Glucocorticoid receptor [1,2]

- Effect on embryo development: Hydrocortisone acetate affects the development of mouse embryos. It can cause macroscopic - visible dilatation of the venous marginal blood sinus of the foot plates in mouse embryos. It may also lead to other developmental abnormalities, interfering with normal limb development [1]
- Effect on immunoglobulin metabolism: In normal and low - pathogen mice, Hydrocortisone acetate reduces the serum concentration of all sub - classes of IgG (γ2a, γ2b, and γ1), as well as IgA and IgM. Turnover studies using 131I - labeled γ2a subclass of IgG show that high - dose corticosteroids cause a significantly shortened survival (increased catabolic rate) of IgG, contributing to hypogammaglobulinemia. The increase in fractional catabolism is due to an increase in endogenous catabolism, not excess loss in the urine or stool [2]

- Embryo development experiment: Pregnant mice were injected with Hydrocortisone acetate at a certain dose during pregnancy. The specific injection dose and frequency are not mentioned in the literature. After a certain period, the embryos were isolated, and the morphological changes of the embryos were observed, especially the development of the foot plates, to assess the impact of Hydrocortisone acetate on embryo development [1]
- Immunoglobulin metabolism experiment: Normal and low - pathogen mice were given Hydrocortisone acetate, and the administration route, dose, and frequency are not mentioned in the literature. Blood samples were taken at different time points, and the serum concentrations of IgG sub - classes, IgA, and IgM were measured. 131I - labeled γ2a subclass of IgG was used for turnover studies, and the catabolic rate of IgG was calculated by detecting the radioactivity in the blood [2]
- Additional Info - Hydrocortisone acetate is a corticosteroid drug. Its mechanism of action may be related to binding to the glucocorticoid receptor, regulating gene expression, and then affecting various physiological processes. It has a cell - stabilizing effect, which can stabilize lipoprotein membranes and prevent lysosomes from releasing hydrolytic enzymes. However, in some cases, it may also delay the repair of cellular injury, possibly due to the stimulation of the synthesis of enzymes deaminating amino acids [1]

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% 5744 Rat Subcutaneous Injection LD50 250 mg/kg Arzneimittel-Forschung. Drug Research., 27(2102), 1977 [PMID:580008] 5744 Mouse Intraperitoneal Injection LD50 2300 mg/kg Compilation of LD50 Values of New Drugs. 5744 Mouse Subcutaneous Injection LD50 45050 ug/kg National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program., JAN1986

[1]. The effect of hydrocortisone acetate on the development of mouse embryos. J Embryol Exp Morphol. 1968 Nov;20(3):355-66.
[2]. The effect of hydrocortisone on immunoglobulin metabolism. J Clin Invest. 1970 Sep;49(9):1679-84.

21-Cardiolide acetate is a tertiary α-hydroxy ketone and also a cortisol ester. Hydrocortisone acetate is the synthetic acetate 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 the transcription of genes encoding anti-inflammatory mediators such as cytokines and lipocortin. Lipocorticoids inhibit phospholipase A2, thereby preventing the release of arachidonic acid from membrane phospholipids and inhibiting the synthesis of prostaglandins and leukotrienes. See also: Hydrocortisone acetate; Promocaine hydrochloride (ingredient); Hydrocortisone acetate; Neomycin sulfate (ingredient); Chloramphenicol; Hydrocortisone acetate (ingredient)... See more...

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Drug Indications
For the relief of inflammatory and pruritus symptoms in corticosteroid-responsive dermatitis.
It is also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addison's disease). In addition, it is used to treat a variety of immune and allergic diseases, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.

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Mechanism of Action
Hydrocortisone binds to cytoplasmic glucocorticoid receptors. After binding to the receptor, the newly formed receptor-ligand complex translocates to the cell nucleus and binds to multiple glucocorticoid response elements (GREs) in the promoter regions of target genes. The DNA-bound receptor then interacts with basic transcription factors, leading to increased expression of specific target genes. The anti-inflammatory effect of glucocorticoids is thought to be related to lipocortin, a phospholipase A2 inhibitory protein that controls the biosynthesis of prostaglandins and leukotrienes by inhibiting arachidonic acid. Specifically, glucocorticoids induce the synthesis of lipocortin-1 (annexin-1), which then 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 this effect. In other words, the two main products of inflammation—prostaglandins and leukotrienes—are suppressed 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. In addition, glucocorticoids suppress the immune system through mechanisms including decreased lymphatic system function, reduced immunoglobulin and complement concentrations, lymphopenia, and interference with antigen-antibody binding.

C23H32O6

404.4966

404.219

C, 68.29; H, 7.97; O, 23.73

50-03-3

Hydrocortisone 17-butyrate;13609-67-1;Hydrocortisone 17-valerate;57524-89-7;Hydrocortisone hemisuccinate;2203-97-6;Hydrocortisone;50-23-7;Hydrocortisone phosphate;3863-59-0

5744

White to light yellow solid powder

1.3±0.1 g/cm3

576.6±50.0 °C at 760 mmHg

223 °C (dec.)(lit.)

196.2±23.6 °C

0.0±3.6 mmHg at 25°C

1.573

2.51

2

6

4

29

786

7

CC(=O)OCC(=O)[C@]1(CC[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)CC[C@]34C)O)C)O

ALEXXDVDDISNDU-JZYPGELDSA-N

InChI=1S/C23H32O6/c1-13(24)29-12-19(27)23(28)9-7-17-16-5-4-14-10-15(25)6-8-21(14,2)20(16)18(26)11-22(17,23)3/h10,16-18,20,26,28H,4-9,11-12H2,1-3H3/t16-,17-,18-,20+,21-,22-,23-/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] acetate

hydrocortisone acetate; 50-03-3; Cortisol 21-acetate; Hydrocortisone 21-acetate; Cortell; Cortifoam; Cortef acetate; Cortisol acetate;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

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

DMSO : ≥ 38 mg/mL (~93.94 mM)
H2O : ~1 mg/mL (~2.47 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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