Fluocortolone
(Synonyms: 氟可龙) 目录号 : GC49631
A glucocorticoid
Cas No.:152-97-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fluocortolone is a glucocorticoid.1,2 It inhibits progesterone 3α-hydroxysteroid dehydrogenase in rat cortical homogenates (IC50 = 40 µM).1 Fluocortolone (3, 6, and 12 mg/kg) decreases adjuvant-induced paw edema in rats.2
1.StÜrenburg, H.J., Fries, U., and Kunze, K.Glucocorticoids and anabolic/androgenic steroids inhibit the synthesis of GABAergic steroids in rat cortexNeuropsychobiology35(3)143-146(1997) 2.Bhargava, A.S.Effect of anti-inflammatory agents on adjuvant-induced edema modified for primary testPharmacol. Res. Commun.3(1)83-91(1971)
| Cas No. | 152-97-6 | SDF | Download SDF |
| 别名 | 氟可龙 | ||
| Canonical SMILES | C[C@@]12[C@](C[C@H]([C@@H]2C(CO)=O)C)([H])[C@@]3([H])[C@@]([C@H](C1)O)([H])[C@@]4(C([C@H](C3)F)=CC(C=C4)=O)C | ||
| 分子式 | C22H29FO4 | 分子量 | 376.5 |
| 溶解度 | Chloroform: soluble,Methanol: soluble,Water: soluble | 储存条件 | -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 | 2.656 mL | 13.2802 mL | 26.5604 mL |
| 5 mM | 0.5312 mL | 2.656 mL | 5.3121 mL |
| 10 mM | 0.2656 mL | 1.328 mL | 2.656 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。
Fluocortolone: pharmacokinetics and effect on plasma cortisol level
Eur J Clin Pharmacol 1986;30(4):433-8.PMID:3743619DOI:10.1007/BF00607956.
The pharmacokinetics of Fluocortolone and its effect on plasma cortisol levels are described after oral administration of 20, 50 and 100 mg to 9 healthy adults. The concentrations of Fluocortolone and cortisol in plasma were measured simultaneously by HPLC with UV detection. Fluocortolone was rapidly absorbed after all doses, giving the maximum plasma level after 1.4-2.1 h. After ingestion of 20, 50 and 100 mg, the peak levels were 199, 419 and 812 ng/ml, respectively. The maximum plasma levels and areas under the plasma level-time curves increased in proportion to the dose. Post-maximum plasma levels declined monoexponentially with a half-life of 1.76 h. Plasma half-life (t1/2 = 1.76 h), volume of distribution (1.03 l/kg) and oral clearance (6.9 ml/min/kg) were independent of the dose. The intensity and duration of adrenal suppression was dose dependent. Maximum suppression was observed 8 hours after Fluocortolone. Clearcut suppression of cortisol levels after 24 hours was only seen following 100 mg Fluocortolone.
Fluocortolone: pharmacokinetics and effect on ACTH and cortisol secretion during daily and alternate-day administration
Eur J Clin Pharmacol 1988;35(2):177-81.PMID:2847930DOI:10.1007/BF00609249.
The pharmacokinetics of Fluocortolone and its effect on the circadian rhythm of plasma cortisol and ACTH have been studied during different schedules of oral administration. Groups of 6 healthy male adults were given a single daily dose of Fluocortolone 5, 10 and 20 mg, and another group received 20 mg every second day. Administration to all groups was continued for 8 days. Pharmacokinetic parameters of Fluocortolone (half lives of absorption-t1/2a and elimination t1/2e, volume of distribution V and oral clearance (CL/f) were independent of the duration of treatment and dose. Areas under the plasma level curves, AUC and Cmax values increased in proportion to the dose, indicating dose linearity of Fluocortolone pharmacokinetics. A normal morning cortisol peak occurred during all treatment schedules, which indicates that circadian cortisol secretion was not seriously affected by the glucocorticoid treatment. On the other hand, when the level of circulating Fluocortolone was high the 12.00 a.m. and 4.00 p.m. cortisol levels were diminished compared to the pre and posttreatment values. There was no definite correlation between the ACTH and cortisol levels, either on treatment or on control days. ACTH levels were suppressed by daily treatment with the 20 mg dose. Thus, even during administration of a high dose of a glucocorticoid, the circadian secretion of cortisol can be preserved if the treatment is adjusted according to the half-life of the drug.
