Isoflupredone
(Synonyms: 异氟泼尼松) 目录号 : GC49634
A glucocorticoid and mineralocorticoid receptor agonist
Cas No.:338-95-4
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
Isoflupredone is an agonist of glucocorticoid and mineralocorticoid receptors (EC50s = 0.877 and 0.007 nM, respectively, in transactivation assays).1 It inhibits LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages (IC50 = 25.5 nM).2 Topical application of a solution containing isoflupredone inhibits croton oil-induced ear edema in rats (ED50 = 51.9 nM). Isoflupredone (0.6 mg/day) increases mean arterial pressure (MAP) and decreases the levels of potassium and sodium in the plasma and urine, respectively, in sheep.3 It reduces tumor levels of uridine incorporation into 18S and 28S rRNA in a P1798 murine lymphoma model when administered at a dose of 25 mg/kg.4
1.Grossmann, C., Scholz, T., Rochel, M., et al.Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: A comparison of their glucocorticoid and mineralocorticoid propertiesEur. J. Endocrinol.151(3)397-406(2004) 2.Park, K.-K., Ko, D.-H., You, Z., et al.Synthesis and pharmacological evaluations of new steroidal anti-inflammatory antedrugs: 9α-Fluoro-11β,17α,21-trihydroxy-3,20-dioxo-pregna-1,4-diene-16α-carboxylate (FP16CM) and its derivativesSteroids71(1)83-89(2006) 3.Coghlan, J.P., Denton, D.A., Mills, E.H., et al.Steroid antagonism of the ’hypertensinogenic’ activity of 9α-fluoroprednisoloneLife Sci.35(26)2609-2612(1984) 4.Stevens, J., Mashburn, L.T., and Hollander, V.P.Effect of 9α-fluoroprednisolone and ?-asparaginase on uridine incorporation into ribosomal RNA of P1798 lymphosarcomaBiochim. Biophys. Acta186(2)332-339(1969)
| Cas No. | 338-95-4 | SDF | Download SDF |
| 别名 | 异氟泼尼松 | ||
| Canonical SMILES | F[C@]12[C@@]([C@@](CC[C@]3(O)C(CO)=O)([H])[C@]3(C)C[C@@H]2O)([H])CCC4=CC(C=C[C@@]41C)=O | ||
| 分子式 | C21H27FO5 | 分子量 | 378.4 |
| 溶解度 | DMSO : 25 mg/mL (66.06 mM; ultrasonic and warming and heat to 60°C) | 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 | 2.6427 mL | 13.2135 mL | 26.4271 mL |
| 5 mM | 0.5285 mL | 2.6427 mL | 5.2854 mL |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6427 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。
Pharmacokinetics and pharmacodynamics of intra-articular Isoflupredone following administration to horses with lipopolysaccharide-induced synovitis
BMC Vet Res 2022 Dec 13;18(1):436.PMID:36514067DOI:10.1186/s12917-022-03537-5.
Background: Intra-articular corticosteroids, such as Isoflupredone acetate, are commonly used in the treatment of joint inflammation, especially in performance horses. Following administration in a non-inflamed joints blood concentrations of Isoflupredone were low and detectable for only a short period of time post-administration compared to synovial fluid concentrations. For some drugs, inflammation can affect pharmacokinetics, therefore, the goal of the current study was to describe the pharmacokinetics of Isoflupredone acetate following intra-articular administration using a model of acute synovitis. Secondarily, pharmacodynamic effects, including effects on joint circumference, joint flexion, and lameness following intra-articular administration of Isoflupredone acetate in the experimental model were described. Methods: Sixteen horses received a single intra-articular dose of 8 mg of Isoflupredone acetate or saline 12 h post-administration of lipopolysaccharide. Blood and urine samples were collected up to 72 h and synovial fluid for 28 days post-administration, drug concentrations determined by liquid chromatography- mass spectrometry and pharmacokinetic analysis performed. Joint circumference, maximum angle of pain free joint flexion and lameness were evaluated prior to and post-treatment. Results: The maximum Isoflupredone plasma concentration was 2.45 ± 0.61 ng/mL at 2.5 ± 0.75 h and concentrations were less than the limit of quantitation by 72 h. Isoflupredone was below detectable concentrations in urine by 72 h post-administration in all horses and no longer detectable in synovial fluid by 96 h post-administration. Joint circumference was significantly decreased in the Isoflupredone treatment group compared to the saline group at 24 and 48 h post drug administration. Pain free joint flexion was significantly different between the saline and Isoflupredone treatment groups on day 4 post-treatment. Conclusions: Synovial fluid concentrations and maximum plasma concentrations of Isoflupredone differed slightly between the current study and a previous one describing administration into a non-inflamed joint, however, the detection time of Isoflupredone in blood was comparable. Effects of Isoflupredone on joint circumference and degree of pain free joint flexion suggest a short duration of effect with respect to alleviation of lipopolysaccharide induced synovitis, however, results of this study support future studies of the anti-inflammatory effects of intra-articular Isoflupredone acetate.
