4-oxo Isotretinoin
(Synonyms: 4-酮13-顺式维甲酸) 目录号 : GC49244An active metabolite of isotretinoin
Cas No.:71748-58-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
4-oxo Isotretinoin is an active metabolite of the retinoid isotretinoin .1 It is formed from isotretinoin by several cytochrome P450 (CYP450) isoforms, including CYP3A, CYP2B6, and CYP2C19.2 4-oxo Isotretinoin (10 µM) increases protein expression of cytokeratin 7 (CK7) and CK19 in normal human epidermal keratinocytes.3 It inhibits proliferation of retinoid-sensitive UM-SCC-22A and UM-SCC-35 head and neck squamous cell carcinoma (HNSCC) cells in a concentration-dependent manner.4 4-oxo Isotretinoin has been found in influent and effluent wastewater.5 It is teratogenic to mouse embryos when administered to pregnant dams at a dose of 100 mg/kg on day 11 of gestation.6
1.Colburn, W.A., Vane, F.M., and Shorter, H.J.Pharmacokinetics of isotretinoin and its major blood metabolite following a single oral dose to manEur. J. Clin. Pharmacol.24(5)689-694(1983) 2.Sonawane, P., Cho, H.E., Tagde, A., et al.Metabolic characteristics of 13-cis-retinoic acid (isotretinoin) and anti-tumour activity of the 13-cis-retinoic acid metabolite 4-oxo-13-cis-retinoic acid in neuroblastomaBr. J. Pharmacol.171(23)5330-5344(2014) 3.Baron, J.M., Heise, R., Blaner, W.S., et al.Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitroJ. Invest. Dermatol.125(1)143-153(2005) 4.Klaassen, I., Brakenhoff, R.H., Smeets, S.J., et al.Metabolism and growth inhibition of four retinoids in head and neck squamous normal and malignant cellsBr. J. Cancer85(4)630-635(2001) 5.Yeung, K.W.Y., Zhou, G.-J., HilscherovÁ, K., et al.Current understanding of potential ecological risks of retinoic acids and their metabolites in aquatic environmentsEnviron. Int.136105464(2020) 6.Kochhar, D.M., and Penner, J.D.Developmental effects of isotretinoin and 4-oxo-isotretinoin: The role of metabolism in teratogenicityTeratology36(1)67-75(1987)
Cas No. | 71748-58-8 | SDF | |
别名 | 4-酮13-顺式维甲酸 | ||
Canonical SMILES | OC(/C=C(C)\C=C\C=C(C)\C=C\C(C(C)(CC1)C)=C(C)C1=O)=O | ||
分子式 | C20H26O3 | 分子量 | 314.4 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 15 mg/ml | 储存条件 | -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 | 3.1807 mL | 15.9033 mL | 31.8066 mL |
5 mM | 0.6361 mL | 3.1807 mL | 6.3613 mL |
10 mM | 0.3181 mL | 1.5903 mL | 3.1807 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。