Desisobutyryl-ciclesonide-CIC-AP-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDesisobutyryl-ciclesonideCat. No.: HY-111490CAS No.: 161115-59-9Synonyms: CIC-AP; Ciclesonide active principle分式: CHO分量: 470.6作靶点: Glucocorticoid Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mon

2、ths-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (106.25 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1249 mL 10.6247 mL 21.2495 mL5 mM 0.4250 mL 2.1249 mL 4.2499 mL10 mM 0.2125 mL 1.0625 mL 2.1249 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物

3、和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.31 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.31 mM); C

4、lear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.31 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Desisobutyryl-ciclesonideCiclesonide 的活性代谢产物。Desisobutyryl-ciclesonide 对糖质激素受体 (glucocorticoid receptor) 具有亲和。IC50 & Target Glucocort

5、icoid receptor 1体外研究 Ciclesonide, an inhaled corticosteroid with almost no affinity for the glucocorticoid receptor, is highly effectivein downregulating in vitro pro-inflammatory activities of airway parenchymal cells when converted into theactive metabolite Desisobutyryl-ciclesonide. Peripheral bl

6、ood mononuclear cell proliferation to C. albicans isdose-dependently inhibited by 0.3-3.0 M Ciclesonide and Desisobutyryl-ciclesonide but inhibition byDesisobutyryl-ciclesonide is higher. A significant proliferation to PhlP5 is observed only in cultures fromatopic subjects: an effective downregulati

7、on is already detected at 0.03 M Ciclesonide and 0.003 MDesisobutyryl-ciclesonide (complete inhibition at 3 M Ciclesonide and 0.03 M Desisobutyryl-ciclesonide). 3M Ciclesonide and Desisobutyryl-ciclesonide reduce the PhlP5-specific T-cell blast proliferation andinterleukin 4-producing cell proportio

8、n. In PBMCs cultures from atopic patients, both Ciclesonide (CIC) andDesisobutyryl-ciclesonide (des-CIC) induce a dose-dependent downregulation of PhlP5-induced proliferation.The effect is already significantat 0.03 M Ciclesonide and at 0.003 M Desisobutyryl-ciclesonide (pPhlP5-induced PBMC prolifer

9、ation is higher for Desisobutyryl-ciclesonide than for Ciclesonide at 0.003 M (p 1.PROTOCOLCell Assay 1 Peripheral blood mononuclear cells are isolated from non atopic and atopic asthmatic children sensitized toPhleum pratense (PhlP5). Proliferation toward Candida albicans or PhlP5 in the presence o

10、f Ciclesonide orDesisobutyryl-ciclesonide (0.003-3.0 M) is evaluated as 3Hthymidine incorporation. Modulation of PhlP5-specific T-cell blasts proliferation and PhlP5-induced interleukin 4 expression by Ciclesonide andDesisobutyryl-ciclesonide are measured 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Silvestri M, et al. Ciclesonide modulates in vitro allergen-driven activation of blood mononuclear cells and allergen-specific T-cell blasts.Immunol Lett. 2012 Jan 30;141(2):190-6.McePdfHeightCaution: Product has not bee