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Clascoterone

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Chemical Structure| 19608-29-8 同义名 : Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;Winlevi;CB-03-01
CAS号 : 19608-29-8
货号 : A560996
分子式 : C24H34O5
纯度 : 98%
分子量 : 402.524
MDL号 : MFCD18384978
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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
动物实验配方：
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]
实验方案
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
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.