Desoxycorticosterone pivalate targets the mineralocorticoid receptor (MR). As a pure mineralocorticoid, its mechanism of action involves acting as a mineralocorticoid, which is crucial for sodium retention, potassium excretion, and water balance in the body. It mimics the action of endogenous aldosterone.

In vitro, desoxycorticosterone pivalate is characterized as a mineralocorticoid receptor agonist. It binds to the mineralocorticoid receptor and activates downstream signaling pathways involved in electrolyte and water homeostasis. Its activity is similar to that of aldosterone, the primary endogenous mineralocorticoid.

For the majority of dogs with PH, a beginning dose of 1.5 mg/kg of deoxycorticosterone pivalate (DOCP) effectively controls clinical symptoms and serum electrolyte concentrations. Additional dose reductions are frequently needed to maintain an injection interval of 28-30 days. Animals that are growing and young seem to need bigger amounts [1].
In vivo, desoxycorticosterone pivalate is used for the management of canine hypoadrenocorticism (Addison's disease). A starting dosage of 1.5 mg/kg is effective in controlling clinical signs and serum electrolyte concentrations in the majority of dogs with primary hypoadrenocorticism. It effectively restores electrolyte balance by maintaining sodium and potassium homeostasis.

In vitro assays for desoxycorticosterone pivalate typically involve measuring its binding affinity for the mineralocorticoid receptor. Radioligand binding studies using ³H-aldosterone are performed on membranes from cells expressing the receptor. Functional assays measure its ability to activate mineralocorticoid receptor-mediated transcription using reporter gene assays.

For in vitro cell-based assays, cells expressing the mineralocorticoid receptor are cultured and treated with desoxycorticosterone pivalate at various concentrations. Receptor activation is confirmed by measuring the expression of mineralocorticoid receptor target genes via qRT-PCR. Cell viability is assessed by standard assays.

In vivo animal studies with desoxycorticosterone pivalate are conducted in dogs with hypoadrenocorticism. The compound is administered intramuscularly as a microcrystalline suspension. Serum electrolyte concentrations (sodium, potassium) and clinical signs are monitored. The compound's efficacy in restoring electrolyte balance has been demonstrated.

Desoxycorticosterone pivalate (CAS: 808-48-0) has a molecular weight of 414.58 g/mol and a molecular formula of C26H38O4. Appearance: white, odorless, stable in air. Solubility: sparingly soluble in acetone, slightly soluble in methanol, ether and vegetable oils. Storage: room temperature.

Protein Binding
90%
Desoxycorticosterone pivalate is an approved veterinary drug with an established safety profile. In dogs, it is generally well-tolerated at therapeutic doses. Overdose may cause electrolyte imbalances. It is contraindicated in animals with hypersensitivity to the compound. It is not approved for human use.

[1]. Evaluation of a low-dose desoxycorticosterone pivalate treatment protocol for long-term management of dogs with primary hypoadrenocorticism. J Vet Intern Med. 2019 May;33(3):1266-1271.

[2]. Masticatory Muscle Myositis: Pathogenesis, Diagnosis, and Treatment.

11-Deoxycorticosterone neovalerate is a neovalerate, belonging to the mineralocorticoid class. Its function is related to corticosterone. Deoxycorticosterone neovalerate is a mineralocorticoid and an analogue of deoxycorticosterone. It is white, odorless, and stable in air. It is practically insoluble in water, slightly soluble in acetone, and slightly soluble in methanol, ether, and vegetable oils. Under US federal law, this drug can only be used by a licensed veterinarian or under their guidance. See also: Deoxycorticosterone (containing the active moiety). Indications: For the treatment of adrenocortical insufficiency, particularly multiple sclerosis, congenital cerebral palsy, polyarteritis nodosa, and rheumatoid arthritis. Currently approved only for the treatment of Addison's disease in cats and dogs. For the treatment of mineralocorticoid deficiency caused by primary adrenocortical insufficiency (Addison's disease) in dogs. Mechanism of Action: Deoxycorticosterone pitava binds to mineralocorticoid receptors. Mineralocorticoids are a class of steroid hormones secreted by the adrenal cortex, crucial for a variety of metabolic processes, including electrolyte regulation. Deoxycorticosterone pitavaate exerts its effects by interacting with the mineralocorticoid receptor (MR), forming a steroid-receptor complex with the receptor protein. This complex enters the cell nucleus, binds to chromatin, and initiates the transcription of cellular DNA into messenger RNA. Steroid hormones appear to induce the transcription and synthesis of specific proteins, thus producing the physiological effects observed after administration.

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Pharmacodynamics
Deoxycorticosterone pitavaate, used to treat adrenal insufficiency, is a mineralocorticoid and an analogue of deoxycorticosterone. It primarily acts on the metabolism of sodium, potassium, and water. After administration, sodium excretion decreases, and potassium excretion increases; therefore, the concentration of sodium in the blood increases, while the concentration of potassium decreases. Simultaneously, the volume of blood and extracellular fluid increases, and the hematocrit decreases. It also increases the reabsorption rate of sodium in the renal tubules.
Desoxycorticosterone pivalate (DOCP) is a long-acting injectable mineralocorticoid receptor agonist used in veterinary medicine for the management of Addison's disease in dogs. It is a synthetic steroid that acts as a pure mineralocorticoid. It is an approved veterinary drug in many countries.

C26H38O4

414.58

414.277

808-48-0

808-48-0 (pivalate);56-47-3 (acetate);

11876263

White to off-white solid powder

1.111 g/cm3

529.012ºC at 760 mmHg

198-204ºC

1.534

5.292

0

4

5

30

787

6

C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)COC(=O)C(C)(C)C)CCC4=CC(=O)CC[C@]34C

VVOIQBFMTVCINR-WWMZEODYSA-N

InChI=1S/C26H38O4/c1-24(2,3)23(29)30-15-22(28)21-9-8-19-18-7-6-16-14-17(27)10-12-25(16,4)20(18)11-13-26(19,21)5/h14,18-21H,6-13,15H2,1-5H3/t18-,19-,20-,21+,25-,26-/m0/s1

[2-[(8S,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 2,2-dimethylpropanoate

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)

DMSO : ~5 mg/mL (~12.06 mM)

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.)