Tretinoin (Aberela)
(Synonyms: 维生素A酸; Vitamin A acid; all-trans-Retinoic acid; ATRA) 目录号 : GC18147
A vitamin A metabolite and RAR ligand
Cas No.:302-79-4
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
| Cell experiment [1]: | |
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Cell lines |
Mesangial cell |
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Preparation Method |
Mesangial cells were treated with Tretinoin (Aberela) at different concentrations. |
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Reaction Conditions |
0 ~ 25 µm Tretinoin (Aberela); 0 to 24 hours |
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Applications |
Tretinoin (Aberela) increased catalase activity and decreased glutathione levels in a dose-and time-dependent manner, thereby preventing H2O2 -induced cell injury. In glomerular mesangial cells, Tretinoin (Aberela) increased catalase mRNA and γ-glutamylcysteine synthetase (catalytic subunit) mRNA levels. |
| Animal experiment [2]: | |
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Animal models |
Male Fischer 344 rats |
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Preparation Method |
The difference between the control group and the experimental group(Tretinoin (Aberela)) was observed |
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Dosage form |
1 mg/kg/day Tretinoin (Aberela); Oral medicine |
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Applications |
In male Fischer 344 rats, Tretinoin (Aberela) at 1 mg/kg/day did not cause any toxic effects. Renal cortical protein levels were lower in Tretinoin (Aberela) -treated rats than in control animals of comparable age. |
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References: [1]: Manzano VM, Puyol MR, et,al. Tretinoin prevents age-related renal changes and stimulates antioxidant defenses in cultured renal mesangial cells. J Pharmacol Exp Ther. 1999 Apr;289(1):123-32. PMID: 10086995. |
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Tretinoin (Aberela) is a vitamin A-derived, non-peptidic, small lipophilic molecule that acts as ligand for nuclear RA receptors (RARs), converting them from transcriptional repressors to activators[5].
In cultured human mesangial cells, Tretinoin (Aberela) increased the reduced glutathione content and the catalase activity in a dose- and time-dependent way, which then prevented the cytotoxicity of H2O2 [1].A549 cells were incubated with free Tretinoin (Aberela) (TTN), blank nanocapsules (LNC) and Tretinoin (Aberela) -loaded lipid-core nanocapsules (TTN-LNC). TTN-LNC induced apoptosis and cell cycle arrest at the G1-phase while TTN did not. TTN-LNC showed higher cytotoxic effects than TTN on A549 cells evaluated[4].The combination of As-ODN-hTR and All-trans Tretinoin (Aberela) has a synergistic anti-tumor effect. This anti-tumor effect can be mainly attributed to apoptosis induced by a decrease in telomerase activity. Bcl-2 plays an important role in this process [7].
In male nmri mice, Tretinoin (Aberela) significantly inhibited cellular immunity and increased humoral immunity. Tretinoin (Aberela) decreased lymphocyte proliferation, decreased NBT, and interleukin-17 secretion, but increased interleukin-10 secretion [2]. In patients with facial acne, clindamycin phosphate Tretinoin (Aberela) Gel (CTG) (1.2% clindamycin phosphate, 0.025% Tretinoin (Aberela) in a gel base (Velac)) was significantly more effective than 0.025% Tretinoin (Aberela), which relayed on the anti-inflammatory efficacy of Tretinoin (Aberela) [3].The delivery of Tretinoin (Aberela) by polymeric micelles prolonged the blood circulation and enhanced the accumulation of Tretinoin (Aberela) in the tumor tissue compared with the administration of free Tretinoin (Aberela). Tumor growth was significantly delayed and the survival time of mice was prolonged following the treatment by Tretinoin (Aberela) polymeric micelles demonstrating the improved anticancer activity of Tretinoin (Aberela) [6].
References:
[1]: Manzano VM, Puyol MR, et,al. Tretinoin prevents age-related renal changes and stimulates antioxidant defenses in cultured renal mesangial cells. J Pharmacol Exp Ther. 1999 Apr;289(1):123-32. PMID: 10086995.
