설파독신

설파독신
설파독신 구조식 이미지
카스 번호:
2447-57-6
한글명:
설파독신
동의어(한글):
설파독신
상품명:
Sulfadoxine
동의어(영문):
sulphadoxine;4-AMINO-N-(5,6-DIMETHOXY-4-PYRIMIDINYL)BENZENESULFONAMIDE;SULFADOXIN;Sulfadimoxine;Sulfadumoxine;4-sulfanilamido-5,6-dimethoxypyrimidine;fanzil;wr4873;fanasil;ro4-4393
CBNumber:
CB8171942
분자식:
C12H14N4O4S
포뮬러 무게:
310.33
MOL 파일:
2447-57-6.mol
MSDS 파일:
SDS

설파독신 속성

녹는점
190-194°C
끓는 점
298°C (rough estimate)
밀도
1.4006 (rough estimate)
굴절률
1.6270 (estimate)
저장 조건
Keep in dark place,Inert atmosphere,Room temperature
용해도
에탄올에 용해됩니다. 수산화암모늄(9:1) 20mg/ml
물리적 상태
가루
산도 계수 (pKa)
6.16±0.50(Predicted)
색상
하얀색
수용성
209.8mg/L(온도 미표시)
Merck
14,8906
BRN
625453
BCS Class
3/1
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xi
위험 카페고리 넘버 36/37/38
안전지침서 26
WGK 독일 2
RTECS 번호 DA9500000
HS 번호 29350090
독성 LD50 in mice (microcrystals, mg/kg): 5200 orally, 2900 s.c., 2900 i.p. (Bhni)
그림문자(GHS): GHS hazard pictogramsGHS hazard pictograms
신호 어: Warning
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 GHS hazard pictograms P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H411 장기적 영향에 의해 수생생물에 유독함 수생 환경유해성 물질 - 만성 구분 2
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P272 작업장 밖으로 오염된 의복을 반출하지 마시오.
P273 환경으로 배출하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P302+P352 피부에 묻으면 다량의 물로 씻으시오.
P333+P313 피부자극성 또는 홍반이 나타나면 의학적인 조치·조언를 구하시오.
NFPA 704
0
2 0

설파독신 MSDS


Sulformethoxine

설파독신 C화학적 특성, 용도, 생산

개요

Sulfadoxin is a sulfonamide antibiotic that inhibits dihydropteroate synthetase (DHPS), an enzyme involved in folic acid synthesis. Sulfadoxin competes with 4-aminobenzoate (PABA), the native substrate of DHPS, and inhibits PABA incorporation into folic acid. Folate is essential for purine and pyrimidine synthesis, therefore, sulfadoxin has antiproliferative activity in non-resistant P. falciparum. Sulfadoxin inhibits growth of P. falciparum in vitro, but potency varies between non-resistant (IC50 = 4 ng/ml) and resistant strains (IC50 = 3,970 ng/ml).

화학적 성질

White Crystalline Solid

정의

ChEBI: A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.

Antimicrobial activity

Its antibacterial activity is relatively poor. Used alone it has a slow and uncertain effect against malaria parasites. Resistance of malaria parasites to the combination with pyrimethamine is common in many endemic areas.

Pharmaceutical Applications

An ultra-long-acting sulfonamide. It is no longer prescribed alone, but is used in combination with pyrimethamine as the antimalarial agent Fansidar. It is poorly soluble in water.

Pharmacology

In terms of antibacterial action, this drug is analogous to other sulfanilamides; however, it possesses very prolonged action. Its half-life is from 120 to 200 h. Sulfadoxine is used for infectious diseases caused by microorganisms that are sensitive to the sulfanilamide drugs, such as infections of respiratory organs, gastric and urinary tracts; purulent infections of various localization, osteomyelitis, sinusitis, and other infections. It is used in combination with antimalarial drugs. Synonyms of this drug are sulfarmethoxine, fanasil, and fansidar.

Pharmacokinetics

Oral absorption :Extensive
Cmax 500 mg oral: c. 60 mg/L after 3–4 h
Plasma half-life:c.6 days
Volume of distribution:0.13 L/kg
Plasma protein binding:94%
The extremely long half-life allows administration at weekly intervals. The acetyl metabolite has a similarly long half-life, but sulfadoxine is less extensively metabolized than many other sulfonamides.

Clinical Use

Sulfadoxine is used only in combination with pyrimethamine.

부작용

Side effects are those common to the group. There have been many reports of Stevens–Johnson syndrome following its use and the combination with pyrimethamine is no longer recommended for the prophylaxis of malaria.

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