아시트레틴

아시트레틴
아시트레틴 구조식 이미지
카스 번호:
55079-83-9
한글명:
아시트레틴
동의어(한글):
아시트레틴
상품명:
Acitretin
동의어(영문):
etretin;Acitren;Acitreti;Acetretin;ro10-1670;ACITRETIN;SORIATANE;NEOTIGASON;Acritretin;Acitretin A
CBNumber:
CB7184686
분자식:
C21H26O3
포뮬러 무게:
326.43
MOL 파일:
55079-83-9.mol
MSDS 파일:
SDS

아시트레틴 속성

녹는점
228-230°C
끓는 점
404.46°C (rough estimate)
밀도
1.1348 (rough estimate)
굴절률
1.4700 (estimate)
저장 조건
-20°C
용해도
물에는 거의 녹지 않으며, 테트라히드로푸란에는 조금 녹고, 아세톤과 에탄올(96%)에는 약간 녹으며, 시클로헥산에는 매우 녹습니다.
물리적 상태
가루
산도 계수 (pKa)
4.72±0.33(Predicted)
색상
Light yellow to yellow
최대 파장(λmax)
352nm(MeOH)(lit.)
Merck
14,112
안정성
감광성
CAS 데이터베이스
55079-83-9(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 T,N
위험 카페고리 넘버 61-36/38-50/53
안전지침서 53-26-45-60-61-37/39
유엔번호(UN No.) UN 3077 9/PG 3
WGK 독일 3
RTECS 번호 RA8460000
F 고인화성물질 8-10-21
위험 등급 9
포장분류 III
HS 번호 2918992090
유해 물질 데이터 55079-83-9(Hazardous Substances Data)
독성 LD50 i.p. in mice (mg/kg): >4000 (1 day), 700 (10 days), 700 (20 days) (Bollag, 1978)
그림문자(GHS): GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
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
H360 태아 또는 생식능력에 손상을 일으킬 수 있음 생식독성 물질 구분 1A, 1B 위험 GHS hazard pictograms
H410 장기적 영향에 의해 수생생물에 매우 유독함 수생 환경유해성 물질 - 만성 구분 1 경고 GHS hazard pictograms P273, P391, P501
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P273 환경으로 배출하지 마시오.
P302+P352 피부에 묻으면 다량의 물로 씻으시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P308+P313 노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.
NFPA 704
0
2 0

아시트레틴 MSDS


Etretin

아시트레틴 C화학적 특성, 용도, 생산

개요

Acitretin is the free acid form of etretinate useful in the treatment of severe psoriasis and other disorders of keratinization. Although the two compounds have virtually the same efficacy and teratogenic side-effects, acitretin is advantageous for child-bearing women, as its shorter half-life reduces the necessary contraception period from two years to only one month after treatment ceases.

화학적 성질

Crystalline Solid

용도

Acitretin, a retinoid that binds to nuclear receptors and regulates gene expression, is a potent activator of the α-secretase ADAM10 gene expression and apoptosis inducer via the CD95 signalling pathway. Acitretin is a systemic retinoid drug used in the treatment of severe psoriasis.

Indications

Unlike isotretinoin, acitretin (Soriatane) is not primarily sebosuppressive. Rather, it promotes normalization of dysregulated keratinocyte proliferative activity in the epidermis and is also antiinflammatory. Oral absorption is optimal when acitretin is taken with a fatty meal; peak levels are reached approximately 3 hours after ingestion, while steady-state plasma levels are achieved after approximately 3 weeks of daily dosing. The mean terminal elimination half-life of the parent compound is 49 hours. However, when consumed with ethanol, acitretin may be transesterified to form etretinate, a retinoid that is stored in adipose tissue, resulting in a much longer half-life (3–4 months or longer).

World Health Organization (WHO)

Acitretin, a retinol derivative, was introduced in 1989 for the treatment of severe psoriasis. By the end of 1990, acitretin was confirmed to be metabolized in part to etretinate. Marketing authorization was suspended temporarily in France while the product information was modified to conform to the recommendations issued by the Committee for Proprietary Medicinal Products of the European Communities. Acitretin remains registered in several countries. See also WHO comment for etretinate.

일반 설명

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
Acitretin is a major metabolite of etretinate and belongs to the class of retinoid and is typically used for treating psoriasis. Acitretin inhibits excessive cell growth and keratinisation which are the major symptoms of psoriasis, therefore reducing plaque formation and scaling.

Mechanism of action

Acitretin (Soriatane) is a synthetic derivative of vitamin A that is particularly effective in treating the pustular and erythrodermic forms of psoriasis. It is the main metabolite of etretinate; ingestion of alcohol with acitretin increases the amount of detectable etretinate. It is accumulated in fatty tissue with a prolonged elimination half-life of approximately 120 days. Most patients show improvement within 2 to 4 weeks, although some patients may need as long as 6 months of therapy before a response is noted.

Pharmacology

Like other systemic retinoids, acitretin is a serious teratogen and should not be prescribed for women of childbearing potential unless no acceptable alternative is available and the patient has acknowledged in writing that she understands the need to use two effective forms of contraception during therapy and for 3 years following discontinuation of therapy. Because of the much longer half-life of etretinate, which may be formed when ethanol is ingested with acitretin, female patients of childbearing potential must also agree not to ingest alcohol during treatment and for 2 months following its discontinuation. Other toxicities are similar to those of isotretinoin; they include cutaneous irritation and inflammation, bone and joint pain, hyperlipidemia, hepatic enzyme elevation, and tendinous and ligamentous calcifications.Alopecia (hair loss) may also occur in some patients.

Clinical Use

Acitretin is most useful for the treatment of severe psoriasis, particularly the pustular and erythrodermic variants. Psoriatic nail changes and arthritis also may respond. Combining the drug with ultraviolet light therapy (Re-UVB, in the case of ultraviolet B radiation, or Re-PUVA, with psoralen plus ultraviolet A radiation) permits the use of lower doses of both acitretin and ultraviolet radiation. Other conditions for which the drug may be especially useful include congenital and acquired hyperkeratotic disorders, such as the ichthyoses and palmoplantar keratodermas, and severe lichen planus.

부작용

Side effects are dose dependent and include elevation of triglycerides, hepatitis, hair loss, thinning of the nails, cheilitis, xerosis, and stickiness of the skin. Gemfibrozil (300 mg b.i.d.) corrects elevated lipid levels on this therapy.

아시트레틴 준비 용품 및 원자재

원자재

준비 용품


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