Identification and Exploration of Novel Macrophage M2-Related Biomarkers and Potential Therapeutic Agents in Endometriosis
Front Mol Biosci 2021 Jul 6;8:656145.PMID:34295919DOI:10.3389/fmolb.2021.656145.
Endometriosis (EM) is a chronic neuroinflammatory disorder that is associated with pain and infertility that affects ∼10% of reproductive-age women. The pathophysiology and etiology of EM remain poorly understood, and diagnostic delays are common. Exploration of the underlying molecular mechanism, as well as novel diagnostic biomarkers and therapeutic targets, is urgently needed. Inflammation is known to play a key role in the development of lesions, which are a defining feature of the disorder. In our research, the CIBERSORT and WGCNA algorithms were used to establish a weighted gene co-expression network and to identify macrophage-related hub genes using data downloaded from the GEO database (GSE11691, 7305). The analysis identified 1,157 differentially expressed genes (DEGs) in EM lesions, of which five were identified as being related to M2 macrophages and were validated as differentially expressed by qRT-PCR and immunohistochemistry (IHC). Of these putative novel biomarker genes, bridging integrator 2 (BIN2), chemokine receptor 5 (CCR5), and macrophage mannose receptor 1 (MRC1) were upregulated, while spleen tyrosine kinase (SYK) and metalloproteinase 12 (ADAM12) were downregulated in ectopic endometria vs. normal endometria. Meanwhile, 23 potentially therapeutic small molecules for EM were obtained from the cMAP database, among which topiramate, Isoflupredone, adiphenine, dexverapamil, MS-275, and celastrol were the top six molecules with the highest absolute enrichment values. This is our first attempt to use the CIBERSORT and WGCNA algorithms for the identification of novel Mϕ2 macrophage-related biomarkers of EM. Our findings provide novel insights into the impact of immune cells on the etiology of EM; nevertheless, further investigation of these key genes and therapeutic drugs is needed to validate their effects on EM.
Disposition of Isoflupredone acetate in plasma, urine and synovial fluid following intra-articular administration to exercised Thoroughbred horses
Drug Test Anal 2016 Jan;8(1):141-7.PMID:26333097DOI:10.1002/dta.1834.
The use of Isoflupredone acetate in performance horses and the scarcity of published pharmacokinetic data necessitate further study. The objective of the current study was to describe the plasma pharmacokinetics of Isoflupredone acetate as well as time-related urine and synovial fluid concentrations following intra-articular administration to horses. Twelve racing-fit adult Thoroughbred horses received a single intra-articular administration (8 mg) of Isoflupredone acetate into the right antebrachiocarpal joint. Blood, urine and synovial fluid samples were collected prior to and at various times up to 28 days post drug administration. All samples were analyzed using liquid chromatography-Mass Spectrometry. Plasma data were analyzed using a population pharmacokinetic compartmental model. Maximum measured plasma Isoflupredone concentrations were 1.76 ± 0.526 ng/mL at 4.0 ± 1.31 h and 1.63 ± 0.243 ng/mL at 4.75 ± 0.5 h, respectively, for horses that had synovial fluid collected and for those that did not. The plasma beta half-life was 24.2 h. Isoflupredone concentrations were below the limit of detection in all horses by 48 h and 7 days in plasma and urine, respectively. Isoflupredone was detected in the right antebrachiocarpal and middle carpal joints for 8.38 ± 5.21 and 2.38 ± 0.52 days, respectively. Results of this study provide information that can be used to regulate the use of intra-articular Isoflupredone in the horse.
