FLUTICASONE FUROATE

FLUTICASONE FUROATE 구조식 이미지
카스 번호:
397864-44-7
상품명:
FLUTICASONE FUROATE
동의어(영문):
AvaMys;Veramyst;AllerMist;Gw 685698x;GSK 685 698;Unii-js86977wnv;FLUTICASONE FUROATE;Fluticasone Foruate;Fluticasone Furoate-d3;Fluticasone Impurity 31 (Fluticasone Furoate)
CBNumber:
CB51509114
분자식:
C27H29F3O6S
포뮬러 무게:
538.58
MOL 파일:
397864-44-7.mol
MSDS 파일:
SDS

FLUTICASONE FUROATE 속성

녹는점
250-252°C (dec.)
끓는 점
625.2±55.0 °C(Predicted)
밀도
1.39
저장 조건
-20°C Freezer
용해도
클로로포름(약간 용해됨, 가열, 초음파 처리), 메탄올(약간 용해됨)
산도 계수 (pKa)
12.52±0.70(Predicted)
물리적 상태
고체
물리적 상태
단단한 모양
색상
흰색에서 황백색까지

안전

FLUTICASONE FUROATE C화학적 특성, 용도, 생산

개요

Fluticasone furoate is a new corticosteroid derivative launched as a nasal spray for the treatment of seasonal and perennial allergic rhinitis in adults and in children aged ≥2 years. It is structurally closely related to the previously marketed intranasal corticosteroid fluticasone propionate (FP). Both of these steroids contain the unusual S-fluoromethyl carbothioate group, which confers high lipophilicity and hence enhanced binding and retention of the drug by the nasal tissue. Additionally, the carbothioate group rapidly undergoes first-pass metabolism by CYP3A4, thus minimizing systemic exposure of the parent drug. Fluticasone furoate is a potent ligand for the glucocorticoid receptor (GR), with a relative receptor affinity (RRA) of 2,989 with reference to dexamethasone RRA of 100.
Following intranasal administration, most of the dose is eventually swallowed and undergoes incomplete absorption and extensive firstpass metabolism in the liver and gut, resulting in negligible systemic exposure. Pharmacokinetic studies using oral solution dosing and intravenous dosing show that at least 30% of fluticasone furoate is absorbed and then rapidly cleared from plasma. The most common adverse reactions (W1% incidence) included headache, epistatix, sinus and throat pain, nasal ulceration, back pain, pyrexia, and cough. Fluticasone furoate is chemically derived starting from a readily available corticosteroid, 6a,9a-difluoro-11b,17a-dihydroxy-16a-methyl-3-oxoandrosta-1,4-diene-17b-carboxylic acid, by first converting the carboxylic acid group to the corresponding carbothioic acid via activation with carbonyl diimidazole followed by reaction with hydrogen sulfide gas. Subsequently, selective acylation of the 17a-hydroxyl group with 2-furoyl chloride and alkylation of the 17b-carbothioic acid group with bromofluoromethane under basic conditions provides fluticasone furoate.

화학적 성질

White to Off-White Solid

용도

Fluticasone-d3 Furoate is an isotope labelled form of Fluticasone Furoate (F599510). Fluticasone Furoate is a synthetic corticosteroid derived from fluticasone for treatment of seasonal allergic rhinitis.

정의

ChEBI: A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a 2-furoyl s bstituent at position 17. Used in combination with vilanterol trifenate for treatment of bronchospasm associated with chronic obstructive pulmonary disease.

FLUTICASONE FUROATE 준비 용품 및 원자재

원자재

준비 용품


FLUTICASONE FUROATE 공급 업체

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