Glucocorticoid receptor (GR)

Hydrocortisone phosphate has no lethal effect on MH60 cells that are IL-6-independent, but it inhibits the biological activities of IL-6 and IL-3 with IC50s of 6.7 and 21.4 μM, respectively [3]. PHA responses in peripheral lymphocyte (PBL) and T lymphocyte cultures are inhibited by hydrocortisone phosphate (0.12-60 μM; 72 hours) [3].

In mice, oral hydrocortisone phosphate (30 mg/kg) given twice a day for five days decreases weight loss and enhances food intake [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.

Absorption, Distribution and Excretion
Topical corticosteroids are absorbed through normal, intact skin. Skin inflammation and/or other conditions can increase percutaneous absorption. Corticosteroids are primarily metabolized in the liver and then excreted via the kidneys. Some topical corticosteroids and their metabolites are also excreted via bile. Metabolism/Metabolites Primarily metabolized in the liver via CYP3A4. Biological Half-Life 6-8 hours

Protein Binding
95%

[1]. Inhibitory effects of anti-inflammatory drugs on interleukin-6 bioactivity. Biol Pharm Bull. 2001 Jun;24(6):701-3.

[2]. In vitro and in vivo application of pH-sensitive colon-targeting polysaccharide hydrogel used for ulcerative colitis therapy. Carbohydr Polym. 2015 Oct 5;130:243-53.

[3]. The immunosuppressive potency in vitro of physiological and synthetic steroids on lymphocyte cultures. Int J Immunopharmacol. 1987;9(4):469-73.

Cortisol phosphate is a steroidal phosphate, a 21-O-phosphate derivative of cortisol. It is a cortisol ester, steroidal phosphate, 11β-hydroxysteroid, 3-oxo-Δ⁴steroid, 17α-hydroxysteroid, and tertiary α-hydroxy ketone. It is the conjugate acid of cortisol phosphate (2-). Pharmacological Indications: Used to relieve inflammatory and pruritus symptoms of corticosteroid-sensitive skin diseases. Also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addison's disease). It is also used to treat various immune and allergic diseases, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease. Mechanism of Action: Hydrocortisone binds to cytoplasmic glucocorticoid receptors. After binding to the receptor, the newly formed receptor-ligand complex translocates to the nucleus and binds to multiple glucocorticoid response elements (GREs) in the promoter region of target genes. DNA-binding receptors then interact with basic transcription factors, leading to increased expression of specific target genes. The anti-inflammatory effects of corticosteroids are thought to be related to lipocortin, a phospholipase A2 inhibitor that controls the biosynthesis of prostaglandins and leukotrienes by inhibiting arachidonic acid. Specifically, glucocorticoids induce the synthesis of lipocortin-1 (annexin-1), which binds to the cell membrane, preventing phospholipase A2 from contacting its substrate, arachidonic acid. This results in reduced arachidonic acid production. The expression of cyclooxygenases (COX-1 and COX-2) is also inhibited, thereby enhancing the above effects. In other words, both major products of inflammation—prostaglandins and leukotrienes—are inhibited by glucocorticoids. Glucocorticoids can also stimulate lipocortin-1 to escape into the extracellular space. Lipocortictin-1 binds to leukocyte membrane receptors, inhibiting various inflammatory responses, including epithelial cell adhesion, migration, chemotaxis, phagocytosis, respiratory burst, and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines, etc.) from neutrophils, macrophages, and mast cells. Furthermore, glucocorticoids suppress the immune system through mechanisms including decreased lymphatic system function, reduced immunoglobulin and complement concentrations, lymphopenia, and interference with antigen-antibody binding.

C21H31O8P

442.43984

442.176

3863-59-0

Hydrocortisone 17-butyrate;13609-67-1;Hydrocortisone acetate;50-03-3;Hydrocortisone 17-valerate;57524-89-7;Hydrocortisone hemisuccinate;2203-97-6;Hydrocortisone;50-23-7; 6000-74-4

441407

Typically exists as solid at room temperature

1.42g/cm3

669.9ºC at 760mmHg

358.9ºC

1.596

1.898

4

8

4

30

848

7

C[C@@]12[C@](C(COP(O)(O)=O)=O)(O)CC[C@@]1([H])[C@]3([H])CCC4=CC(CC[C@]4(C)[C@@]3([H])[C@@H](O)C2)=O

BGSOJVFOEQLVMH-VWUMJDOOSA-N

InChI=1S/C21H31O8P/c1-19-7-5-13(22)9-12(19)3-4-14-15-6-8-21(25,17(24)11-29-30(26,27)28)20(15,2)10-16(23)18(14)19/h9,14-16,18,23,25H,3-8,10-11H2,1-2H3,(H2,26,27,28)/t14-,15-,16-,18+,19-,20-,21-/m0/s1

[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-oxoethyl] dihydrogen phosphate

Hydrocortisone phosphate; 3863-59-0; Cortisol 21-phosphate; Hydrocortisone 21-phosphate; 2Y87E22X71; DTXSID7048160; NSC-529660; PREGN-4-ENE-3,20-DIONE, 11,17-DIHYDROXY-21-(PHOSPHONOOXY)-;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)