2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor
  3. Glucocorticoid Receptor
  4. Desisobutyryl-ciclesonide

Desisobutyryl-ciclesonide  (Synonyms: CIC-AP; Ciclesonide active principle)

Cat. No.: HY-111490 Purity: 98.84%
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Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.

For research use only. We do not sell to patients.

Desisobutyryl-ciclesonide Chemical Structure

Desisobutyryl-ciclesonide Chemical Structure

CAS No. : 161115-59-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
5 mg USD 140 In-stock
10 mg USD 190 In-stock
25 mg USD 390 In-stock
50 mg USD 550 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Desisobutyryl-ciclesonide:

Desisobutyryl-ciclesonide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Desisobutyryl-ciclesonide

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.

IC50 & Target

Glucocorticoid receptor[1]
In Vitro

Ciclesonide, an inhaled corticosteroid with almost no affinity for the glucocorticoid receptor, is highly effective in downregulating in vitro pro-inflammatory activities of airway parenchymal cells when converted into the active metabolite Desisobutyryl-ciclesonide. Peripheral blood mononuclear cell proliferation to C. albicans is dose-dependently inhibited by 0.3-3.0 μM Ciclesonide and Desisobutyryl-ciclesonide but inhibition by Desisobutyryl-ciclesonide is higher. A significant proliferation to PhlP5 is observed only in cultures from atopic subjects: an effective downregulation is already detected at 0.03 μM Ciclesonide and 0.003 μM Desisobutyryl-ciclesonide (complete inhibition at 3 μM Ciclesonide and 0.03 μM Desisobutyryl-ciclesonide). 3 μM Ciclesonide and Desisobutyryl-ciclesonide reduce the PhlP5-specific T-cell blast proliferation and interleukin 4-producing cell proportion. In PBMCs cultures from atopic patients, both Ciclesonide (CIC) and Desisobutyryl-ciclesonide (des-CIC) induce a dose-dependent downregulation of PhlP5-induced proliferation. The effect is already significantat 0.03 μM Ciclesonide and at 0.003 μM Desisobutyryl-ciclesonide (p<0.001, each comparison),with an early complete inhibition observed at 3μM Ciclesonide and at 0.03 μM Desisobutyryl-ciclesonide. The inhibitory activity toward PhlP5-induced PBMC proliferation is higher for Desisobutyryl-ciclesonide than for Ciclesonide at 0.003 μM (p<0.05), 0.03 μM (p<0.001) and 0.3 μM (p<0.05)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Desisobutyryl-ciclesonide Related Antibodies
Molecular Weight

470.60

Formula

C28H38O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@@]3(C(CO)=O)[C@@](O[C@H](O3)C4CCCCC4)([H])C[C@@]1([H])[C@]5([H])CCC6=CC(C=C[C@]6(C)[C@@]5([H])[C@@H](O)C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (212.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1249 mL 10.6247 mL 21.2495 mL
5 mM 0.4250 mL 2.1249 mL 4.2499 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.53%

COA (256 KB) HNMR (231 KB) LCMS (357 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Peripheral blood mononuclear cells are isolated from non atopic and atopic asthmatic children sensitized to Phleum pratense (PhlP5). Proliferation toward Candida albicans or PhlP5 in the presence of Ciclesonide or Desisobutyryl-ciclesonide (0.003-3.0 μM) is evaluated as [3H]thymidine incorporation. Modulation of PhlP5-specific T-cell blasts proliferation and PhlP5-induced interleukin 4 expression by Ciclesonide and Desisobutyryl-ciclesonide are measured[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1249 mL 10.6247 mL 21.2495 mL 53.1237 mL
5 mM 0.4250 mL 2.1249 mL 4.2499 mL 10.6247 mL
10 mM 0.2125 mL 1.0625 mL 2.1249 mL 5.3124 mL
15 mM 0.1417 mL 0.7083 mL 1.4166 mL 3.5416 mL
20 mM 0.1062 mL 0.5312 mL 1.0625 mL 2.6562 mL
25 mM 0.0850 mL 0.4250 mL 0.8500 mL 2.1249 mL
30 mM 0.0708 mL 0.3542 mL 0.7083 mL 1.7708 mL
40 mM 0.0531 mL 0.2656 mL 0.5312 mL 1.3281 mL
50 mM 0.0425 mL 0.2125 mL 0.4250 mL 1.0625 mL
60 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8854 mL
80 mM 0.0266 mL 0.1328 mL 0.2656 mL 0.6640 mL
100 mM 0.0212 mL 0.1062 mL 0.2125 mL 0.5312 mL
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Desisobutyryl-ciclesonide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Desisobutyryl-ciclesonide161115-59-9CIC-AP Ciclesonide active principleGlucocorticoid ReceptorInhibitorinhibitorinhibit

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