Isotretinoin(Synonyms: 异维A酸; 13-cis-Retinoic acid)

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Isotretinoin (Synonyms: 异维A酸; 13-cis-Retinoic acid) 纯度: 99.88%

Isotretinoin(13-cis-Retinoic acid)可作用于重度粉刺,还可用于脑癌,胰腺癌等化疗。

Isotretinoin(Synonyms: 异维A酸; 13-cis-Retinoic acid)

Isotretinoin Chemical Structure

CAS No. : 4759-48-2

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Isotretinoin 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus

生物活性

Isotretinoin(13-cis-Retinoic acid) is a medication used for the treatment of severe acne. It was first developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more. Target: RAR/RXR Isotretinoin has been the most effective and long-lasting drug for the treatment of severe acne for more than 30 years and can achieve long-term remission in 70-80% of patients after a single course. The new evidence-based European S3-guideline recommends the use of Isotretinoin as a first-line medication for the treatment of severe papulopustular or conglobate acne, especially when prognostically unfavorable factors are present: family history of acne, early onset, marked seborrhea, localization on the trunk, scarring, psychosocial disability or persistent/late-type acne [1]. Five patients with pityriasis rubra pilaris were treated with isotretinoin from September 1982 through 1985. Isotretinoin at an average dose of 1.16 mg/kg/day for 16 to 24 weeks caused complete or almost complete clearing in four of the five patients [2]. isotretinoin produces significant anti-inflammatory effects by inhibition of monocyte and neutrophil chemotaxis across intact biologic barriers in vivo [3]. Isotretinoin 5 mg/day is effective in reducing the number of acne lesions, and improving patients dermatologic quality of life, with minimal adverse effects [4]. Clinical indications: Acne Toxicity: Isotretinoin is teratogenic. It also causes mucocutaneous side effects suck as cheilitis, dry skin, and dry eyes.

IC50 & Target

Human Endogenous Metabolite

 

Clinical Trial

分子量

300.44

Formula

C20H28O2

CAS 号

4759-48-2

中文名称

异维甲酸;异曲替酯;β顺式维甲酸;异维A酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (166.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3285 mL 16.6423 mL 33.2845 mL
5 mM 0.6657 mL 3.3285 mL 6.6569 mL
10 mM 0.3328 mL 1.6642 mL 3.3285 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.32 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.32 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.92 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Thielitz, A. and H. Gollnick, [Isotretinoin. How should it be used?]. Hautarzt, 2013. 64(4): p. 263-8.

    [2]. Norris, D.A., et al., Isotretinoin produces significant inhibition of monocyte and neutrophil chemotaxis in vivo in patients with cystic acne. J Invest Dermatol, 1987. 89(1): p. 38-43.

    [3]. Rademaker, M., J.M. Wishart, and N.M. Birchall, Isotretinoin 5 mg daily for low-grade adult acne vulgaris – a placebo-controlled, randomized double-blind study. J Eur Acad Dermatol Venereol, 2013.

    [4]. Dicken, C.H., Isotretinoin treatment of pityriasis rubra pilaris. J Am Acad Dermatol, 1987. 16(2 Pt 1): p. 297-301.

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