Hydrocortisone 21-hemisuccinate (sodium salt)
(Synonyms: 氢化可的松琥珀酸钠) 目录号 : GC43873
A derivative of cortisol
Cas No.:125-04-2
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
Hydrocortisone 21-hemisuccinate is a water-soluble form of the endogenous hormone cortisol. It can bind to glucocorticoid receptors, initiating the transcription of anti-inflammatory and immunosuppressive mediators and inhibiting proinflammatory cytokine activity (IC50 = 6.7 µM for IL-6). It is commonly used to supplement media for long-term epithelial or endothelial cell cultures and to differentiate pluripotent stem cells.
| Cas No. | 125-04-2 | SDF | |
| 别名 | 氢化可的松琥珀酸钠 | ||
| Canonical SMILES | [H][C@]12[C@@]([C@@](CC[C@]3(O)C(COC(CCC([O-])=O)=O)=O)([H])[C@]3(C)C[C@@H]2O)([H])CCC4=CC(CC[C@@]41C)=O.[Na+] | ||
| 分子式 | C25H33O8•Na | 分子量 | 484.5 |
| 溶解度 | ≤20mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.064 mL | 10.3199 mL | 20.6398 mL |
| 5 mM | 0.4128 mL | 2.064 mL | 4.128 mL |
| 10 mM | 0.2064 mL | 1.032 mL | 2.064 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。
Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs
Pharmaceutics 2020 Dec 15;12(12):1213.PMID:33333795DOI:10.3390/pharmaceutics12121213.
Polymer-based solid microstructures (MSts) have the potential to significantly increase the quantity and range of drugs that can be administered across the skin. MSt arrays are used to demonstrate their capacity to bypass the skin barrier and enhance permeability by creating microchannels through the stratum corneum, in a minimally invasive manner. This study is designed to demonstrate the ability of MSts to exceed the current boundaries for transdermal delivery of compounds with different molecular weights, partition coefficients, acid dissociation constants, melting points, and water solubilities. In vitro permeation of a range of selected molecules, including acetyl salicylic acid (aspirin), galantamine, selegiline hydrochloride (Sel-HCl), insulin, caffeine, hydrocortisone (HC), Hydrocortisone 21-hemisuccinate sodium salt (HC-HS) and bovine serum albumin (BSA) has been studied across excised porcine skin with and without poke and patch application of MSts. Permeation of the molecules was monitored using Franz diffusion cells over 24 h. MSts significantly increased the permeation of all selected molecules up to 40 times, compared to topical applications of the molecules without MSts. The greatest increase in permeation was observed for caffeine with 70 ± 8% permeation and the lowest enhancement was observed for HC with a 2.4 ± 1.3% increase in permeation. The highest obtained flux was BSA (8133 ± 1365 μg/cm2/h) and the lowest flux observed for HC (11 ± 4 μg/cm2/h). BSA and HC also showed the highest (16,275 ± 3078 μg) and the lowest (73 ± 47 μg) permeation amount after 24 h respectively. MSt-treated skin exhibits greatly increased permeation. The molecule parameters (size, acid dissociation constant, partition coefficient and solubility)-traditional hurdles associated with passive diffusion through intact skin-are overcome using MSt skin treatment.
Glucocorticoids inhibit acetylcholine-induced current in chromaffin cells
Am J Physiol 1989 Nov;257(5 Pt 1):C906-12.PMID:2596584DOI:10.1152/ajpcell.1989.257.5.C906.
The effects of dexamethasone, a synthetic glucocorticoid, on membrane excitability and on the acetylcholine (ACh)-induced inward current (IACh) were studied in dispersed guinea pig adrenal medullary cells by using the whole cell version of the patch-clamp technique. Bath application of 10 microM dexamethasone had no effect on the resting membrane conductance or voltage-gated Na+, Ca2+, or K+ channels, whereas it reversibly inhibited the IACh at a holding potential of -70 mV. Intracellular application of dexamethasone through the patch electrode did not modify the IACh. Application of 10 microM dexamethasone neither shifted the dose-response curve of the peak IACh to the right [dissociation constant (Kd) = 50 microM] nor affected its Hill coefficient (1.2) but inhibited the current amplitudes by approximately 41% in the cells sufficiently pretreated with dexamethasone. Furthermore, fractional inhibition of the IACh at the end of approximately 50-s application was the same for any concentration of ACh (3-100 microM). The dose-response curve of the inhibition by dexamethasone showed a good fit to the theoretical line assuming an inhibition constant (Ki) of 10 microM and a Hill coefficient of 1. Hydrocortisone 21-hemisuccinate sodium salt (25 microM) and prednisolone 21-hemisuccinate sodium salt (25 microM) inhibited the IACh to a lesser extent than 25 microM dexamethasone. These results suggest that dexamethasone binds to the specific site on the outer cell membrane, probably on the ACh receptor-coupled channel, and inhibits the IACh in a noncompetitive manner, thus controlling the immediate catecholamine release from the adrenal medulla.