[2]: Froushani SM, Galeh HE. New insight into the immunomodulatory mechanisms of Tretinoin in NMRI mice. Iran J Basic Med Sci. 2014 Sep;17(9):632-7. PMID: 25691937; PMCID: PMC4322144.
[3]: Richter JR, F?rstr?m LR, et,al. Efficacy of the fixed 1.2% clindamycin phosphate, 0.025% tretinoin gel formulation (Velac) and a proprietary 0.025% tretinoin gel formulation (Aberela) in the topical control of facial acne. J Eur Acad Dermatol Venereol. 1998 Nov;11(3):227-33. PMID: 9883434.
[4]: Schultze E, Ourique A, et,al. Encapsulation in lipid-core nanocapsules overcomes lung cancer cell resistance to tretinoin. Eur J Pharm Biopharm. 2014 May;87(1):55-63. doi: 10.1016/j.ejpb.2014.02.003. Epub 2014 Feb 11. PMID: 24525073.
[5]: Rhinn M, Dollé P. Retinoic acid signalling during development. Development. 2012 Mar;139(5):843-58. doi: 10.1242/dev.065938. PMID: 22318625.
[6]: Chansri N, Kawakami S, et,al. Anti-tumor effect of all-trans retinoic acid loaded polymeric micelles in solid tumor bearing mice. Pharm Res. 2008 Feb;25(2):428-34. doi: 10.1007/s11095-007-9398-x. Epub 2007 Jul 31. PMID: 17665288.
[7]: Xu Q, Zhang Z, et,al. Antisense oligonucleotides and all-trans retinoic acid have a synergistic anti-tumor effect on oral squamous cell carcinoma. BMC Cancer. 2008 Jun 3;8:159. doi: 10.1186/1471-2407-8-159. PMID: 18522733; PMCID: PMC2427037.
维甲酸 (Aberela) 是一种维生素 A 衍生的非肽类亲脂性小分子，可作为核 RA 受体 (RAR) 的配体，将其从转录抑制因子转化为激活因子[5] .
在培养的人系膜细胞中，维甲酸 (Aberela) 以剂量和时间依赖性方式增加还原型谷胱甘肽含量和过氧化氢酶活性，从而阻止 H2O2 的细胞毒性[1]。 A549 细胞与游离维甲酸 (Aberela) (TTN)、空白纳米胶囊 (LNC) 和载有维甲酸 (Aberela) 的脂质核心纳米胶囊 (TTN-LNC) 一起孵育。 TTN-LNC 在 G1 期诱导细胞凋亡和细胞周期停滞，而 TTN 则没有。 TTN-LNC 对评估的 A549 细胞表现出比 TTN 更高的细胞毒性作用[4]。As-ODN-hTR 和全反式维甲酸 (Aberela) 的组合具有协同抗肿瘤作用。这种抗肿瘤作用主要归因于端粒酶活性降低诱导的细胞凋亡。 Bcl-2在这个过程中起着重要作用[7]。
在雄性 nmri 小鼠中，维甲酸 (Aberela) 显着抑制细胞免疫并增加体液免疫。维甲酸 (Aberela) 减少淋巴细胞增殖，减少 NBT 和白细胞介素 17 的分泌，但增加白细胞介素 10 的分泌[2]。在面部痤疮患者中，克林霉素磷酸酯维甲酸 (Aberela) 凝胶 (CTG)（1.2% 克林霉素磷酸酯、0.025% 维甲酸 (Aberela) 在凝胶基质 (Velac) 中）比 0.025% 维甲酸 (Aberela) 更有效，继发维甲酸 (Aberela) 抗炎作用的影响[3]。相比之下，聚合物胶束递送维甲酸 (Aberela) 可延长血液循环并增强维甲酸 (Aberela) 在肿瘤组织中的积累服用游离维甲酸 (Aberela)。维甲酸（Aberela）聚合物胶束处理后小鼠肿瘤生长显着延迟，存活时间延长，证明维甲酸（Aberela）抗癌活性得到改善[6]。
| Cas No. | 302-79-4 | SDF | |
| 别名 | 维生素A酸; Vitamin A acid; all-trans-Retinoic acid; ATRA | ||
| 化学名 | (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoic acid | ||
| Canonical SMILES | CC1=C(C(CCC1)(C)C)C=CC(=CC=CC(=CC(=O)O)C)C | ||
| 分子式 | C20H28O2 | 分子量 | 300.4 |
| 溶解度 | DMSO: 60 mg/mL (199.73 mM) | 储存条件 | Store at -20°C, sealed storage, away from moisture and light |
| 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 | 3.3289 mL | 16.6445 mL | 33.2889 mL |
| 5 mM | 0.6658 mL | 3.3289 mL | 6.6578 mL |
| 10 mM | 0.3329 mL | 1.6644 mL | 3.3289 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 |
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| % 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，
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1. 首先保证母液是澄清的；
2.
