Niclosamide

Niclosamide 구조식 이미지
카스 번호:
50-65-7
상품명:
Niclosamide
동의어(영문):
NICLOSAMID;YOMESAN;niclocide;tredemine;bayluscid;NICLOSAMIDE (BAY2353);5-CHLORO-N-(2-CHLORO-4-NITROPHENYL)-2-HYDROXYBENZAMIDE;mato;b2353;hl2447
CBNumber:
CB6147451
분자식:
C13H8Cl2N2O4
포뮬러 무게:
327.12
MOL 파일:
50-65-7.mol
MSDS 파일:
SDS

Niclosamide 속성

녹는점
225-230°
끓는 점
424.5±45.0 °C(Predicted)
밀도
1.6646 (rough estimate)
굴절률
1.6200 (estimate)
저장 조건
Sealed in dry,Room Temperature
용해도
아세톤:메탄올:용해성50mg/mL(메탄올:아세톤(1:1))
물리적 상태
담황색 고체
산도 계수 (pKa)
7.45±0.43(Predicted)
색상
노란색
수용성
13.32mg/L(25 ºC)
BRN
2820605
BCS Class
4
안정성
제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°에서 최대 3개월 동안 보관할 수 있습니다.
InChIKey
RJMUSRYZPJIFPJ-UHFFFAOYSA-N
CAS 데이터베이스
50-65-7(CAS DataBase Reference)
EPA
Niclosamide (50-65-7)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험 카페고리 넘버 50
안전지침서 29
유엔번호(UN No.) UN 3077 9/PG 3
WGK 독일 2
RTECS 번호 VN8400000
HS 번호 29242990
유해 물질 데이터 50-65-7(Hazardous Substances Data)
독성 LD50 oral in rat: 2500mg/kg
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H400 수생생물에 매우 유독함 수생 환경유해성 물질 - 급성 구분 1 경고 GHS hazard pictograms P273, P391, P501
예방조치문구:
P273 환경으로 배출하지 마시오.
P391 누출물을 모으시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

Niclosamide MSDS


Niclosamide

Niclosamide C화학적 특성, 용도, 생산

화학적 성질

Yellowish-white or yellowish, fine crystals.Yellow-white crystalline powder, odorless, tasteless. Melting point 225-230 ℃. Insoluble in water, soluble in hot ethanol, chloroform, cyclohexanone, diethyl ether and sodium hydroxide solution.

용도

Niclosamide has been used extensively in the treatment of tapeworm infections caused by Taenia saginata, Taenia solium, Diphyllobothrium latum, Fasciolopsis buski, and Hymenolepis nana. It is an effective alternative to praziquantel for treating infections caused by T. saginata (beef tapeworm), T. solium (pork tapeworm), and D. latum (fish tapeworm) and is active against most other tapeworm infections. It is absorbed by intestinal cestodes but not nematodes.A single dose is usually adequate to produce a cure rate of 95%.With H. nana (dwarf tapeworm), a longer treatment course (up to 7 days) is necessary. Niclosamide is administered orally after the patient has fasted overnight and may be followed in 2 hours by purging (magnesium sulfate 15–30 g) to encourage complete expulsion of the cestode, especially T. solium, although this is not always considered necessary. Cure is assessed by follow-up stool examination in 3 to 5 months.With the availability of other agents, niclosamide is no longer widely used.The most widely employed agents are praziquantel and the benzimidazoles.

Antimicrobial activity

Useful activity is restricted to intestinal tapeworms, including Taeniarhynchus saginatus (syn. Taenia saginata), Taenia solium, Diphyllobothrium latum and Hymenolepis nana. It is not effective against larval stages of tapeworms.

일반 설명

A cell-permeable salicylanilide that, in addition to its well-known antihelmintic efficacy, acts as a mammalian mTORC1, but not mTORC2, signaling inhibitor mechanistically distinct from rapamycin. Likely a direct consequence of autophagy activation, Niclosamide is demonstrated to induce Wnt-independent Frizzled1 and Dishevelled-2 downregulation. Unrelated to its autophagy induction activity, Niclosamide is also shown to inhibit Stat3 signaling (IC50 = 0.25 M in HeLa reporter assays). Efficiently inhibits breast cancer stem-like cells in vitro and in vivo.

Pharmaceutical Applications

A synthetic chlorinated nitrosalicylanilide available for oral administration.

Mechanism of action

For many years, niclosamide (Niclocide) was widely used to treat infestations of cestodes. Niclosamide is a chlorinated salicylamide that inhibits the production of energy derived from anaerobic metabolism. It may also have adenosine triphosphatase (ATPase) stimulating properties. Inhibition of anaerobic incorporation of inorganic phosphate into ATP is detrimental to the parasite. Niclosamide can uncouple oxidative phosphorylation in mammalian mitochondria, but this action requires dosages that are higher than those commonly used in treating worm infections.
The drug affects the scolex and proximal segments of the cestodes, resulting in detachment of the scolex from the intestinal wall and eventual evacuation of the cestodes from the intestine by the normal peristaltic action of the host's bowel. Because niclosamide is not absorbed from the intestinal tract, high concentrations can be achieved in the intestinal lumen.The drug is not ovicidal.

Pharmacokinetics

Conflicting data exist relative to the level of absorption of niclosamide from the gut. The metabolized drug is passed in the feces and urine, staining them yellow.

Clinical Use

5-Chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamideor 2,5 -dichloro-4 -nitrosalicylanilide (Cestocide, Mansonil,Yomesan) occurs as a yellowish white, water-insolublepowder. It is a potent taeniacide that causes rapid disintegrationof worm segments and the scolex. Penetration of thedrug into various cestodes appears to be facilitated by thedigestive juices of the host, in that very little of the drug isabsorbed by the worms in vitro. Niclosamide is well toleratedfollowing oral administration, and little or no systemicabsorption of it occurs. A saline purge 1 to 2 hours after ingestion of the taeniacide is recommended to remove thedamaged scolex and worm segments. This procedure ismandatory in the treatment of pork tapeworm infestation toprevent possible cysticercosis resulting from release of liveova from worm segments damaged by the drug.

부작용

No serious side effects are associated with niclosamide use, although some patients report abdominal discomfort and loose stools.

Safety Profile

Poison by intravenous and intraperitoneal routes. Moderately toxic by ingestion. Experimental reproductive effects. Human mutation data reported. When heated to decomposition it emits very toxic fumes of Cl and NOx.

Niclosamide 준비 용품 및 원자재

원자재

준비 용품


Niclosamide 공급 업체

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