Retinoic acid 是维生素A的代谢产物,在细胞生长,分化和器官发生中起重要作用。 Retinoic acid是RAR核受体的天然激动剂,对RARα/β/γ的IC50为14 nM。 Retinoic acid与PPARβ/δ结合的Kd值为17 nM。Retinoic acid 可以通过激活视黄酸受体抑制转录因子 Nrf2。
生物活性 | Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist ofRARnuclear receptors, withIC50s of 14 nM for RARα/β/γ. Retinoic acid bind toPPARβ/δwithKdof 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha. |
IC50& Target[2][5] | PPARα 103 nM (Kd) | PPARγ 178 nM (Kd) | PPARβ/δ 17 nM (Kd) | Human Endogenous Metabolite |
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体外研究 (In Vitro) | Retinoic acid (All-trans-retinoic acid, ATRA) is a highly potent derivative of vitamin A that is required for virtually all essential physiological processes and functions because of its involvement in transcriptional regulation of over 530 different genes. Retinoic acid exerts its actions by serving as an activating ligand of nuclear retinoic acid receptors (RARα-γ), which form heterodimers with retinoid X receptors (RXRα-γ)[1]. Retinoic acid (RA) bound to PPARα and PPARγ with a low affinity demonstrated by Kdvalues of 100-200 nM. In contrast, Retinoic acid associates with PPARβ/δ with a Kdof 17 nM, revealing both high affinity and isotype selectivity[2]. Undifferentiated P19 cells express the Retinoic acid (RA) receptors RARα, RARβ, RARγ, and PPARβ/δ, as well as the Retinoic acid -binding proteins CRABP-II and FABP5. Induction of differentiation by treatment of cells with Retinoic acid results in transient up-regulation of CRABP-II and down-regulation of FABP5 that are observed at the level of both the respective proteins and mRNAs. Following the initial decrease, the level of both FABP5 protein and mRNA increases to attain a 2-2.5-fold higher level in mature neurons as compared with undifferentiated P19 cells. Induction of differentiation does not markedly affect the levels of either RARα or PPARβ/δ. The level of RARγ mRNA decreases by about 5-fold by day 4 and remained low in mature neurons[3]. Retinoic acid (RA) is a morphogen derived from retinol (vitamin A) that plays important roles in cell growth, differentiation, and organogenesis. The Retinoic acid interacts with retinoic acid receptor (RAR) and retinoic acid X receptor (RXR) which then regulate the target gene expression[4].
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结构分类 | - Ketones, Aldehydes, Acids
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(166.42 mM;ultrasonic and warming and heat to 60℃) 配制储备液 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;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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 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); Suspended solution; Need ultrasonic and warming
此方案可获得 2.5 mg/mL (8.32 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.32 mM); Suspended solution
此方案可获得 ≥ 2.5 mg/mL (8.32 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil 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,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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 4. 请依序添加每种溶剂: 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: 2.5 mg/mL (8.32 mM); Suspended solution; Need ultrasonic 5. 请依序添加每种溶剂: 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (8.32 mM); Suspended solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |