- RetapaMulin API
- tetapaMulin
- (1S,2R,3S,4S,6R,7R,8R,14R)-4-ethenyl-3-hydroxy-2,4,7,14-tetraMethyl-9-oxotricyclo[5.4.3.0^{1,8}]tetradecan-6-yl 2-{[(1R,3S,5S)-8-Methyl-8-azabicyclo[3.2.1]octan-3-yl]sulfanyl}acetate
- Rebapamulin
- SB-275833
- Acetic acid, 2-[[(3-exo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]thio]-, (3aS,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester
- Retapamulin, >=98%
- Retamole
- CS-329
- RetapamulinQ: What is
Retapamulin Q: What is the CAS Number of
Retapamulin Q: What is the storage condition of
Retapamulin Q: What are the applications of
Retapamulin
- Rui he Maureen
- 3-(2,5-dioxopyrrolidin-7-yl)propanoicacid
- N-Boc-piperidine-5-carbaldehyde
- Acetonitrile,2,3'-(nitrosoimino)bis-
- (3aR,4R,5R,7S,8S,9R,9aS,12R)-8-Hydroxy-4,7,9,12-tetramethyl-5-((3-(((3-exo)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl)thio)prop-1-en-2-yl)oxy)-7-vinyloctahydro-4,9a-propanocyclopenta[8]annulen-3(3aH)-one
- レタパムリン
- [[(1R,5S)-8-メチル-8-アザビシクロ[3.2.1]オクタン-3β-イル]チオ]酢酸(3aS,4R,5S,6S,8R,9R,9aR,10R)-6-エテニルデカヒドロ-5-ヒドロキシ-4,6,9,10-テトラメチル-1-オキソ-3a,9-プロパノ-3aH-シクロペンタシクロオクテン-8-イル
- (1S,2R,3S,4S,6R,7R,8R,14R)-4-エテニル-3-ヒドロキシ-2,4,7,14-テトラメチル-9-オキソトリシクロ[5.4.3.01,8]テトラデカン-6-イル 2-{[(1R,5S)-8-メチル-8-アザビシクロ[3.2.1]オクタン-3-イル]スルファニル}アセタート