| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Dichlorisone acetate functions as a glucocorticoid receptor (GR) agonist. It diffuses across cell membranes and binds to the cytosolic GR. The ligand-receptor complex then translocates to the nucleus, where it modulates gene transcription, leading to the suppression of pro-inflammatory mediators and the induction of anti-inflammatory proteins. It also exhibits binding affinity for the mineralocorticoid receptor (NR3C2) and other receptors.
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| ln Vitro |
Dichlorisone acetate exerts its primary effect as a potent anti-inflammatory agent in vitro. Its activity is linked to its interaction with the glucocorticoid receptor and downstream signaling pathways. It has also demonstrated antiviral activity, showing inhibition of SARS-CoV-2-induced cytotoxicity in Caco-2 cells at 10 µM. Its specific IC₅₀ for various targets is available in bioactivity databases.
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| ln Vivo |
In vivo, dichlorisone acetate is used for its anti-inflammatory properties. It is applied topically to treat inflammatory and allergic conditions. Its activity is mediated through the glucocorticoid receptor. The compound has also been studied for its effects on metabolic disorders and has been used as an internal standard in analytical methods for quantifying glucocorticoids in equine plasma.
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| Enzyme Assay |
In vitro receptor binding assays are used to characterize its affinity for the glucocorticoid receptor and other nuclear receptors. These assays typically involve competitive binding studies using radiolabeled ligands and membrane preparations from cells expressing the target receptor. Functional assays measure GR-mediated transcriptional activity using reporter genes in cell lines.
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| Cell Assay |
Dichlorisone acetate is used in cell culture to study glucocorticoid signaling. It is typically applied to cells at micromolar concentrations. Its anti-inflammatory effects are assessed by measuring the production of inflammatory cytokines and other mediators. Its antiviral activity has been evaluated in Caco-2 cells.
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| Animal Protocol |
In vivo animal studies for dichlorisone acetate are not extensively documented in the provided literature. It has been used in research related to alopecia and as a standard in analytical studies. Toxicological studies have been conducted to assess its safety profile.
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| ADME/Pharmacokinetics |
Published pharmacokinetic data for dichlorisone acetate is limited. The compound has a molecular weight of 455.37 g/mol and is soluble in DMSO. It is a synthetic corticosteroid, and its pharmacokinetic properties are expected to be similar to other topical glucocorticoids, with absorption through the skin and metabolism in the liver.
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| Toxicity/Toxicokinetics |
The toxicological profile of dichlorisone acetate is characteristic of topical corticosteroids. Common local side effects include burning, stinging, and dryness. Prolonged use can lead to systemic absorption and adrenal suppression. The compound is considered a hazardous substance and should be handled with appropriate safety precautions.
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| Additional Infomation |
Dichlorisone is a corticosteroid hormone.
Dichlorisone acetate is a synthetic glucocorticoid corticosteroid used as an anti-inflammatory agent. It is also known as Diloderm and Dermocid. It is not approved for systemic use in humans and is primarily a research tool for studying glucocorticoid receptor signaling and inflammation. |
| Molecular Formula |
C23H28O5CL2
|
|---|---|
| Molecular Weight |
455.37142
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| Exact Mass |
454.131
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| CAS # |
79-61-8
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| Related CAS # |
7008-26-6;79-61-8 (acetate);
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| PubChem CID |
5388959
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| Appearance |
White to off-white solid powder
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| Density |
1.34g/cm3
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| Boiling Point |
596.2ºC at 760 mmHg
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| Flash Point |
314.4ºC
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| Index of Refraction |
1.585
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| LogP |
3.736
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
881
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| Defined Atom Stereocenter Count |
7
|
| SMILES |
CC(=O)OCC(=O)[C@]1(CC[C@@H]2[C@@]1(C[C@@H]([C@]3([C@H]2CCC4=CC(=O)C=C[C@@]43C)Cl)Cl)C)O
|
| InChi Key |
YNNURTVKPVJVEI-GSLJADNHSA-N
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| InChi Code |
InChI=1S/C23H28Cl2O5/c1-13(26)30-12-19(28)22(29)9-7-16-17-5-4-14-10-15(27)6-8-20(14,2)23(17,25)18(24)11-21(16,22)3/h6,8,10,16-18,29H,4-5,7,9,11-12H2,1-3H3/t16-,17-,18-,20-,21-,22-,23-/m0/s1
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| Chemical Name |
[2-[(8S,9R,10S,11S,13S,14S,17R)-9,11-dichloro-17-hydroxy-10,13-dimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate
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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 |
| 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) |
DMSO : ~4.35 mg/mL (~9.55 mM)
H2O : < 0.1 mg/mL |
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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 | 2.1960 mL | 10.9801 mL | 21.9602 mL | |
| 5 mM | 0.4392 mL | 2.1960 mL | 4.3920 mL | |
| 10 mM | 0.2196 mL | 1.0980 mL | 2.1960 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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