23674-86-4CCCC(=O)O[C@]1(C(=O)COC(C)=O)CC[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21CWYQPLTPSGFELIB-JTQPXKBDSA-NDifluprednate is a corticosteroid hormone and a butyrate ester.
23674-86-4Pharmaceuticals -> Dermatologicals -> Corticosteroids, dermatological preparations
Pharmaceuticals -> Listed in ZINC15
Breast Feeding; Lactation; Anti-Inflammatory Agents; Corticosteroids, Ophthalmic; Glucocorticoids;
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
안전 정보는 참고용이며, 공급업체의 물질안전보건자료(SDS), 관련 법규 및 전문가 평가를 대체하지 않습니다.
This chemical does not meet GHS hazard criteria for 20% (1 of 5) of reports.
Danger
H302+H312+H332 (20%): Harmful if swallowed, in contact with skin or if inhaled [Warning Acute toxicity, oral; acute toxicity, dermal; acute toxicity, inhalation]
P203, P260, P261, P264, P270, P271, P280, P301+P317, P302+P352, P304+P340, P317, P318, P319, P321, P330, P362+P364, P405, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 5 reports by companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
D - Dermatologicals
S - Sensory organs
QD - Dermatologicals
QS - Sensory organs
Corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). It is postulated that these proteins control the biosynthesis of potent mediators of infammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Difluprednate is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB), the drug’s active metabolite. Endogenous tissue esterases then metabolize DFB to the inert metabolite hydroxyfluoroprednisolone butyrate (HFB), which limits systemic exposure to the active compound.
A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system.
Difluprednate penetrates the corneal epithelium rapidly and effectively. Low systemic absorption.
78.5% of radioactivity was excreted aftert 24 hours, and 99.5% by 7 days after a single dose of labeled difluprednate instilled in the right eyes of pigmented rabbits.
불러오는 중…
DTXSID0046773CHEMBL1201749CHEBI:31485White Solid
개요Difluprednate is a synthetic glucocorticoid that potently activates the glucocorticoid receptor (Ki = 78 pM). In vivo, ocular administration of difluprednate (0.05% w/v) increases intraocular pressure in sheep. Formulations containing difluprednate have been used to treat diabetic macular edema and inflammation following cataract surgery.
용도Difluprednate-d3 is the isotope labeled form of Difluprednate (D445925), a corticosteroid (derivative of prednisolone), approved for the treatment of post-operative ocular inflammation.
일반 설명Difluprednate, 21-(acetyloxy)-6α,9-difluoro-11β-hydroxy-17-(1-oxobutoxy)pregna-1,4-diene-3,20-dione is being developed (phase III) as a topical ophthalmicemulsion to treat inflammatory eye diseases.