Adapalene - CAS:106685-40-9

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Adapalene (Synonyms:阿达帕林; CD271)

目录号 : KM19304 CAS No. : 106685-40-9 纯度 : ≥98%

Data Sheet 产品使用指南

Adapalene (CD271) 是第三代合成类视黄醇，局部应用于痤疮。Adapalene 是一种有效的 RAR 激动剂，对 RARβ、RARγ、RARα 的 AC₅₀ 值分别为 2.3 nM、9.3 nM 和 22 nM。Adapalene 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene 具有抗肿瘤活性。

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50mg		In-stock
100mg		In-stock
500mg		In-stock
1g	询价	In-stock
5g	询价	In-stock

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生物活性

Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC₅₀s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.

体外研究

Adapalene (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC₅₀s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively.
Adapalene (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro.
Adapalene (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells.
Adapalene (1-200 μM) inhibits GOT1 activity, with an IC₅₀ of 21.79 μM.
Adapalene (10-10 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC₅₀ of 2.5 nM.

Cell Viability Assay

Cell Line:	Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929)
Concentration:	1-200 μM
Incubation Time:	24 hours
Result:	Inhibited the viability of cancer cells with higher GOT1 protein expression.

Apoptosis Analysis

Cell Line:	ES-2 cells
Concentration:	10, 20, 40 μM
Incubation Time:	24 hours
Result:	Showed a significant increase in apoptosis compared with the control group. Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP.

Cell Cycle Analysis

Cell Line:	LoVo or DLD1 cells
Concentration:	3, 10, 30 μM
Incubation Time:	6, 12, 24 hours
Result:	Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner.

体内研究

Adapalene (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice.

Animal Model:	Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells
Dosage:	15, 20, 65, 100 mg/kg
Administration:	P.o. daily for 21 days
Result:	Significantly reduced tumor weight and volume.

分子式

C₂₈H₂₈O₃

分子量

412.52

CAS号

106685-40-9

中文名称

阿达帕林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 20 mg/mL (48.48 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4241 mL	12.1206 mL	24.2412 mL
5 mM	0.4848 mL	2.4241 mL	4.8482 mL
10 mM	0.2424 mL	1.2121 mL	2.4241 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°C, 6 months; -20°C, 1 month。-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。

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 mg/mL (4.85 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (4.85 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 20.0 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。

临床试验

科研文献

纯度： ≥98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

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分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

体积

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 4 篇科研文献

The molarity calculator equation

The dilution calculator equation