Cefatrizine

Cefatrizine 구조식 이미지
카스 번호:
51627-14-6
상품명:
Cefatrizine
동의어(영문):
s640p;bls640;SKF-60771;eta(r)))-;CEFATRIZINE;cephatriazine;Cephathiamidine;antibioticbl-640;CEPHATHIAMIDINUM;antibioticbl-s640
CBNumber:
CB3116636
분자식:
C18H18N6O5S2
포뮬러 무게:
462.5
MOL 파일:
51627-14-6.mol

Cefatrizine 속성

끓는 점
948.1±65.0 °C(Predicted)
밀도
1.3806 (rough estimate)
굴절률
1.7000 (estimate)
저장 조건
Store at -20°C
용해도
DMSO: 95 mg/mL (201.02 mM);Ethanol: 23 mg/mL (48.67 mM)
산도 계수 (pKa)
2?+-.0.50(Predicted)
수용성
Water: 95 mg/mL (201.02 mM)
CAS 데이터베이스
51627-14-6(CAS DataBase Reference)

안전

독성 LD50 in male, female mice, male, female rats (mg/kg): 6880, 6410, 4325, 4325 i.p. (Matsuzaki)

Cefatrizine C화학적 특성, 용도, 생산

개요

Cefatrizine was synthesized by BristolMyers Co. and Smith Klein & French Laboratories in 1974. It shows two to four times higher activity against gram-positive and four to eight times higher activity against gram-negative bacteria than cephalexin. Cefatrizine also shows excellent oral absorption, and its in vivo activity is 30 to 500 times higher than that of cephalexin.

용도

Cefatrizine is a new orally administered cephalosporin with excellent activity against gram-positive cocci, inhibiting all except enterococci at minimal inhibitory concentrations below 1 μg/ml.

정의

ChEBI: A cephalosporin compound having (1H-1,2,3-triazol-4-ylsulfanyl)methyl and [(2R)-2-amino-2-(4-hydroxyphenyl)]acetamido side-groups. An antibacterial drug first prepared in the 1970s, it has more recently been found to be n inhibitor of eukaryotic elongation factor-2 kinase (eEF2K), which is known to regulate apoptosis, autophagy and ER stress in many types of human cancers.

Antimicrobial activity

A semisynthetic cephalosporin formulated for oral use. The spectrum is similar to that of cefalexin but it is more active against H. influenzae. Wide strain variations in susceptibility have been reported.
It is only partially absorbed when given by mouth. A 500 mg oral dose achieves a concentration of c. 6 mg/L after 1–2 h. The normal half-life of 2.5 h is extended to 5.5 h in end-stage renal failure. Distribution resembles that of cefalexin. It crosses the placenta readily. Plasma protein binding is 40–60%.
Urinary recovery in 6 h is 35% of an oral dose, producing urinary levels of 50–1500 mg/L. It is presumed that the remainder is metabolized, but no metabolites have been identified.
Apart from some mild diarrhea, it is well tolerated. It is available in Japan.

Safety Profile

Moderately toxic byintraperitoneal and subcutaneous routes. An experimentalteratogen. Other experimental reproductive effects. Whenheated to decomposition it emits very highly toxic fumesof NOx and SOx.

Cefatrizine 준비 용품 및 원자재

원자재

준비 용품


Cefatrizine 공급 업체

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