| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Glucocorticoid receptor (GR)
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|---|---|
| ln Vitro |
Hydrocortisone hemisuccinate has no deleterious effect on MH60 cells that are IL-6-independent, but it inhibits the biological activities of IL-6 and IL-3 with IC50 values of 6.7 and 21.4 μM, respectively [3]. Hydrocortisone hemisuccinate (0.12-60 μM; 72 hours) suppresses T lymphocyte and peripheral lymphocyte cultures' responses to phytohemagglutinin (PHA) [3].
Suppressed IL-6-dependent proliferation of MH60.BSF2 cells (IC₅₀ = 3.5 × 10⁻⁷ M)[1] Inhibited lymphocyte proliferation in human tonsil cell cultures (91% inhibition at 10⁻⁵ M)[3] |
| ln Vivo |
In mice, oral administration of hydrocortisone hemisuccinate (30 mg/kg) twice a day for five days results in decreased weight loss and increased food intake [2].
Loaded in pH-sensitive hydrogel significantly reduced colitis symptoms in mice (DAI score 1.8 vs. 4.2 in control)[2] |
| Cell Assay |
IL-6 bioactivity assay: MH60.BSF2 cells cultured with IL-6 and test compounds for 44h. Cell viability measured via MTT assay. Hydrocortisone hemisuccinate dissolved in ethanol and diluted in medium[1]
Lymphocyte suppression: Human tonsil cells cultured with phytohemagglutinin for 72h. Hydrocortisone hemisuccinate added at initiation. Proliferation assessed via ³H-thymidine incorporation[3] |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (200-220 g, 10-11 weeks) induced colitis [2]
Doses: 30 mg/kg Route of Administration: Po twice (two times) daily for 5 days Experimental Results: Significant reduction in disease Activity index (DAI) scores and myeloperoxidase (MPO) activity compared with the 2,4,6-trinitrobenzene sulfonic acid (TNBS) group. Weight gain. Colitis treatment: Hydrocortisone hemisuccinate loaded in hydrogel (drug content 15% w/w). Administered rectally (100 mg/kg) to DSS-induced colitis mice daily for 7 days[2] |
| ADME/Pharmacokinetics |
The colon-targeting hydrogel showed a drug release rate of less than 10% at pH 1.2 (stomach) and more than 80% at pH 7.4 (colon) [2]
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| Toxicity/Toxicokinetics |
Compared with mucosal atrophy induced by free drugs, no obvious histological damage was observed in the colonic tissue [2]
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| References |
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| Additional Infomation |
Hydrocortisone succinate is a derivative of succinic acid, in which one of its carboxyl groups is esterified with the C-21 hydroxyl group of cortisol (hydrocortisone). It is a dicarboxylic acid monoester, hemisuccinate, and tertiary α-hydroxy ketone. Its function is related to cortisol. Hydrocortisone sodium succinate is the sodium salt of hydrocortisone succinate and possesses glucocorticoid properties. The chemical structure of hydrocortisone sodium succinate is similar to that of endogenous hormones, stimulating anti-inflammatory and immunosuppressive activity, and exhibiting mild mineralocorticoid activity. The drug binds to intracellular glucocorticoid receptors and translocates to the cell nucleus, where it initiates the transcription of glucocorticoid-responsive genes (such as various cytokines and lipocortin). Lipocortin inhibits phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and inhibiting the synthesis of prostaglandins and leukotrienes, both potent inflammatory mediators. 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, where it initiates 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.
Structural modifications improve water solubility, superior to hydrocortisone[2] In vitro immunosuppressive efficacy is lower than dexamethasone[3] |
| Molecular Formula |
C25H34O8
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|---|---|
| Molecular Weight |
462.54
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| Exact Mass |
462.225
|
| Elemental Analysis |
C, 64.92; H, 7.41; O, 27.67
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| CAS # |
2203-97-6
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| Related CAS # |
Hydrocortisone acetate;50-03-3;Hydrocortisone;50-23-7;Hydrocortisone phosphate;3863-59-0;Hydrocortisone hemisuccinate sodium;125-04-2
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| PubChem CID |
16623
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| Appearance |
White to off-white solid powder
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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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| 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 |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
908
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| Defined Atom Stereocenter Count |
7
|
| SMILES |
C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2[C@H](C[C@]4([C@H]3CC[C@@]4(C(=O)COC(=O)CCC(=O)O)O)C)O
|
| InChi Key |
VWQWXZAWFPZJDA-CGVGKPPMSA-N
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| InChi Code |
InChI=1S/C25H34O8/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)/t16-,17-,18-,22+,23-,24-,25-/m0/s1
|
| 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
|
| Synonyms |
Oralsome; Cortisol succinate; 2203-97-6; Hydrocortisone succinate; Hydrocortisone hydrogen succinate; ORISTAR HCSHS; CHEBI:31677; Hydroxycortisone succinate; NSC-7576; Hydrocortisone hemisuccinate anhydrous
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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 : ~250 mg/mL (~540.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1620 mL | 10.8099 mL | 21.6198 mL | |
| 5 mM | 0.4324 mL | 2.1620 mL | 4.3240 mL | |
| 10 mM | 0.2162 mL | 1.0810 mL | 2.1620 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.
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