Ulipristal
(Synonyms: 醋酸乌利司他中间体,CDB-3236; Deacetyl CDB-2914) 目录号 : GC17305
A selective progesterone receptor modulator
Cas No.:159811-51-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
Spermatozoa |
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Preparation method |
The solubility of this compound in DMSO is > 21.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.04, 0.4, 4 and 40 μM |
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Applications |
In progesterone-induced spermatozoa, Ulipristal (≥ 0.4 μM) dose-dependently decreased acrosome reaction and hyperactivation. At the dose of 0.4 μM, Ulipristal reduced the percentages of progesterone-induced acrosome-reacted and hyperactivated spermatozoa by 33.1 ± 7.3% and 55.3 ± 16.2%. |
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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. | |
| Cas No. | 159811-51-5 | SDF | |
| 别名 | 醋酸乌利司他中间体,CDB-3236; Deacetyl CDB-2914 | ||
| 化学名 | (8S,11R,13S,14S,17R)-17-acetyl-11-(4-(dimethylamino)phenyl)-17-hydroxy-13-methyl-6,7,8,11,12,13,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3(2H)-one | ||
| Canonical SMILES | CC([C@@]1(O)CC[C@@]2([H])[C@]3([H])CCC4=CC(CCC4=C3[C@](C5=CC=C(N(C)C)C=C5)([H])C[C@@]21C)=O)=O | ||
| 分子式 | C28H35NO3 | 分子量 | 433.58 |
| 溶解度 | ≥ 21.7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3064 mL | 11.5319 mL | 23.0638 mL |
| 5 mM | 0.4613 mL | 2.3064 mL | 4.6128 mL |
| 10 mM | 0.2306 mL | 1.1532 mL | 2.3064 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet