| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
As a glucocorticoid drug, Hydrocortisone hemisuccinate hydrate primarily targets the intracellular glucocorticoid receptor (GR). After entering the body, its active form binds to the glucocorticoid receptor, thereby regulating the expression of downstream inflammation-related genes. It exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and reducing the synthesis of inflammatory mediators. By inhibiting phospholipase A2 activity, this drug blocks the production pathways of potent inflammatory mediators such as prostaglandins and leukotrienes.
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|---|---|
| ln Vitro |
Hydrocortisone hemisuccinate hydrate demonstrates significant immunosuppressive activity in vitro. Research indicates that this compound effectively inhibits the bioactivity of interleukin-6 (IL-6) with an IC₅₀ value of approximately 6.7 μM. Additionally, it inhibits the bioactivity of interleukin-3 (IL-3) with an IC₅₀ value of 21.4 μM. These cytokines play critical roles in inflammatory responses and immune regulation, and their inhibition reflects the typical pharmacological properties of this compound as a glucocorticoid anti-inflammatory drug. Due to its glucocorticoid activity, this compound also controls the biosynthesis of inflammatory mediators by inducing the production of lipocortins.
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| ln Vivo |
Hydrocortisone hemisuccinate hydrate exhibits clear anti-inflammatory activity in in vivo animal models. Studies have confirmed that this compound is orally active and can be used in research related to ulcerative colitis (UC). In glucocorticoid-induced animal models, it is widely used as a tool drug to establish animal models of hyperadrenocorticism or kidney-yin deficiency syndrome. For example, subcutaneous or intramuscular administration of this drug at certain doses in mouse models successfully reproduces animal models reflecting the characteristics of kidney-yin deficiency syndrome in traditional Chinese medicine, manifested by shortened swimming time, reduced hypoxia tolerance, and immunosuppression.
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| Enzyme Assay |
Glucocorticoid receptor binding assays typically employ a radioligand competitive binding method. The brief protocol is as follows: Prepare cytosol from tissues with high glucocorticoid receptor expression (such as rat liver or thymus) or use recombinantly expressed receptor protein. Mix a fixed concentration of radiolabeled ligand (e.g., ³H-dexamethasone, typically 1-10 nM) with serially diluted Hydrocortisone hemisuccinate hydrate (concentration range 10⁻¹⁰ to 10⁻⁵ M), then add the receptor protein and incubate at 4°C for 12-24 hours to reach binding equilibrium. After incubation, adsorb unbound free ligand using dextran-coated charcoal (DCC) suspension, centrifuge at high speed, and measure the radioactivity in the supernatant using a liquid scintillation counter. Generate a competition binding curve by nonlinear regression analysis to calculate the IC₅₀ (concentration required to inhibit 50% of radioligand binding), and convert to the inhibition constant (Ki) using the Cheng-Prusoff equation.
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| Cell Assay |
The IL-6-dependent cell line (e.g., MH60.BSF2 cells) can be used to evaluate the inhibitory effect of this compound on cytokine activity. The standard protocol is as follows: Seed MH60.BSF2 cells in log phase at an appropriate density into 96-well plates, then add a fixed concentration of recombinant IL-6 and serially diluted Hydrocortisone hemisuccinate hydrate (typically prepare a stock solution in DMSO, then dilute with cell culture medium to final concentrations of 0.1-100 μM) to each well. After incubation for 44-48 hours at 37°C in a 5% CO₂ cell culture incubator, add MTT reagent (final concentration 0.5 mg/mL) and incubate for an additional 4 hours. Subsequently, add lysis solution (e.g., DMSO or acidified isopropanol) to dissolve the formazan crystals, and measure the absorbance of each well at 570 nm using a microplate reader. Evaluate the in vitro activity of this compound by calculating the IC₅₀ for inhibition of IL-6-dependent cell proliferation.
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| Animal Protocol |
This compound is commonly used to establish animal models of hyperadrenocorticism or kidney-yin deficiency syndrome. The typical experimental protocol is as follows: Use adult Kunming mice or Wistar/SD rats weighing 16-25 g (mice) or 180-200 g (rats). Prepare Hydrocortisone hemisuccinate hydrate in appropriate solvent and administer at doses of 24.4-48.8 mg/kg (mice) or 5 mg/100 g body weight (rats) via intramuscular, subcutaneous, or oral gavage routes. The dosing regimen can be once daily for 4-14 consecutive days. Evaluation indicators for successful model establishment include: behavioral observations (reduced activity, sluggish response, arched back with curled posture, dull fur), metabolic parameters (weight loss, elevated blood glucose), immunological parameters (thymus and spleen atrophy, decreased phagocytic function), and biochemical parameters (elevated plasma cAMP levels). Yang deficiency models typically require continuous dosing for 9 days combined with drug withdrawal treatment.
