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Azithromycin

Azithromycin 구조식 이미지
카스 번호:
83905-01-5
상품명:
Azithromycin
동의어(영문):
Zeto;xz405;Tobil;Zifin;XZ-450;Azenil;Azimin;Aziwok;Aztrin;Setron
CBNumber:
CB1442887
분자식:
C38H72N2O12
포뮬러 무게:
748.98
MOL 파일:
83905-01-5.mol

Azithromycin 속성

녹는점
113-115°C
알파
D20 -37° (c = 1 in CHCl3)
저장 조건
Store at -20°C
용해도
Practically insoluble in water, freely soluble in anhydrous ethanol and in methylene chloride.
물리적 상태
neat
산도 계수 (pKa)
pKa 8.74 (H2O t=25 I=0.167) (Uncertain);9.45(H2O t=25 I=0.167) (Uncertain)
optical activity
[α]/D 45±2°, c = 1% in ethanol
안정성
Stable. Incompatible with strong oxidizing agents.
CAS 데이터베이스
83905-01-5(CAS DataBase Reference)
EPA
1-Oxa-6-azacyclopentadecan- 15-one, 13-[(2,6-dideoxy-3-C-methyl- 3-O-methyl-.alpha.-L-ribo- hexopyranosyl)oxy]-2-ethyl- 3,4,10-trihydroxy-3,5,6,8, 10,12,14-heptamethyl-11-[[ 3,4,6-trideoxy-3-(dimethylamino)-. beta.-D-xylo-hexopyranosyl] oxy]-, (2R,3S,4R,5R,8R,10R,11R,12S, 13S,14R)-(83905-01-5)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xi,Xn
위험 카페고리 넘버 42/43
안전지침서 22-36/37-45
WGK 독일 2
RTECS 번호 RN6960000
HS 번호 29419090
유해 물질 데이터 83905-01-5(Hazardous Substances Data)
그림문자(GHS):
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H317 알레르기성 피부 반응을 일으킬 수 있음 피부 과민성 물질 구분 1 경고 P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H334 흡입 시 알레르기성 반응, 천식 또는 호흡 곤란 등을 일으킬 수 있음 호흡기 과민성 물질 구분 1 위험 P261, P285, P304+P341, P342+P311,P501
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P284 호흡 보호구를 착용하시오.
P304+P340 흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.
P342+P311 호흡기 증상이 나타나면 의료기관(의사)의 진찰을 받으시오.

Azithromycin MSDS


Azithromycin

Azithromycin C화학적 특성, 용도, 생산

용도

항생제는 호흡기 감염과 같은 다양한 민감한 세균 감염에 사용됩니다. 피부 및 연조직 감염.

용도

아지트로마이신(azithromycin)은 수많은 병균 감염 치료에 사용되는 항생물질이다. 여기에는 중이염, 연쇄상 구균 인두염, 폐렴, 물갈이, 기타 특정 장염이 포함된다. 클라미디아, 임질 등 수많은 성병에 대해서도 사용할 수 있다.다른 약물들과 함께 사용하여 말라리아를 대상으로 사용할 수도 있다.

개요

Azithromycin is a long-acting macrolide antibiotic structurally related to erythromycin A (EA), having a methyl-substituted nitrogen at position 9a in the aglycone ring. Azithromycin is reported to be highly effective in the treatment of respiratory and urinary infections; it has the advantages of being acid-stable and requiring a shorter course of treatment than EA.

화학적 성질

White Crystalline Powder

Originator

Pliva (Yugoslavia)

용도

Labelled Azithromycin, a semi-synthetic macrolide antibiotic; related to Erythromycin A. Antibacterial.

용도

Azithromycin is a semi-synthetic, ring-expanded erythromycin, produced by a Beckmann rearrangement of erythromycin oxime and reduction to the imine ether, followed by reductive methylation. Azithromycin was the first of the azalides and was designed to improve stability and biological half-life of erythromycin A, as well as improve activity against Gram negative bacteria. Since its discovery in 1980 by Djokic and co-workers, azithromycin has enjoyed considerable therapeutic success.

용도

Cephalosporin antibiotic

용도

Azithromycin is a semi-synthetic, ring-expanded erythromycin produced by a Beckmann rearrangement of erythromycin oxime and reduction to the imine ether, followed by reductive methylation. Azithromycin was the first of the azalides and was designed to improve the stability and biological half-life of erythromycin A, as well as improve activity against Gram negative bacteria. Since its discovery in 1980 by Djokic and co-workers, azithromycin has enjoyed considerable therapeutic success.

용도

Labeled Azithromycin, Intended for use as an internal standard for the quantification of Azithromycin by GC- or LC-mass spectrometry

정의

ChEBI: A macrolide antibiotic useful for the treatment of bacterial infections.

상표명

Zithromax (Pfizer); Zmax (Pfizer);Sunamed.

