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17 alpha-propionate

  • 产品货号:CS-01Y78077
  • 产品价格:电议
  • 产品产地:国产
  • 包装类型:5mg 10mg 50mg 100mg
  • 采购热度:246
  • 库存:100
  • CAS号:19608-29-8
  • 方法:
  • 含量:>98.50%
  • 品牌名称:莼试
  • 分子式:C24H34O5
  • 分子量:402.52

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标签:17 alpha-propionate 

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化学性质:                                                                                                             

规格

5mg 10mg 50mg 100mg

CAS

19608-29-8

别名

17α-propionate; CB-03-01

化学名

[(8R,9S,10R,13S,14S,17R)-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] propanoate

分子式

C24H34O5

分子量

402.52

溶解度

DMF: 20mg/mL,DMSO: 10mg/mL,Ethanol: 20mg/mL,Ethanol:PBS (pH 7.2) (1:9): 0.1mg/mL

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

Acne vulgaris is a disorder of the pilosebaceous unit in which the androgens contribute to its onset and persistence. Though the use of antiandrogens is potentially effective; topical use of antiandrogens are not available on the market. Cortexolone 17a-propionate (CB-03-01) is a new potent topical antiandrogen potentially useful in acne vulgaris. CB-03-01 is a new chemical entity that acts at the level of the skin androgen receptor, which blocks testosterone and di-hydrotestosterone from binding to the receptor in the cell.

In vitro: The aim of one in vitro study was to investigate the antiandrogenic activity of a new monoester of cortexolone, cortexolone 17alpha-propionate. Although the compound displayed a strong local antiandrogenic activity in hamster's flank organ test. Its pharmacological activity seemed to be primarily related to its ability to antagonistically compete at androgen receptor level; nevertheless its primary pharmacological target needs to be further investigated. The topical activity of cortexolone 17alpha-propionate with the apparent absence of systemic effects makes this compound to have the potential of representing a novel and safe therapeutic approach for androgen-dependent skin disorders. [1].

In vivo: Cortexolone 17alpha-propionate displayed a strong local antiandrogenic activity in hamster's flank organ test, however, it did not exhibit antiandrogenic activity in rats, nor did it affect gonadotropins hypersecretion. As topical antiandrogen, the steroid resulted about 4 times more active than progesterone and, when compared to known antiandrogen standards, it was about 3 times more potent than flutamide, about 2 times more effective than finasteride and approximately as active as cyproterone acetate. Its pharmacological activity seemed to be primarily related to its ability to antagonistically compete at androgen receptor level; nevertheless its primary pharmacological target needs to be further investigated [1].

Clinical trial: In 2011, Trifu et al. evaluated the safety and efficacy of cortexolone 17alpha-propionate 1% cream in acne vulgaris in comparison to placebo and to tretinoin 0.05% cream. A total of 77 male subjects were randomized to receive cortexolone 17alpha-propionate 1% cream, tretinoin 0.05% cream or placebo once nightly for 8 weeks. cortexolone 17alpha-propionate 1% cream was statistically better than placebo in reducing total lesion count, inflammatory lesion count  and Acne Severity Index, without any major side effects. Further, cortexolone 17alpha-propionate 1% cream showed a faster onset of all the abovementioned improvements and was clinically more effective than tretinoin 0.05% cream, although the results were not statistically significant [2]

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1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

原创作者:上海莼试生物技术有限公司

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