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RETAPAMULIN

RETAPAMULIN Struktur
224452-66-8
CAS-Nr.
224452-66-8
Englisch Name:
RETAPAMULIN
Synonyma:
CS-329;Retamole;SB-275833;Rebapamulin;RETAPAMULIN;tetapaMulin;Rui he Maureen;RetapaMulin API;Retapamulin, >=98%;RetapaMulin (SB-275833)
CBNumber:
CB32455623
Summenformel:
C30H47NO4S
Molgewicht:
517.76
MOL-Datei:
224452-66-8.mol

RETAPAMULIN Eigenschaften

Siedepunkt:
594.9±50.0 °C(Predicted)
Dichte
1.16±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
insoluble in H2O; ≥114.8 mg/mL in EtOH; ≥16.15 mg/mL in DMSO
Aggregatzustand
solid
pka
14.65±0.70(Predicted)
Farbe
White to off-white
InChIKey
STZYTFJPGGDRJD-IFPFAXJDNA-N
CAS Datenbank
224452-66-8(CAS DataBase Reference)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H412 Sch?dlich für Wasserorganismen, mit langfristiger Wirkung. Langfristig (chronisch) gew?ssergef?hrdend Kategorie 3 P273, P501
Sicherheit
P273 Freisetzung in die Umwelt vermeiden.
P501 Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

RETAPAMULIN Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Verwenden

Retapamulin is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM

Pharmazeutische Anwendungen

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.

Nebenwirkungen

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.

RETAPAMULIN Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


RETAPAMULIN Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 229)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Beijing Mediking Biopharm Co., Ltd
+undefined15901403431
sales01@mediking.cn China 150 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32957 60
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 58
Zhejiang ZETian Fine Chemicals Co. LTD
+8618957127338
stella@zetchem.com China 2136 58
Shanghai Arbor Chemical Co., Ltd.
021-60451682
act@arborchemical.com CHINA 904 58
Xiamen AmoyChem Co., Ltd
+86-86-5926051114 +8618959220845
sales@amoychem.com China 6383 58
Changzhou Ditong Chemical Co.,Ltd
+86-0519-88299272
info@edengenechem.com China 2158 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58

224452-66-8()Verwandte Suche:


  • 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
  • 224452-66-8
  • 924452-66-8
  • 22452-66-8
  • C30H47NO4S
  • C30H46NO4S
  • Inhibitors
  • API, Antibiotics
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