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Diflorasone Sale

(Synonyms: 二氟拉松) 目录号 : GC31740

Diflorasone acts as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties.

Diflorasone Chemical Structure

Cas No.:2557-49-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥446.00
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5mg
¥401.00
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10mg
¥491.00
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25mg
¥670.00
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50mg
¥982.00
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100mg
¥1,428.00
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产品描述

Diflorasone acts as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties.

Chemical Properties

Cas No. 2557-49-5 SDF
别名 二氟拉松
Canonical SMILES C[C@@]12[C@](C(CO)=O)(O)[C@@H](C)C[C@@]1([H])[C@]3([H])C[C@H](F)C4=CC(C=C[C@]4(C)[C@@]3(F)[C@@H](O)C2)=O
分子式 C22H28F2O5 分子量 410.45
溶解度 DMSO : 130 mg/mL (316.73 mM) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4364 mL 12.1818 mL 24.3635 mL
5 mM 0.4873 mL 2.4364 mL 4.8727 mL
10 mM 0.2436 mL 1.2182 mL 2.4364 mL
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Research Update

Diflorasone

Topical diflorasone has not been studied during breastfeeding. Since only extensive application of the most potent corticosteroids may cause systemic effects in the mother, it is unlikely that short-term application of topical corticosteroids would pose a risk to the breastfed infant by passage into breastmilk. However, it would be prudent to use the least potent drug on the smallest area of skin possible. It is particularly important to ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated. Only the lower potency corticosteroids should be used on the nipple or areola where the infant could directly ingest the drugs from the skin; diflorasone should be avoided on the nipple.[1] Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking.[2] Any topical corticosteroid should be wiped off thoroughly prior to nursing if it is being applied to the breast or nipple area.

Diflorasone diacetate: vasoconstrictor activity and clinical efficacy of a new topical corticosteroid

Diflorasone diacetate, a new topical corticosteroid, was generally more potent than three high potency reference standards (fluocinonide, beta-methasone 17-valerate and fluocinolone acetonide) when the compounds were dissolved in 95% alcohol and applied in vasoconstrictor assays in healthy volunteers. On the basis of additional vasoconstrictor assay results, a 0-05% concentration of the steroid in a cream vehicle containing 15% propylene glycol was developed for therapeutic evaluation. In a double-blind comparison in 384 patients with dermatoses, 0-05% diflorasone diacetate cream was as effective as 0-05% fluocinonide cream in the therapy of lesions of psoriasis or atopic/neurodermatitis.

Structures from powders: diflorasone diacetate

Diflorasone diacetate, a steroid anti-inflammatory drug (marketed as Diacort or Florone by Pfizer) and used in the treatment of skin disorders, can be prepared as anhydrous form, DD1 (as deposited in the US pharmacopoeia), or as a monohydrated phase, DDW. Heating the DDW form above 90 degrees C, a mixture of DD1 and of a new anhydrous polymorph, DD2 is obtained. Further heating of this mixture, or of pure DD1, up to 230 degrees C (only a few degrees before melting!), generates an elusive anhydrous DD3 polymorph. Their crystal structures, determined uniquely from laboratory powder diffraction data, show the isomorphous character of the DDW and DD1 forms, while the DD2 and DD3 polymorphs crystallize with markedly different unit cells. Crystals of the DD1, DD2 and DDW forms are orthorhombic, P2(1)2(1)2(1), a=29.386(1)A; b=10.4310(9)A, c=8.1422(7)A, V=2495.8(3)A(3) for DD1; a=15.2639(10)A; b=11.7506(7)A, c=13.8931(11)A, V=2491.9(3)A(3) for DD2; a=30.311(2)A; b=10.6150(9)A, c=7.9337(7)A, V=2552.7(4)A(3) for DDW; while the lattice parameters for the monoclinic P2(1)DD3 species are a=11.5276(10)A; b=13.8135(11)A, c=7.8973(7)A, beta=103.053(6) degrees , V=1225.0(2)A(3). These compounds have also been fully characterized by thermo analytical methods, as well by (13)C, (19)F, and (1)H NMR spectroscopy.

Diflorasone diacetate ointment 0.05% versus betamethasone dipropionate ointment 0.05% in moderate-severe plaque-type psoriasis

We report the results of a 2-week double-blind, parallel clinical trial comparing two superpotent topical glucocorticosteroid ointments, diflorasone diacetate 0.05% and betamethasone dipropionate 0.05%, in psoriatic adults. Both corticosteroid ointments were fast acting and highly efficacious. 40 of the 44 patients who initially enrolled completed the trial. There were no statistically significant differences between the two glucocorticoids with respect to erythema, scaling, induration or the investigator's global evaluation after either 1 or 2 weeks of therapy. The level of patient satisfaction with the efficacy and cosmetic acceptability of these two category I glucocorticoids was similar. No systemic or local adverse reactions were noted.

Comparative efficacy of once a day diflorasone diacetate and twice a day betamethasone valerate ointment applications in eczematous dermatitis

The efficacy of once a day applications of 0.05% diflorasone diacetate ointment and twice a day applications of 0.1% betamethasone valerate ointment was compared in 70 patients with eczematous dermatitis. Altogether 32 patients completed the 3-week study. Fourteen patients in the diflorasone group and 6 on betamethasone left the study earlier because of total (100%) improvement of lesions. Eight patients left because of unsatisfactory progress and 6 because of personal reasons. There were only two noticeable differences observed between treatment groups. At Week 2, the diflorasone diacetate group improved significantly more than the betamethasone valerate group with respect to pruritus. At Week 3, this difference in the improvement of pruritus was marginally significant in favour of diflorasone diacetate. Excluding the complications due to a secondary infection, no adverse reactions were recorded in the diflorasone diacetate-treated patients; 1 betamethasone valerate-treated patient developed telangiectasia. The once a day applications of diflorasone diacetate not only proved to be slightly more efficacious than the twice a day applications of betamethasone valerate, but also provided the advantages of patient convenience and compliance.