| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Glucocorticoid receptor (GR); acts as a GR agonist.
|
|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Unlabeled desisobutyryl ciclesonide has high affinity for the glucocorticoid receptor, producing anti-inflammatory effects by inhibiting pro-inflammatory cytokine production (e.g., IL-4, IL-5, IL-13). |
| ln Vivo |
Ciclesonide is administered via inhalation for asthma and allergic rhinitis; desisobutyryl ciclesonide is the active metabolite responsible for local anti-inflammatory activity in the lungs.
|
| Enzyme Assay |
GR binding affinity is measured by competitive binding assays using [3H]-dexamethasone and cytosolic GR preparations; specific binding is determined with excess unlabeled desisobutyryl ciclesonide.
|
| Cell Assay |
Human lung epithelial cells (e.g., A549, BEAS-2B) are treated with 0.1-1000 nM desisobutyryl ciclesonide; anti-inflammatory activity is assessed by measuring LPS-induced cytokine (IL-6, IL-8, TNF-alpha) suppression via qPCR or ELISA.
|
| Animal Protocol |
PK studies in animals or humans: biological samples (plasma, urine) are collected after ciclesonide administration; desisobutyryl ciclesonide-d11 is added as internal standard; samples are processed by protein precipitation and analyzed by LC-MS/MS.
|
| ADME/Pharmacokinetics |
Desisobutyryl ciclesonide-d11 is used as an internal standard to quantify the active metabolite in PK studies; ciclesonide has low oral bioavailability (<1%) but high lung deposition and local activity with minimal systemic exposure.
|
| Toxicity/Toxicokinetics |
Ciclesonide is well-tolerated with low systemic toxicity; potential adverse effects are those typical of inhaled glucocorticoids (oral candidiasis, dysphonia); minimal adrenal suppression due to rapid hepatic clearance of the active metabolite.
|
| References | |
| Additional Infomation |
Ciclesonide (brand name Alvesco, Omnaris) is an FDA-approved inhaled corticosteroid for asthma and allergic rhinitis; the d11-labeled version is an analytical standard and not a marketed drug.
|
| Molecular Formula |
C28H27D11O6
|
|---|---|
| Molecular Weight |
481.67
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.0761 mL | 10.3806 mL | 20.7611 mL | |
| 5 mM | 0.4152 mL | 2.0761 mL | 4.1522 mL | |
| 10 mM | 0.2076 mL | 1.0381 mL | 2.0761 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