Pharmacodynamics of Isoflupredone acetate in an endotoxin-induced mastitis model
J Dairy Sci 2003 Mar;86(3):792-8.PMID:12703615DOI:10.3168/jds.S0022-0302(03)73661-3.
The effect of intravenous administration of the steroidal drug Isoflupredone acetate on lactating dairy cows with mastitis induced using gram-negative bacterial endotoxin was investigated. Cows were randomly assigned to one of four treatment groups: untreated controls, Isoflupredone acetate only, mastitis only, and mastitis plus Isoflupredone acetate. Isoflupredone acetate was given to treated groups at a dose of 20 mg intravenously, once. Mastitic cows receiving treatment were given Isoflupredone acetate after the development of clinical signs. When compared with untreated mastitic controls, cows with endotoxin-induced mastitis treated with Isoflupredone acetate did not exhibit measurable differences in heart rate, rectal temperature, rumen motility, or changes in mammary gland surface area in the 14 h following the administration of intramammary endotoxin. Healthy cows treated with Isoflupredone acetate had a higher heart rate over the 14 h after drug administration than did untreated healthy controls. When compared with untreated mastitic controls, cows treated with Isoflupredone acetate did not exhibit statistically significant differences in milk production following endotoxin-induced mastitis.
Effect of Isoflupredone acetate with or without insulin on energy metabolism, reproduction, milk production, and health in dairy cows in early lactation
J Dairy Sci 2007 Sep;90(9):4181-91.PMID:17699036DOI:10.3168/jds.2006-897.
Glucocorticoids are commonly used to treat cows with clinical ketosis and fatty liver disease, but their use is controversial. The objectives of the present study were to investigate the effects of Isoflupredone acetate alone or with insulin on the energy metabolism of dairy cows in early lactation in a large double-blind, randomized clinical trial. A total of 1,162 Holstein cows and first-lactation heifers were randomly assigned to receive 1 of 3 treatments between the day of parturition and 8 DIM: group A, 20-mg i.m. injection of Isoflupredone and 100 units of insulin; group B, 20-mg i.m. injection of Isoflupredone; group C (control group), 10-mL i.m. injection of sterile water. Treatments were randomized across 24 dairy farms located near Guelph, Ontario, Canada. Serum samples obtained at the time of treatment and at wk 1 and 2 following treatment were analyzed for beta-hydroxybutyrate, nonesterified fatty acids, glucose, calcium, potassium, sodium, and chloride. Cows were assigned a body condition score at the time of enrollment. Data were analyzed using a repeated-measures mixed model that accounted for the effects of parity and body condition score, and the random effects of cow and farm. Cows that received Isoflupredone with insulin and Isoflupredone alone had higher beta-hydroxybutyrate and nonesterified fatty acid concentrations 1 wk after treatment compared with control cows. Cows that received Isoflupredone acetate plus insulin had lower glucose concentrations at 1 wk after treatment. Calcium concentrations 1 wk after treatment were lower for cows that received Isoflupredone and insulin or Isoflupredone only compared with control cows. Serum sodium, potassium, and chloride concentrations were not influenced by treatment. The effect of treatment on the proportion of cows with subclinical ketosis was evaluated with a logistic regression model. Over the 2 wk following treatment, a significant increase in the prevalence of subclinical ketosis was observed in the Isoflupredone plus insulin group relative to the control group. Among 972 cows that were not ketotic at enrollment, cows that received Isoflupredone acetate plus insulin or Isoflupredone acetate only were, respectively, 1.72 and 1.59 times more likely than control cows to develop subclinical ketosis 1 wk after treatment. There were no treatment effects on test-day milk production, milk fat and protein percentages, or the intervals from calving to first insemination or pregnancy.