| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
| Targets |
Glucocorticoid receptor (GR)
|
|---|---|
| ln Vitro |
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] With an IC50 of 6.7 and 21.4 μM, respectively, hydrocortisone sodium hemisuccinate suppresses the biological activities of IL-6 and IL-3. It has no cytotoxic effect on MH60 cells that are IL-6-independent [3]. In T lymphocyte and peripheral lymphocyte cultures, hydrocortisone sodium hemisuccinate (0.12–60 μM; 72 hours) suppresses phytohemagglutinin (PHA) responses [3]. |
| ln Vivo |
Loaded in pH-sensitive hydrogel significantly reduced colitis symptoms in mice (DAI score 1.8 vs. 4.2 in control)[2]
In mice, oral administration of hydrocortisone sodium hemisuccinate (30 mg/kg) twice a day for five days results in decreased weight loss and increased food intake [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 |
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]
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. |
| ADME/Pharmacokinetics |
Colon-targeted hydrogel showed <10% drug release at pH 1.2 (stomach) vs. >80% at pH 7.4 (colon)[2]
|
| Toxicity/Toxicokinetics |
No significant histological damage in colon tissues vs. free drug-induced mucosal atrophy[2]
|
| References |
|
| Additional Infomation |
Hydrocortisone succinate is a derivative of succinic acid in which one of the carboxy groups is esterified by the C-21 hydroxy group of cortisol (hydrocortisone). It is a dicarboxylic acid monoester, a hemisuccinate and a tertiary alpha-hydroxy ketone. It is functionally related to a cortisol.
Hydrocortisone Sodium Succinate is the sodium salt of hydrocortisone succinate with glucocorticoid property. Hydrocortisone sodium succinate is chemically similar to the endogenous hormone that stimulates anti-inflammatory and immunosuppressive activities, in addition to exhibiting minor mineralocorticoid effects. This agent binds to intracellular glucocorticoid receptors and is translocated into the nucleus, where it initiates the transcription of glucocorticoid-responsive genes, such as various cytokines and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both potent mediators of inflammation. Hydrocortisone Hemisuccinate is the synthetic hemisuccinate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties. Hydrocortisone acetate initially binds to the cytoplasmic glucocorticoid receptor; then the receptor-ligand complex is translocated to the nucleus where it initiates the transcription of genes encoding for anti-inflammatory mediators, such as cytokines and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes. |
| Molecular Formula |
C25H33NAO8
|
|---|---|
| Molecular Weight |
484.52
|
| Exact Mass |
484.207
|
| Elemental Analysis |
C, 61.97; H, 6.87; Na, 4.74; O, 26.42
|
| CAS # |
125-04-2
|
| Related CAS # |
Hydrocortisone hemisuccinate;2203-97-6
|
| PubChem CID |
16623
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
685.5ºC at 760mmHg
|
| Flash Point |
231.1ºC
|
| Vapour Pressure |
9.36E-22mmHg at 25°C
|
| LogP |
0.862
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
33
|
| Complexity |
908
|
| 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
|
| 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 |
Hydrocortisone sodium succinate; 125-04-2; A-hydroCort; Solu-Cortef; Nositrol; Cortop; Cortisol 21-(sodium succinate); Flebocortid;
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.0639 mL | 10.3195 mL | 20.6390 mL | |
| 5 mM | 0.4128 mL | 2.0639 mL | 4.1278 mL | |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0639 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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