切换导航

Ulipristal

现货
Catalog No.
B2134
孕激素受体调节剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 610.00
现货
5mg
¥ 580.00
现货
50mg
¥ 2,950.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Ulipristal is a novel and selective progesterone receptor modulator (SPRM) for emergency contraception after an unprotected intercourse or contraceptive failure. Ulipristal can be used for the treatment of benign gynecological conditions such as uterine myoma [1]. SPRMs is a new class of agent which can act on the progesterone receptor. SPRMs have been involved in exerting clinically relevant tissue-selective progesterone agonist, antagonist, or mixed agonist/antagonist effects on progesterone target tissues [2].

In vitro: Ulipristal acetate dose dependently suppressed progesterone-induced acrosome reaction and hyperactivation in human spermatozoa. Ulipristal acetate modulated human sperm functions by acting as progesterone antagonists [3].

In vivo: In the terminal deoxynucleotide transferase–mediated dUTP nick-end labeling assay, UPA-treated myomas increased cell death when compared with untreated myomas [4].

Clinical trials: UPA seemed to be a reasonably tolerable and effective method of emergency contraception (EC)when used within 120 hours of intercourse. UPA is at least as effective as LNG when used in the first 72 hours after unprotected intercourse [1].

References:
[1]. Richardson A R, Maltz F N. Ulipristal acetate: review of the efficacy and safety of a newly approved agent for emergency contraception[J]. Clinical therapeutics, 2012, 34(1): 24-36.
[2]. Chwalisz K, Perez M C, DeManno D, et al. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis[J]. Endocrine reviews, 2005, 26(3): 423-438.
[3]. Ko J K Y, Huang V W, Li R H W, et al. An in vitro study of the effect of mifepristone and ulipristal acetate on human sperm functions[J]. Andrology, 2014, 2(6): 868-874.
[4]. Courtoy G E, Donnez J, Marbaix E, et al. In vivo mechanisms of uterine myoma volume reduction with ulipristal acetate treatment[J]. Fertility and sterility, 2015, 104(2): 426-434. e1.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt433.58
Cas No.159811-51-5
FormulaC28H35NO3
Solubility≥21.7mg/mL in DMSO
Chemical Name[(8S,11R,13S,14S,17R)-17-acetyl-11-[4-(dimethylamino)phenyl]-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate
SDFDownload SDF
Canonical SMILESCC(=O)C1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)OC(=O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

精子

制备方法

在DMSO中的溶解度大于21.7 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.04、0.4、4和40 μM

实验结果

在孕激素刺激的精子中,Ulipristal (≥ 0.4 μM) 呈剂量依赖性地降低顶体反应和超活化。在0.4 μM剂量下,Ulipristal将出现顶体反应和超活化(由孕酮诱导)的精子的百分比降低了33.1 ± 7.3%和55.3 ± 16.2%。

References:

[1]. Ko J K Y, Huang V W, Li R H W, et al. An in vitro study of the effect of mifepristone and ulipristal acetate on human sperm functions[J]. Andrology, 2014, 2(6): 868-874.

质量控制

化学结构

Ulipristal