Antimicrobial activity

It is less potent than erythromycin A against Gram-positive isolates, but is more active against Gram-negative bacteria. It is four times more potent than erythromycin A against H. influenzae, N. gonorrhoeae and Campylobacter spp., and twice as active against Mor. catarrhalis. It also exhibits superior potency against Enterobacteriaceae, notably Esch. coli, Salmonella enterica serotypes, and Shigella spp. It is active against Mycobacteria, notably the M. avium complex and against intracellular micro-organisms such as Legionella and Chlamydia spp.
Chemical modification at the 9 position of the erythronolide A ring of erythromycin A blocks the internal ketalization and markedly improves acid stability. At pH 2, loss of 10% activity occurred in less than 4 s with erythromycin A, but took 20 min with azithromycin. The AUC at 0–24 h is 4.5 mg.h/L. The level is only slightly increased on repeated dosing.
Binding to plasma protein varies with the concentration, from around 50% at 0.05 mg/L to 7.1% at 1 mg/L. The apparent elimination half-life is dependent upon sampling interval: between 8 and 24 h it ranged from 11 to 14 h; between 24 and 72 h it was 35–40 h.
It rapidly penetrates the tissues, reaching levels that approach or, in some cases, exceed the simultaneous plasma levels and persist for 2–3 days. Only about 6% of the dose is found in urine in the first 24 h.

일반 설명

The spectrum of antimicrobial activity of azithromycin issimilar to that observed for erythromycin and clarithromycinbut with some interesting differences. In general,it is more active against Gram-negative bacteria and less activeagainst Gram-positive bacteria than its close relatives.The greater activity of azithromycin against H. influenzae,M. catarrhalis, and M. pneumoniae coupled with its extendedhalf-life permits a 5-day dosing schedule for thetreatment of respiratory tract infections caused by thesepathogens. The clinical efficacy of azithromycin in the treatmentof urogenital and other sexually transmitted infectionscaused by Chlamydia trachomatis, N. gonorrhoeae, H.ducreyi, and Ureaplasma urealyticum suggests that singledosetherapy with it for uncomplicated urethritis or cervicitismay have advantages over use of other antibiotics.

Pharmaceutical Applications

A semisynthetic derivative of erythromycin A, supplied as the dihydrate for oral administration.

생물학적 활성

Macrolide antibiotic. Inhibits 50S ribosomal subunit formation and elongation at transpeptidation step in gram-positive and gram-negative organisms. Orally active with improved pharmacokinetics over erythromycin in mouse models.

Pharmacokinetics

Oral absorption:37%
Cmax 250 mg oral: 0.17 mg/L after 2.2 h
500 mg oral: 0.4 mg/L after2h
Plasma half-life (terminal): 11–40 h
Volume of distribution: 31 L/kg
Plasma protein binding :7–50%
Chemical modification at the 9 position of the erythronolide A ring of erythromycin A blocks the internal ketalization and markedly improves acid stability. At pH 2, loss of 10% activity occurred in less than 4 s with erythromycin A, but took 20 min with azithromycin. The AUC at 0–24 h is 4.5 mg.h/L. The level is only slightly increased on repeated dosing.
Binding to plasma protein varies with the concentration, from around 50% at 0.05 mg/L to 7.1% at 1 mg/L. The apparent elimination half-life is dependent upon sampling interval: between 8 and 24 h it ranged from 11 to 14 h: between 24 and 72 h it was 35–40 h.
It rapidly penetrates the tissues, reaching levels that approach or, in some cases, exceed the simultaneous plasma levels and persist for 2–3 days. Only about 6% of the dose is found in urine in the first 24 h.

부작용

Azithromycin is well tolerated with little gastrointestinal disturbance.

효소 저해제

This orally active erythromycin derivative (FW = 749.00 g/mol; CAS 83905-01-5; Solubility: 100 mM in DMSO), also known by the trade names Zithromax?, Azyth?, Sumamed?, is a macrolide antibiotic that targets the assembly of 50S ribosomal subunits and inhibits the transpeptidation step in many Gram-positive and Gram-negative microorganisms. Azithromycin’s large volume of distribution (23 L/kg) and peak serum level (0.4 μg/mL) indicate an extensive tissue distribution, allowing it to achieve high, bacteriocidal levels at sites of infection. It is also taken up by cells (even phagocytes), localizing mainly in cell granules and cytosol and allowing it to be effective against suchh intracellular pathogens as Listeria monocytogenes. Azithromycin is also effective against respiratory, urogenital, and dermal infections. Microbial Targets: Aerobic & Facultative Gram-positive Microorganisms: Staphylococcus aureus (including MRSA), Streptococcus agalactiae, S. pneumoniae; S. pyogenes; Aerobic & Facultative Gram-negative Microorganisms: Haemophilus influenza, Neisseria gonorrhoeae, Bordetella pertussis, Legionella pneumophila. Key Pharmacokinetic Parameters: See Appendix II in Goodman & Gilman’s THE PHARMACOLOGICAL BASIS OF THERAPEUTICS, 12th Edition (Brunton, Chabner & Knollmann, eds.) McGraw-Hill Medical, New York.

Azithromycin 준비 용품 및 원자재

원자재

준비 용품


Azithromycin 공급 업체

글로벌( 352)공급 업체
공급자 전화 팩스 이메일 국가 제품 수 이점
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 661 60
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23982 58
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3203 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21909 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20680 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32457 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2543 55
Hubei XinRunde Chemical Co., Ltd.
+8615102730682; +8618874586545
02783214688 bruce@xrdchem.cn CHINA 541 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24196 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 1771 55

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