엠트리시타빈

엠트리시타빈
엠트리시타빈 구조식 이미지
카스 번호:
143491-57-0
한글명:
엠트리시타빈
동의어(한글):
엠트리시타빈
상품명:
Emtricitabine
동의어(영문):
FUMITREMORGIN C;EMTRICITABIN;EMtriva;FTC;EMTRITABINE;SM-Q;BW1592;CS-895;BW 1592;BW-1592
CBNumber:
CB5266199
분자식:
C8H10FN3O3S
포뮬러 무게:
247.25
MOL 파일:
143491-57-0.mol
MSDS 파일:
SDS

엠트리시타빈 속성

녹는점
136-140°C
알파
D25 -133.60° (c = 0.23 in MeOH)
끓는 점
443.3±55.0 °C(Predicted)
밀도
1.82±0.1 g/cm3(Predicted)
저장 조건
Keep in dark place,Inert atmosphere,2-8°C
용해도
클로로포름(약간 용해됨)
물리적 상태
고체
물리적 상태
단단한 모양
산도 계수 (pKa)
13.83±0.10(Predicted)
색상
흰색에서 연한 노란색
최대 파장(λmax)
280nm(H2O)(lit.)
Merck
14,3565
BCS Class
1
InChIKey
XQSPYNMVSIKCOC-NTSWFWBYSA-N
CAS 데이터베이스
143491-57-0(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
RTECS 번호 UW7360500
HS 번호 2934990002
유해 물질 데이터 143491-57-0(Hazardous Substances Data)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고 GHS hazard pictograms
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

엠트리시타빈 C화학적 특성, 용도, 생산

화학적 성질

White to Off-White Crystalline Solid

용도

Labeled Emtricitabine, intended for use as an internal standard for the quantification of Emtricitabine by GC- or LC-mass spectrometry.

정의

ChEBI: An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infect on.

원료

Resistance is associated with a substitution in the HIV-1 reverse transcriptase gene at codon 184 (M184V/I). Emtricitabineresistant isolates are cross-resistant to lamivudine. HIV-1 isolates with the K65R substitution in the reverse transcriptase coding region have reduced susceptibility.

일반 설명

Emtricitabine is an orally active NRTI whose pharmacokineticsare favorable for once-daily administration.

Pharmaceutical Applications

A synthetic nucleoside analog of cytosine, formulated for oral use.

Pharmacokinetics

Oral absorption: capsules 93%
Cmax 200 mg oral once daily: 1.8 ± 0.7 mg/L
Plasma half-life: c. 10 h
Volume of distribution: 1.4 ± 0.3 L/kg
Plasma protein binding: <4%
Absorption and distribution
It is rapidly and extensively absorbed. There is moderate CNS penetration. The estimated semen:plasma ratio is approximately 4. There are presently no data on levels in breast milk.
Metabolism and excretion
It does not inhibit human cytochrome P450 enzymes. About 80% is excreted in the urine, the rest in feces. Renal clearance is greater than the estimated creatinine clearance, suggesting elimination by both glomerular filtration and active tubular secretion. There may be competition for elimination with other compounds that are renally excreted. Exposure is significantly increased in renal insufficiency, but dose reductions are not generally recommended. It is unlikely that a dose adjustment would be required in the presence of hepatic impairment.

Clinical Use

Treatment of HIV infection (in combination with other antiretroviral drugs)

부작용

At least 10% of patients suffer headache, diarrhea, nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough and rhinitis. Skin hyperpigmentation is common (≥10%) in pediatric patients. Emtricitabine competes with lamivudine for the enzymes involved in intracellular phosphorylation; their co- administration is contraindicated.

엠트리시타빈 준비 용품 및 원자재

원자재

준비 용품


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