Ciclesonide
(Synonyms: 环索奈德; RPR251526) 目录号 : GC17571A prodrug form of desisobutyryl-ciclesonide
Cas No.:126544-47-6
Sample solution is provided at 25 µL, 10mM.
Ciclesonide(RPR251526) is a glucocorticoid used to treat obstructive airway diseases.Target: Glucocorticoid ReceptorCiclesonide (CIC) is an inhaled glucocorticosteroid. CIC (5 microM) was rapidly hydrolyzed by NHBE cells (approximately 30% conversion at 4h), with almost complete conversion by 24h. In liver and NHBE cells, major involvement of cytosolic carboxylesterases, with some contribution by cholinesterases, was indicated. The highest level of conversion was found in the liver, the site of inactivation of des-CIC through rapid oxidation by cytochrome P450. Carboxylesterases in bronchial epithelial cells probably contribute significantly to the conversion to des-CIC in the target organ, whereas low systemic levels of des-CIC are a result of the high metabolic clearance by the liver following CIC inhalation [1]. Ciclesonide may have some advantage although it is not as yet licensed in all countries for paediatric use [2].
References:
[1]. Mutch, E., et al., The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochem Pharmacol, 2007. 73(10): p. 1657-64.
[2]. Barnes, N.C., The properties of inhaled corticosteroids: similarities and differences. Prim Care Respir J, 2007. 16(3): p. 149-54.
Cas No. | 126544-47-6 | SDF | |
别名 | 环索奈德; RPR251526 | ||
化学名 | 2-((6aR,6bS,7S,8aS,8bS,10R,11aR,12aS,12bS)-10-cyclohexyl-7-hydroxy-6a,8a-dimethyl-4-oxo-2,4,6a,6b,7,8,8a,8b,11a,12,12a,12b-dodecahydro-1H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-8b-yl)-2-oxoethyl isobutyrate | ||
Canonical SMILES | CC(C(OCC([C@@]12[C@@](O[C@@](O2)([H])C3CCCCC3)([H])C[C@@]4([H])[C@]([C@]5([H])[C@](O)([H])C[C@@]41C)([H])CCC6=CC(C=C[C@@]65C)=O)=O)=O)C | ||
分子式 | C32H44O7 | 分子量 | 540.69 |
溶解度 | ≥ 15.8mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.8495 mL | 9.2474 mL | 18.4949 mL |
5 mM | 0.3699 mL | 1.8495 mL | 3.699 mL |
10 mM | 0.1849 mL | 0.9247 mL | 1.8495 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
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