| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
The molecular target is the glucocorticoid receptor (GR), where hydrocortisone acts as a high-affinity agonist; it also binds the mineralocorticoid receptor with lower affinity, contributing to sodium retention and potassium excretion, and it activates anti-inflammatory transcription while suppressing NF-κB and AP-1 signaling.
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|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
In vitro, hydrocortisone-d2 binds GR with high affinity, activates glucocorticoid-responsive reporter gene expression, and suppresses LPS-induced NF-κB activation and proinflammatory cytokine production in macrophages and lymphocytes; the deuterated form retains GR agonist activity while enabling LC-MS/MS quantification. |
| ln Vivo |
In vivo, hydrocortisone-d2 restores glucocorticoid activity in adrenalectomized animals, suppresses inflammation in adjuvant arthritis and carrageenan paw edema models, and regulates glucose metabolism and vascular tone; the labeled form is used to quantify plasma and tissue concentrations and GR occupancy.
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| Enzyme Assay |
Noncellular binding assays incubate recombinant human GR ligand-binding domain or rat thymus cytosol with [3H]dexamethasone and increasing concentrations of hydrocortisone-d2; bound and free radioligand are separated by hydroxyapatite or filtration, and IC50 and Ki values are calculated to quantify GR affinity and selectivity over the mineralocorticoid receptor.
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| Cell Assay |
Cellular transactivation assays use COS-7 or A549 cells transfected with GR and a glucocorticoid-responsive luciferase reporter; hydrocortisone-d2 is tested for agonist potency, and NF-κB inhibition is assessed in LPS-stimulated macrophages by p65 immunoblotting and cytokine ELISA.
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| Animal Protocol |
Animal protocols administer hydrocortisone-d2 orally or intravenously to adrenalectomized rats or mice with adjuvant arthritis or carrageenan paw edema at doses of 1–50 mg/kg; inflammation scores, glucose levels, and electrolyte balance are measured, and plasma and tissue concentrations are quantified by LC-MS/MS to relate GR occupancy to metabolic and anti-inflammatory effects.
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| References |
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| Molecular Formula |
C21H30O5
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|---|---|
| Molecular Weight |
362.459907054901
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| Exact Mass |
364.221
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| CAS # |
1257650-73-9
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| Related CAS # |
Hydrocortisone;50-23-7
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| PubChem CID |
71309567
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| Appearance |
White to off-white solid
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| LogP |
1.6
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| tPSA |
94.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
684
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| Defined Atom Stereocenter Count |
7
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| SMILES |
[2H]C1C([C@@]2([C@@H]3[C@@H](CCC2=CC1=O)[C@@H]4CC[C@@]([C@]4(C[C@@H]3O)C)(C(=O)CO)O)C)[2H]
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| InChi Key |
JYGXADMDTFJGBT-VFWCAETDSA-N
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| InChi Code |
InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1/i5D,7D/t5?,7?,14-,15-,16-,18+,19-,20-,21-
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| Chemical Name |
(8S,9S,10R,11S,13S,14S,17R)-1,2-dideuterio-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
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. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 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
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|---|---|
| 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 | 2.7589 mL | 13.7946 mL | 27.5893 mL | |
| 5 mM | 0.5518 mL | 2.7589 mL | 5.5179 mL | |
| 10 mM | 0.2759 mL | 1.3795 mL | 2.7589 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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