更新于：2024-11-01

AP-736

更新于：2024-11-01

概要

研发状态

概要

基本信息

药物类型

小分子化药

别名-

靶点

Melanin x TYR

作用机制

黑色素抑制剂、TYR抑制剂(酪氨酸酶抑制剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Amorepacific Corp.

在研机构

Amorepacific Corp.

非在研机构-

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C26H31NO5

InChIKeyWDLDXQVTSRCDMN-UHFFFAOYSA-N

CAS号1365531-21-0

关联

100 项与 AP-736 相关的临床结果

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100 项与 AP-736 相关的转化医学

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100 项与 AP-736 相关的专利（医药）

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项与 AP-736 相关的文献（医药）

2018-12-01·International Journal of Pharmaceutics2区 · 医学

Development and evaluation of topical formulations for a novel skin whitening agent (AP736) using Hansen solubility parameters and PEG-PCL polymers

2区 · 医学

Article

作者: Beak, Heung Soo ; Joo, Yung Hyup ; Il Kim, Soo ; Choi, Joonho ; Shin, Hong-Ju

AP736 itself is a novel skin whitening agent reported to exhibit anti-melanogenic and tyrosinase inhibitory activity. However, formulating a topical product has been difficult because AP736 is insoluble in water as well as in many oils. In this study, we aimed to develop a new topical delivery system in which AP736 is not only physically stable, but also suitably delivered to the skin. By calculating each HSP (Hansen Solubility Parameters), ethylenedioxy moiety-containing compounds could be easily selected for the formulation ingredients of AP736. Although diethylene glycol monoethyl ether with the highest solubility of AP736 enalbes to make AP736-incorporated water-in-oil emulsions well, the recrystallization of AP736 was observed in oil-in-water emulsions. Therefore, we fabricated polymeric nanoparticles (PNPs) in order to encapsulate AP736 to prevent its recrystallization. We used three different PEG-PCL polymers with various chain lengths and ethylenedioxy moiety-containing surfactants (i.e. Choleth) for fabricating PNPs. The prepared PNPs had a mean particle size from 50 nm to 200 nm. Most of PNPs showed the good encapsulation efficiency up to 90%. In particular, Choleth-24 had a significant role in encapsulating AP736 in PNPs. After encapsulation of AP736, no significant changes were observed in the sizes of tested PNPs within 4 weeks. Further, the recrystallization of AP736 was not observed in oil-in-water emulsions after 24 weeks of storage at 40 °C. In vitro permeation study using Strat-M showed that PNPs containing Choleth-24 has the faster release pattern compared to PNPs using Tween 80 and saturated in D.I. water. These results are demonstrating that PNPs might be an effective vehicle for stabilization in oil-in-water emulsions and topical application of AP736.

2017-05-01·Experimental Dermatology3区 · 医学

AP736 induces miR‐125b expression for the efficient whitening and anti‐ageing action in human epidermal cells

3区 · 医学

Letter

作者: Shin, Hong‐Ju ; Hwang, Jung‐Ah ; Lee, John Hwan ; Bae, Il‐Hong ; Park, Young‐Ho ; Kim, Yong Jin ; Joo, Yung Hyup ; Kim, Kyu‐Han ; Lee, Chang Seok ; Baek, Heung Soo ; Kim, Jin Woong

This study examined whether AP736 inhibits melanogenesis in human melanocytes by increasing miR-125b expression, a depigmentation inducer.It also tested whether AP736 suppression of MMP expression and ROS production, which contribute to the anti-aging efficacy of AP736, involves increased miR-125b expression in human keratinocytes.Results suggest the possibility that AP736 acts through a novel mechanism involving induction of miR-125b expression to cause the inhibition of melanin synthesis in melanocytes.AP736 also simultaneously suppresses MMP-1 and MMP-3 expression as well as ROS production, at least in part, through a signaling pathway involving miR-125b induction in keratinocytes.Taken together this study provides the first evidence to support a role for increased miR-125b expression in the antimelaogenic and anti-aging actions of AP736.

2015-11-01·International Journal of Molecular Medicine3区 · 医学

A novel adamantyl benzylbenzamide derivative, AP736, inhibits melanogenesis in B16F10 mouse melanoma cells via glycogen synthase kinase 3β phosphorylation

3区 · 医学

Article

作者: Lee, John Hwan ; Kim, Beom Joon ; Kwon, Tae-Rin ; Oh, Chang Taek ; Park, Eun-Seok ; Shin, Song Seok ; Shin, Hong-Ju ; Beak, Heung Soo ; Kim, Jeong-Hwan ; Lee, Chang Seok ; Joo, Yung Hyup

Recently, much effort has been made to develop effective dermatological depigmenting compounds. In this study, we investigated the novel candidate compound, AP736 (an adamantyl benzylbenzamide derivative), and its effects on melanogenesis in B16F10 melanoma cells, as well as the mechanisms involved. AP736 has been reported to exert anti-melanogenic effects in melanocytes in vitro and in artificial skin equivalents through the inhibition of key melanogenic enzymes and the suppression of the cAMP-protein kinase A (PKA)-cAMP response element‑binding protein (CREB) signaling pathway. Thus, we examined another pathway of melanogenesis involving the effects of AP736 on the glycogen synthesis kinase 3β (GSK3β) pathway. Melanin content and tyrosinase activity were measured using a spectrophotometer after the cells were treated with AP736. The AP736-induced activation of signaling pathways was examined by western blot analysis. We confirmed that AP736 decreased melanin production in a dose-dependent manner; however, it did not directly inhibit tyrosinase, the rate-limiting melanogenic enzyme. The expression of microphthalmia-associated transcription factor, tyrosinase, and related signal transduction pathways was also investigated. The Wnt signaling pathway is deeply involved in melanogenesis; therefore, phosphorylation by GSK3β was assessed following treatment with AP736. AP736 induced GSK3β phosphorylation (inactivation), but it did not alter the level of β-catenin. Furthermore, the expression of α-melanocyte-stimulating hormone-induced tyrosinase was downregulated by AP736. Our data suggest that AP736 exerts hypopigmentary effects through the downregulation of tyrosinase via GSK3β phosphorylation.

100 项与 AP-736 相关的药物交易

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