Determination of Fluocortolone pivalate and Fluocortolone hexanoate in suppositories using reverse-phase HPLC
Farmaco 2000 Feb;55(2):125-7.PMID:10782383DOI:10.1016/s0014-827x(00)00003-3.
Fluocortolone and its esters are synthetic corticosteroids used topically in the treatment of various skin disorders. A method that can be successfully used for the separation and determination of Fluocortolone pivalate and Fluocortolone hexanoate in suppositories was developed. This method is based on reverse-phase HPLC on Supelcosil LC-18 (25 cm x 4.6 mm, 5 microns), using methanol-acetonitrile-water-glacial acetic acid (17:46:37:0.4 v/v/v/v) as mobile phase at a flow rate of 3.0 ml/min. Detection was carried out using a UV detector at 238 nm. The method developed was validated, and calibration curves were established dependent on peak area. The validated ranges for Fluocortolone pivalate and Fluocortolone hexanoate are 15-305 micrograms/ml (r = 0.9995) and 15-315 micrograms/ml (r = 0.9996), respectively. The limits of detection and the limits of quantification for both esters were also determined.
Differential effects of hydrocortisone, Fluocortolone, and aldosterone on nocturnal sleep in humans
Acta Endocrinol (Copenh) 1987 Sep;116(1):129-37.PMID:3661052DOI:10.1530/acta.0.1160129.
Previous experiments have suggested that sleep processes are sensitive to influences of corticosteroids. The present experiment was designed to compare effects of three different corticosteroids on human sleep: Fluocortolone (a synthetic pure glucocorticoid), cortisol which possesses glucocorticoid and mineralocorticoid activity, and aldosterone (the major mineralocorticoid). Ten male adult subjects were tested in four experimental nights according to a double-blind latin-square design under conditions of either 1.0 mg of aldosterone, 20 mg of Fluocortolone, 80 mg of hydrocortisone, or placebo. Substances were administered orally (Fluocortolone, 23.00 h) or infused iv throughout the night (hydrocortisone, aldosterone) starting at 23.00 h. Hydrocortisone and Fluocortolone induced a substantial reduction of rapid eye movement sleep. Hydrocortisone increased slow wave sleep activity. No such effect was observed after Fluocortolone. Effects on sleep processes of aldosterone, in general, seemed to be neglegible. The results demonstrate differential effects of synthetic glucocorticoid, cortisol, and aldosterone on sleep in humans, which may be attributed to the heterogeneity of corticosteroid receptors in the brain.
Pharmacokinetics of Fluocortolone in man
Eur J Clin Pharmacol 1986;30(5):615-7.PMID:3758149DOI:10.1007/BF00542423.
The kinetics of the synthetic corticoid Fluocortolone was determined in 9 healthy female volunteers after a single oral dose of 20 mg. The maximal plasma level Fluocortolone (Cmax) of 202 +/- 70 ng/ml occurred within 85 +/- 32 min of oral intake after which it declined monoexponentially. Total plasma clearance was 6.48 +/- 2.07 ml/min X kg and the clearance of unbound Fluocortolone was 60.38 +/- 26.67 ml/min X kg. Plasma protein binding was 83 to 95%. The volume of distribution at steady-state was 1.01 +/- 0.341/kg for total Fluocortolone and 11.21 +/- 3.771/kg for unbound drug. The results of the study characterize the kinetics of unbound Fluocortolone for the first time. In addition, the kinetics of total Fluocortolone presented here confirm values calculated previously.