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Diflucortolone 21-valerate

(Synonyms: 戊酸双氟可龙) 目录号 : GC48491

A glucocorticoid

Diflucortolone 21-valerate Chemical Structure

Cas No.:59198-70-8

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10mg
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产品描述

Diflucortolone 21-valerate is a glucocorticoid.1 It has anti-inflammatory effects in a rat model of croton oil-induced ear edema when applied topically (ED50 = 9.7 µg/ml).2 Diflucortolone 21-valerate (0.1%) also induces skin inflammation and thins the epidermis in hairless dogs following chronic topical administration and increases allergic- and non-allergic-mediated skin inflammation in mouse models of atopic dermatitis when applied topically prior to and following sensitization.3,1 Formulations containing diflucortolone 21-valerate have been used in the treatment of inflammatory or allergic skin conditions.

1.Igawa, K., Katayama, I., Minatohara, K., et al.Topical glucocorticoid augments both allergic and non-allergic cutaneous reactions in mice when applied at the afferent stage of contact sensitivityAllergol. Int.46(1)33-41(1997) 2.Yamada, K., Hattori, S., Hakoda, T., et al.A fundamental study on a bioassay for the antiphlogistic effect of topically applied antiinflammatory agentsNihon Yakurigaku Zasshi75(8)789-798(1979) 3.Kimura, T., and Doi, K.Dorsal skin reactions of hairless dogs to topical treatment with corticosteroidsToxicol. Pathol.27(5)528-535(1999)

Chemical Properties

Cas No. 59198-70-8 SDF
别名 戊酸双氟可龙
Canonical SMILES F[C@@]12[C@](C[C@@H](C([C@@]2(C=C3)C)=CC3=O)F)([H])[C@@]4([H])[C@](C[C@@H]1O)([C@H]([C@@H](C4)C)C(COC(CCCC)=O)=O)C
分子式 C27H36F2O5 分子量 478.6
溶解度 DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 10 mg/ml 储存条件 -20°C
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1 mg 5 mg 10 mg
1 mM 2.0894 mL 10.4471 mL 20.8943 mL
5 mM 0.4179 mL 2.0894 mL 4.1789 mL
10 mM 0.2089 mL 1.0447 mL 2.0894 mL
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Research Update

[Anti-inflammatory effects of methylprednisolone aceponate in animals]

Nihon Yakurigaku Zasshi 1991 Nov;98(5):409-17.PMID:1813371DOI:10.1254/fpj.98.5_409.

In the case of dermal application of the drugs to croton oil-induced ear edema in rats and picryl chloride-induced delayed type hypersensitivity in mice, the anti-inflammatory effect of methylprednisolone aceponate (MPA) was slightly weaker than those of clobetasol 17-propionate and Diflucortolone 21-valerate, but stronger than those of hydrocortisone 17-butyrate and hydrocortisone 17-butyrate 21-propionate. Betamethasone 17-valerate applied dermally was less and more effective than MPA to ear edema in rats and delayed type hypersensitivity in mice, respectively. The anti-inflammatory effect of MPA was weaker in subcutaneous administration than in topical application to the two inflammatory models. It was suggested that MPA has strong anti-inflammatory effects and weak systemic effects by topical application. Methylprednisolone 17-propionate (MP-17P) and methylprednisolone (MP), unesterified in only the C-21 position and in both the C-17 and 21 positions of MPA, respectively, showed weaker anti-inflammatory activities than MPA by topical application to croton oil-induced ear edema. The ratio of the anti-inflammatory effects by topical application to subcutaneous administration of MPA was higher than those of MP-17P and MP. The excellent characteristics of MPA as a dermal anti-inflammatory drug are suggested to be derived from di-esterification of MP, which has a weak activity intrinsically.