Acitretin-d3
(Synonyms: Ro 10-1670-d3) 目录号 : GC45762
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Acitretin-d3 is intended for use as an internal standard for the quantification of acitretin by GC- or LC-MS. Acitretin is a retinoid and an active metabolite of the retinoid etretinate that has antiproliferative activities.1,2 It binds to cellular retinoic acid binding protein I (CRABP-I) and CRABP-II (Kds = 3 and 15 nM, respectively, for the mouse recombinant proteins) but has low affinity for human recombinant retinoic acid receptor-retinoid X receptor (RAR-RXR) heterocomplexes.3,4 Acitretin inhibits proliferation (IC50 = 6.6 μM) and suppresses TNF-α- and IFN-γ-induced protein levels of STAT1, NF-•B, and RANTES in HaCaT keratinocytes when used at concentrations up to 50 μM.5 It inhibits proliferation of HL-60, SCC-4, SCC-15, and A431, but not MCF-7, cancer cells, when used at a concentration of 30 μM.1 Acitretin (20 μg per mouse) decreases the severity of psoriatic-like skin lesions in K14-VEGF transgenic mice.2 Formulations containing acitretin have been used in the treatment of psoriasis.
|1. Frey, J.R., Peck, R., and Bollag, W. Antiproliferative activity of retinoids, interferon α and their combination in five human transformed cell lines. Cancer Lett. 57(3), 223-227 (1991).|2. An, J., Zhang, D., Wu, J., et al. The acitretin and methotrexate combination therapy for psoriasis vulgaris achieves higher effectiveness and less liver fibrosis. Pharmacol. Res. 121, 158-168 (2017).|3. Norris, A.W., Cheng, L., GiguÈre, V., et al. Measurement of subnanomolar retinoic acid binding affinities for cellular retinoic acid binding proteins by fluorometric titration. Biochim. Biophys. Acta. 1209(1), 10-18 (1994).|4. Tian, K., Norris, A.W., Lin, C.L., et al. The isolation and characterization of purified heterocomplexes of recombinant retinoic acid receptor and retinoid X receptor ligand binding domains. Biochemistry 36(19), 5669-5676 (1997).|5. Zhang, M., Zhu, L., Feng, Y., et al. Effects of acitretin on proliferative inhibition and RANTES production of HaCaT cells. Arch. Dermatol. Res. 300(10), 575-581 (2008).
| Cas No. | N/A | SDF | |
| 别名 | Ro 10-1670-d3 | ||
| Canonical SMILES | CC1=C(OC([2H])([2H])[2H])C=C(C)C(/C=C/C(C)=C/C=C/C(C)=C/C(O)=O)=C1C | ||
| 分子式 | C21H23D3O3 | 分子量 | 329.5 |
| 溶解度 | Soluble 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0349 mL | 15.1745 mL | 30.349 mL |
| 5 mM | 0.607 mL | 3.0349 mL | 6.0698 mL |
| 10 mM | 0.3035 mL | 1.5175 mL | 3.0349 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。
Stability-indicating validation of acitretin and isoacitretin in human plasma by LC-ESI-MS/MS bioanalytical method and its application to pharmacokinetic analysis
Biomed Chromatogr 2011 Jun;25(6):680-8.PMID:20845366DOI:10.1002/bmc.1503
LC- ESI- MS/MS simultaneous bioanalytical method was developed to determine acitretin and its metabolite isoacitretin in human plasma using Acitretin-d3 used as the internal standard for both analytes. The compounds were extracted using protein precipitation coupled with liquid-liquid extraction with flash freezing technique. Negative mass transitions (m/z) of acitretin, isoacitretin and Acitretin-d3 were detected in multiple reactions monitoring (MRM) mode at 325.4 → 266.3, 325.2 → 266.1 and 328.3 → 266.3, respectively, with a turbo ion spray interface. The chromatographic separation was achieved on an Ascentis-RP amide column (4.6 × 150 mm, 5 µm) with mobile phase delivered in isocratic mode. The method was validated over a concentration range of 1.025-753.217 ng/mL for acitretin and 0.394-289.234 ng/mL for isoacitretin with a limit of quantification of 1.025 and 0.394 ng/mL. The intra-day and inter-day precisions were below 8.1% for acitretin and below 13.8% for isoacitretin, while accuracy was within ±7.0 and ±10.6% respectively. For the first time, the best possible conditions for plasma stability of acitretin and isoacitretin are presented and discussed with application to clinical samples.