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| ADME/Pharmacokinetics |
Hydrocortisone hemisuccinate hydrate is a prodrug of hydrocortisone and is hydrolyzed to the active hydrocortisone in vivo. This compound is orally active, suggesting that it can be absorbed through the gastrointestinal tract. As a derivative with enhanced water solubility, Hydrocortisone hemisuccinate has improved dissolution characteristics compared to the parent compound. The active form, hydrocortisone, exhibits high plasma protein binding (>90%), primarily to corticosteroid-binding globulin and albumin. The drug is mainly metabolized in the liver, with metabolites excreted renally. Detailed pharmacokinetic parameters such as half-life, bioavailability, and volume of distribution for this compound are limited in the currently available literature, with most research focusing on in vitro and in vivo pharmacodynamic studies.
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| Toxicity/Toxicokinetics |
As a glucocorticoid drug, the toxicity of Hydrocortisone hemisuccinate hydrate is closely related to the dosage and duration of administration. As a laboratory research compound, this product is for research use only and not for human use. Long-term, high-dose use of glucocorticoids can lead to a range of adverse reactions, including iatrogenic hyperadrenocorticism (Cushing's syndrome), hyperglycemia, immunosuppression, osteoporosis, and muscle wasting. In mouse models, administration of this compound at certain doses results in observable manifestations including weight loss, reduced activity, dull fur, and arched back with curled posture, reflecting the metabolic derangements and immunosuppression caused by glucocorticoid excess. This compound is classified for research and development purposes only and is not intended for use in foods, cosmetics, or human/veterinary drugs.
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| References |
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| Additional Infomation |
Hydrocortisone hemisuccinate is the synthetic hemisuccinate form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive effects. Hydrocortisone acetate first binds to cytoplasmic glucocorticoid receptors; then, the receptor-ligand complex translocates to the nucleus, initiating the transcription of genes encoding anti-inflammatory mediators such as cytokines and lipocortin. Lipocorticoids inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and inhibiting the synthesis of prostaglandins and leukotrienes.
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| Molecular Formula |
C25H36O9
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|---|---|
| Molecular Weight |
480.55
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| Exact Mass |
462.225
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| CAS # |
83784-20-7
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| Related CAS # |
2203-97-6
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| PubChem CID |
219121
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| Appearance |
White to off-white solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
685.5±55.0 °C at 760 mmHg
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| Melting Point |
>195°C (dec.) (lit.)
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| Flash Point |
231.1±25.0 °C
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| Vapour Pressure |
0.0±4.8 mmHg at 25°C
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| Index of Refraction |
1.587
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| LogP |
2.13
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
908
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@]12[C@@](O)(C(=O)COC(=O)CCC(=O)O)CC[C@H]1[C@@H]1CCC3=CC(CC[C@]3(C)[C@H]1[C@H](C2)O)=O.O
|
| InChi Key |
AFLWPAGYTPJSEY-CODXZCKSSA-N
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| InChi Code |
InChI=1S/C25H34O8.H2O/c1-23-9-7-15(26)11-14(23)3-4-16-17-8-10-25(32,24(17,2)12-18(27)22(16)23)19(28)13-33-21(31)6-5-20(29)30;/h11,16-18,22,27,32H,3-10,12-13H2,1-2H3,(H,29,30);1H2/t16-,17-,18-,22+,23-,24-,25-;/m0./s1
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| Chemical Name |
4-[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy]-4-oxobutanoic acid;hydrate
|
| Synonyms |
Hydrocortisone 21-hemisuccinate hydrate; NSC757049; 83784-20-7; hydrocortisone hemisuccinate; NSC 757049; LIU00Z1Z84; NSC-757049; RefChem:923122; .
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (208.1 mM）
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0809 mL | 10.4047 mL | 20.8095 mL | |
| 5 mM | 0.4162 mL | 2.0809 mL | 4.1619 mL | |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0809 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT02768740
Conditions:Septic ShockProducts are for research use only; We do not sell to patients
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