Inhibitory effects of anti-inflammatory drugs on interleukin-6 bioactivity
Biol Pharm Bull 2001 Jun;24(6):701-3.PMID:11411563DOI:10.1248/bpb.24.701.
Interleukin-6 (IL-6) is known as a proinflammatory cytokine involved in immune response, inflammation, and hematopoiesis. Inhibitory effects of anti-inflammatory drugs on IL-6 bioactivity using IL-6-dependent hybridoma have been evaluated. Three out of 16 nonsteroidal anti-inflammatory drugs (NSAIDs) showed IC50 values of less than 100 microM, which were in the order of oxyphenylbutazone hydrate (IC50=7.5 microM)>meclofenamic acid sodium salt (31.9 microM)>sulindac (74.9 microM). Steroidal anti-inflammatory drugs (SAIDs) exhibited significant inhibitory effects at 100 microM on the IL-6 bioactivity, and their inhibitory potencies were in the order of budesonide (IC50=2.2 microM)>Hydrocortisone 21-hemisuccinate (6.7 microM), prednisolone (7.5 microM), betamethasone (10.9 microM)>dexamethasone (18.9 microM) and triamcinolone acetonide (24.1 microM). The results would provide an additional mechanism by which anti-inflammatory drugs display their anti-inflammatory and immunosuppressive effects at higher concentrations.
Identification and analysis of drugs in the solid state by 13C CPMAS NMR: suxamethonium chloride and hydrocortisonum (Corhydron)
Acta Pol Pharm 2008 May-Jun;65(3):295-301.PMID:18646548doi
Cross-polarization (CP) magic angle spinning (MAS) 13C NMR spectroscopy has become a routine tool in pharmacy, employed to identify and characterize drugs in the solid phase. 13C CPMAS NMR spectra were recorded for solid Hydrocortisone 21-hemisuccinate and suxamethonium chloride. White crystalline substances, such as these two drugs, can be easily distinguished; and solid-state 13NMR spectra of remarkably good quality are obtained in less than half an hour. 13C CPMAS chemical shifts for solid suxamethonium chloride and hydrocortisone sodium hemisuccinate are given, as well as cross-polarization kinetic parameters for suxamethonium chloride.
Antiinflammatory screening of the medicinal plant Gynura procumbens
Plant Foods Hum Nutr 2002 Fall;57(3-4):233-44.PMID:12602932DOI:10.1023/a:1021851230890.
Gynura procumbens is used in Thai folk medicine to treat topical inflammation, rheumatism, and viral ailments. In the present work, attempts were made to verify the folk medicinal claim that the crude ethanolic extract of G. procumbens has antiinflammatory action and to relate the activity to particular fractions using a croton oil-induced mouse ear inflammation model. The original ethanolic extract of G. procumbens was partitioned between water and ethyl acetate. The residues were subjected to antiinflammatory evaluation. While the water extract did not show any antiinflammatory activity, the administration of the original organic extract significantly inhibited the increase in ear thickness in response to croton oil (n = 5). The activity of 0.75 mg/ear original organic extract showed similar antiinflammatory activity (inhibition 65.2%) to that of 6 mg/ear Hydrocortisone 21-hemisuccinate sodium salt (inhibition 64.8%). The organic extract was then fractionated with a series of solvents in order of increasing polarity. Each fraction was dried, dissolved in acetone and monitored using the same bioassay. These experiments showed that the hexane and toluene fractions showed significant inhibitions of 44.6% and 34.8%, respectively. These two fractions had similar activities to 4 mg/ear of hydrocortisone (inhibition 35.0%). The possible chemical constituents in the extracts and fractions were investigated using thin layer chromatography and specific color reagents. These tests showed that steroids might be one class of antiinflammatory compounds in this plant.