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LF163892 MONOHYDRATE

LF163892 MONOHYDRATE Struktur
76470-66-1
CAS-Nr.
76470-66-1
Englisch Name:
LF163892 MONOHYDRATE
Synonyma:
Lorabid;LOEACARBEF;LORACARBEF;LF163892 MONOHYDRATE;LORACARBEF MONOHYDRATE;LF163892 MONOHYDRATE USP/EP/BP;3-Chloro-7β-[[(R)-aminophenylacetyl]amino]-1-carbacepham-3-ene-4-carboxylic acid;(6R)-7α-[[(R)-Aminophenylacetyl]amino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;(6R,6β)-7α-[[(R)-Aminophenylacetyl]amino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;(6R,7S)-7-[[(2R)-2-AMino-2-phenylacetyl]aMino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic Acid
CBNumber:
CB7330045
Summenformel:
C16H16ClN3O4
Molgewicht:
349.77
MOL-Datei:
76470-66-1.mol

LF163892 MONOHYDRATE Eigenschaften

Schmelzpunkt:
>196°C (dec.)
Siedepunkt:
662.2±55.0 °C(Predicted)
Dichte
1.52±0.1 g/cm3(Predicted)
storage temp. 
-20°C Freezer, Under inert atmosphere
L?slichkeit
Aqueous Acid (slightly)
pka
3.10±0.40(Predicted)
Aggregatzustand
Solid
Farbe
White to Off-White
BCS Class
2

Sicherheit

LF163892 MONOHYDRATE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Loracarbef is a synthetic C-5 “carba” analogue of cefaclor. The smaller methylene moiety (as compared to sulfur) would be expected to make loracarbef more reactive/potent, and this seems to be the case. It is more stable chemically, however, and this adds to its virtues.

Verwenden

An antibiotic, a synthetic carbacephem analogue of cefaclor, and is more stable chemically.

Definition

ChEBI: A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.

Antimicrobial activity

An oral carbacephem, with carbon replacing sulfur in the fused ring structure. Its structure and properties are otherwise closely related to those of cefaclor, but it has improved chemical stability. Activity and stability to β-lactamases correspond closely to those of cefaclor.
It is almost completely absorbed by the oral route, but food delays absorption. A 500 mg oral dose achieves a serum concentration of around 16 mg/L after 1.3 h. Adequate concentrations are achieved for the treatment of upper respiratory tract infection. Sputum concentrations have been found to be around 2% of the corresponding plasma level. The plasma half-life is about 1 h and protein binding is 25%. Most of the dose is excreted unchanged in the urine, 60% within 12 h. The elimination half-life is increased in patients with impaired renal function. Probenecid delays excretion.
Diarrhea is the most prominent side effect, occurring in about 4% of patients. Other gastrointestinal upsets are also reported. It has been used for the oral treatment of upper respiratory tract infection, skin and soft-tissue infections, and uncomplicated urinary tract infection caused by sensitive organisms, but is not widely available.

Clinical Use

Loracarbef (Lorabid) is the first of a series of carbacephemsprepared by total synthesis to be introduced. Carbacephemsare isosteres of the cephalosporin (or △ 3-cephem) antibioticsin which the 1-sulfur atom has been replaced by a methylene(CH2) group. Loracarbef is isosteric with cefaclor and hassimilar pharmacokinetic and microbiological properties.Thus, the antibacterial spectrum of activity resembles thatof cefaclor, but it has somewhat greater potency againstH. influenzae and M. catarrhalis, including β-lactamase–producing strains. Unlike cefaclor, which undergoes degradationin human serum, loracarbef is chemically stable inplasma. It is absorbed well orally. Oral absorption is delayedby food. The half-life in plasma is about 1 hour.

Nebenwirkungen

Diarrhea is the most common adverse effect with loracarbef and, along with certain other adverse effects, is seen more frequently with children, so this lessens enthusiasm for the drug in patients younger than 12 years.

LF163892 MONOHYDRATE Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


LF163892 MONOHYDRATE Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 35)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
career henan chemical co
+86-0371-86658258 +8613203830695
factory@coreychem.com China 29811 58
Shaanxi Dideu Medichem Co. Ltd
+86-029-89586680 +86-18192503167
1026@dideu.com China 7724 58
AFINE CHEMICALS LIMITED
+86-0571-85134551
sales@afinechem.com China 15352 58
Hangzhou MolCore BioPharmatech Co.,Ltd.
+86-057181025280; +8617767106207
sales@molcore.com China 49734 58
Shaanxi Xianhe Biotech Co., Ltd
+8617709210191
Jerry@xhobio.com China 882 58
Guangzhou PI PI Biotech Inc 020-81716320 +86-13602409664
Sales@pipitech.com China 3633 55
LGM Pharma 1-(800)-881-8210
inquiries@lgmpharma.com United States 2123 70
Chemsky (shanghai) International Co.,Ltd 021-50135380
shchemsky@sina.com China 15402 60
BOC Sciences 1-631-485-4226; 16314854226
info@bocsci.com United States 14055 65
Beijing HuaMeiHuLiBiological Chemical 010-56205725
waley188@sohu.com China 12335 58

  • LORACARBEF MONOHYDRATE
  • LOEACARBEF
  • (6R)-7α-[[(R)-Aminophenylacetyl]amino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
  • (6R,6β)-7α-[[(R)-Aminophenylacetyl]amino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
  • 3-Chloro-7β-[[(R)-aminophenylacetyl]amino]-1-carbacepham-3-ene-4-carboxylic acid
  • (6R,7S)-7-[[(2R)-2-AMino-2-phenylacetyl]aMino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic Acid
  • Lorabid
  • 1-Azabicyclo[4.2.0]oct-2-ene-2-carboxylicacid, 7-[[(2R)-2-aMino-2-phenylacetyl]aMino]-3-chloro-8-oxo-, (6R,7S)-
  • LF163892 MONOHYDRATE
  • LORACARBEF
  • (6R,7S)-7-{[(2R)-2-Ammonio-2-phenylacetyl]amino}-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate, monohydrate
  • LF163892 MONOHYDRATE USP/EP/BP
  • 76470-66-1
  • Amines
  • Drug Analogues
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
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