Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Adapalene sodium salt (Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene (CD271) sodium salt 是第三代合成类视黄醇，局部应用于痤疮。Adapalene sodium salt 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 sodium salt 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene sodium salt 具有抗肿瘤活性。

Adapalene sodium salt(Synonyms: 阿达帕林钠; CD 271 sodium salt)

Adapalene sodium salt Chemical Structure

CAS No. : 911110-93-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Adapalene sodium salt 的其他形式现货产品:

Adapalene

生物活性

Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity[1][2][3].

IC50 & Target

AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1]
体外研究
(In Vitro)

Adapalene sodium salt (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[2].
Adapalene sodium salt (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene sodium salt (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene sodium salt (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene sodium salt (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

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[3]

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
(In Vivo)

Adapalene sodium salt (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3]
Dosage: 15, 20, 65, 100 mg/kg
Administration: P.o. daily for 21 days
Result: Significantly reduced tumor weight and volume.

Clinical Trial

分子量

434.50

Formula

C28H27NaO3
CAS 号

911110-93-5
中文名称

阿达帕林钠
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Shroot B, et, al. Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.

    [2]. Wang Q, et, al. Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315.

    [3]. Shi XN, et, al. Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Mol Med Rep. 2015 Nov;12(5):6501-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务