Diflorasone Diacetate
(Synonyms: 醋酸双氟拉松；二醋酸二氟拉松) 目录号 : GC40867
A corticosteroid
Cas No.:33564-31-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Diflorasone is a corticosteroid with anti-inflammatory activity. It reduces production of the inflammatory cytokines Il-6, Il-4, and macrophage inflammatory protein-2 (Mip-2) and completely inhibits swelling in the ears of toluene-2,4-diisocyaniate-sensitized mice following topical administration of 20 µL of a 0.05% solution. Diflorasone inhibits RANTES and thymus and activation regulated chemokine (TARC) in a dinitrochlorobenzene-induced mouse model of allergic contact dermatitis. It also inhibits proliferation of human keratinocytes in vitro and reduces epidermal thickening in a mouse model of psoriasis induced by imiquimod .
| Cas No. | 33564-31-7 | SDF | |
| 别名 | 醋酸双氟拉松；二醋酸二氟拉松 | ||
| Canonical SMILES | F[C@]12[C@@]([C@@](C[C@H](C)[C@]3(OC(C)=O)C(COC(C)=O)=O)([H])[C@]3(C)C[C@@H]2O)([H])C[C@H](F)C4=CC(C=C[C@@]41C)=O | ||
| 分子式 | C26H32F2O7 | 分子量 | 494.5 |
| 溶解度 | DMSO : 100 mg/mL (202.22 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0222 mL | 10.1112 mL | 20.2224 mL |
| 5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0222 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Diflorasone Diacetate: vasoconstrictor activity and clinical efficacy of a new topical corticosteroid
J Int Med Res 1976;4(6):454-61.PMID:800385DOI:10.1177/030006057600400613.
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
Steroids 2009 Jan;74(1):102-11.PMID:19013475DOI:10.1016/j.steroids.2008.09.014.
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
Dermatology 1993;186(2):129-32.PMID:8428041DOI:10.1159/000247323.
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.
Effects of polyoxypropylene 15 stearyl ether and propylene glycol on percutaneous penetration rate of Diflorasone Diacetate
J Pharm Sci 1979 Mar;68(3):275-80.PMID:423113DOI:10.1002/jps.2600680306.
Theoretical models for percutaneous penetration are described, and a diffusion apparatus useful in the evaluation of transport kinetics of drugs applied to skin is discussed. Experimental data are presented for: (a) the flux of Diflorasone Diacetate through hairless mouse skin, (b) the percutaneous penetration profile of propylene glycol, (c) the effects of vehicle concentrations of polyoxypropylene 15 stearyl ether and propylene glycol on the percutaneous flux of Diflorasone Diacetate, (d) skin--vehicle partition coefficients of Diflorasone Diacetate, (e) the solubility profile of Diflorasone Diacetate as a function of solvent concentration, and (f) the alteration of the skin's resistance to the penetration of Diflorasone Diacetate due to propylene glycol. Excess solvent in a vehicle caused a decrease in the percutaneous flux of Diflorasone Diacetate. Formulations containing 0.05 and 0.1% Diflorasone Diacetate had similar penetration rates when the solvent concentration was optimized for each percentage of Diflorasone Diacetate.
Comparative efficacy of once a day Diflorasone Diacetate and twice a day betamethasone valerate ointment applications in eczematous dermatitis
Curr Med Res Opin 1984;9(4):259-64.PMID:6510015DOI:10.1185/03007998409109589.
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.