Size | Price | Stock | Qty |
---|---|---|---|
50mg |
|
||
100mg |
|
||
Other Sizes |
|
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].
|
---|---|
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].
|
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. |
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 |
C25H34O8
|
---|---|
Molecular Weight |
462.54
|
Exact Mass |
462.225
|
CAS # |
2203-97-6
|
Related CAS # |
Hydrocortisone acetate;50-03-3;Hydrocortisone;50-23-7;Hydrocortisone phosphate;3863-59-0;Hydrocortisone hemisuccinate sodium;125-04-2
|
PubChem CID |
16623
|
Appearance |
White to off-white solid powder
|
Density |
1.3±0.1 g/cm3
|
Boiling Point |
685.5±55.0 °C at 760 mmHg
|
Flash Point |
231.1±25.0 °C
|
Vapour Pressure |
0.0±4.8 mmHg at 25°C
|
Index of Refraction |
1.587
|
LogP |
2.13
|
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 |
Oralsome; Cortisol succinate; Hydrocortisone hemisuccinate anhydrous
|
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) |
DMSO : ~250 mg/mL (~540.51 mM)
|
---|---|
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.