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Adapalene sodium salt
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Adapalene sodium salt图片
CAS NO:911110-93-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
阿达帕林钠
CD 271 sodium salt
产品介绍
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RARβRARγRARαAC50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。
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 potentRARagonist, withAC50s of 2.3 nM, 9.3 nM, and 22 nM forRARβ,RARγ,RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity ofGOT1in 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 (10-6-10-3nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50of 2.5 nM[1].

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].

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.