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克拉司酮 /Clascoterone {[allProObj[0].p_purity_real_show]}

货号:A560996 同义名: Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate

Cortexolone 17 alpha-propionate is a topical and peripherally selective androgen antagonist, which is used in treatment of acne and androgenic alopecia.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Clascoterone 化学结构 CAS号:19608-29-8
Clascoterone 化学结构
CAS号:19608-29-8
Clascoterone 3D分子结构
CAS号:19608-29-8
Clascoterone 化学结构 CAS号:19608-29-8
Clascoterone 3D分子结构 CAS号:19608-29-8
规格 价格 会员价 库存 数量
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Clascoterone 纯度/质量文件 产品仅供科研

货号:A560996 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Androgen Receptor 其他靶点 纯度
Cyproterone acetate ++++

Androgen Receptor, IC50: 7.1 nM

98%
Apalutamide +++

Androgen Receptor, IC50: 16 nM

98%
AZD3514 +

Androgen Receptor, Ki: 2.2 μM

98%
Darolutamide ++++

Androgen receptor, Ki: 11 nM

98%
Flutamide +++

Androgen Receptor, Ki: 55 nM

98%
Galeterone ++

Androgen Receptor, IC50: 384 nM

98%
Enzalutamide +++

Androgen Receptor, IC50: 36 nM

98%
Megestrol 98%
Bicalutamide ++

Androgen Receptor, IC50: 0.16 μM

99%
EPI-001 +

Androgen Receptor, IC50: ~6 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Clascoterone 生物活性

描述 Androgens are C-19 steroids that provide major regulatory influences on male reproductive function[2]. Cortexolone 17 alpha-propionate is a topical and peripherally selective androgen antagonist, which is used in treatment of acne and androgenic alopecia[3]. Clascoterone 1% cream was very well tolerated, and was significantly better than placebo regarding TLC, ILC and ASI, and also clinically more effective than comparator. The product also induced a faster attainment of 50% improvement in all the above parameters[4]. In vitro studies showed that clascoterone binds to androgen receptors with high affinity and inhibits DHT-stimulated signaling. Clascoterone dose-dependently inhibited DHT-induced lipid synthesis and infammatory cytokine production in human primary sebocytes[5]. In hair follicle dermal papilla cells, clascoterone selectively inhibited androgen receptor-regulated pathways that impede hair follicle growth, without affecting the production and secretion of pro-follicle growth factors[6]. Clascoterone cream did not afect the pharmacokinetics of drugs metabolized by CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 or 3A4 to a clinically meaningful extent[7]

Clascoterone 参考文献

[1]Celasco G, Moro L, et al. Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist. Arzneimittelforschung. 2004;54(12):881-6.

[2]A K Roy,et al. Androgen action. Crit Rev Eukaryot Gene Expr. 1995. 5(2), 157-76.

[3]Trifu V, et al. Cortexolone 17α-propionate 1% cream, a new potent antiandrogen for topical treatment of acne vulgaris. A pilot randomized, double-blind comparative study vs. placebo and tretinoin 0·05% cream. Br J Dermatol. 2011. 165(1), 177-83.

[4]Celasco G, et al. Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist. Arzneimittelforschung. 2004. 54(12), 881-6.

[5]Rosette C, Agan FJ, Mazzetti A, et al. Cortexolone 17alpha-propionate (clascoterone) is a novel androgen receptor antagonist that inhibits production of lipids and infammatory cytokines from sebocytes in vitro. J Drugs Dermatol. 2019. 18(5), 412–8.

[6]Rosette C, et al. Cortexolone 17alpha-propionate (clascoterone) is an androgen receptor antagonist in dermal papilla cells in vitro. J Drugs Dermatol. 2019. 18(2), 197–201.

[7]Cassiopea. Winlevi (clascoterone) cream: US prescribing information. 2020.

Clascoterone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.42mL

2.48mL

1.24mL

24.84mL

4.97mL

2.48mL

Clascoterone 技术信息

CAS号19608-29-8
分子式C24H34O5
分子量 402.524
别名 Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;Winlevi;CB-03-01
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(260.85 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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