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Tretinoin
Tretinoin has not been studied during breastfeeding. Breastfeeding should probably be avoided after oral use. Because it is poorly absorbed after topical application, it is considered a low risk to the nursing infant.[1] Do not apply tretinoin directly to the nipple and areola and ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated.
Efficacy of the fixed 1.2% clindamycin phosphate, 0.025% tretinoin gel formulation (Velac) and a proprietary 0.025% tretinoin gel formulation (Aberela) in the topical control of facial acne
Background: A formulation containing agents affecting the non-inflammatory as well as the inflammatory lesions of acne vulgaris at the same time would be efficient, probably showing a high efficacy and possibly a considerable shortening of the duration of treatment. One single formulation would simplify drug administration thereby enhancing patient compliance and possibly leading to improved therapeutic results. In two studies this seems to have been corroborated for the fixed clindamycin phosphate-tretinoin gel formulation.
Objective: This study was designed to assess whether the recently developed fixed formulation of 1.2% clindamycin phosphate and 0.025% tretinoin in a gel base (Velac), further referred to as Clindamycin phosphate Tretinoin Gel is at least as effective as a proprietary 0.025% tretinoin gel formulation (Aberela, Janssen Cilag Ab, Sollentuna, Sweden; further defined as tretinoin) showing an additional anti-inflammatory effect in the treatment of moderate to severe acne vulgaris.
Methods: In a double-blind, randomised study 72 patients were treated with CTG and 73 with tretinoin gel in a once daily regimen for 12 weeks. Responses, irritation as well as possible systemic and other adverse effects were recorded after 4, 8 and 12 weeks of treatment and the improvement, compared to baseline, assessed in all included patients. An additional assessment of the safety parameters was carried out at week 2. Parameters of efficacy were the various acne lesion counts, the overall acne severity grade and the calculated totals of acne lesion counts.
Results: CTG was statistically significantly more effective than tretinoin at the P = 0.05 level in the papular and the total mean inflammatory lesion counts as well as in the estimated or calculated mean overall acne severity scores. CTG and tretinoin gel were equally effective in the remaining parameters: open and closed comedones, the calculated total mean comedone, the pustule as well as the nodule lesion counts. The onset of action was faster for CTG than for tretinoin gel and evident in all assessed parameters except in open comedone lesion counts. In the calculated total mean acne lesion counts, half of all acne lesions had disappeared by week 6 of treatment with CTG, whereas this was recorded at week 9 for tretinoin gel. No clinically relevant changes in the parameters of safety as a consequence of treatment were observed, although the burning component of irritation was shown to be significantly less for CTG than for tretinoin gel. The observed adverse effects were considered minor. Treatment had to be discontinued in five patients on CTG and three on tretinoin.
Conclusion: The addition of clindamycin to tretinoin, as in CTG, enhances the comedolytic efficacy of tretinoin in moderate to severe acne of the face, maintaining at the same time its anti-inflammatory efficacy thus accelerating resolution of all types of acne lesions without affecting the safety of response to both components.