Norgestimate
(Synonyms: 诺孕酯) 目录号 : GC12290A progestin
Cas No.:35189-28-7
Sample solution is provided at 25 µL, 10mM.
Norgestimate is a synthetic progesterone analog.
Progesterone, an endogenous steroid and progestogen sex hormone, is involved in the pregnancy, menstrual cycle, and embryogenesis. Progesterone is reported to belong to steroid hormones, and is the major progestogen in the body. Progesterone is also a crucial metabolic intermediate in the production of other endogenous steroids and plays an key role in brain function as a neurosteroid.
In vitro: Norgestimate was found that, unlike other 19-nortestosterone derivatives, showed high selectivity for the progesterone receptor and low androgenic activity. Moreover, norgestimate and its main active metabolite norelgestromin could not bind to or occupy sex hormone-binding globulin [1].
In vivo: The androgenic and the progestational activity of norgestimate were compared in two animal studies. It was found the difference in the pharmacological response in norgestimate treated rats was equivalent to the difference in the exposure of the animals to either directly administered or metabolically derived levonorgestrel [2].
Clinical trial: Norgestimate (brand names Ortho-Cyclen, Ortho Tri-Cyclen, Previfem, Sprintec, Prefest, others) is a steroidal progestin of the 19-nortestosterone group that is clinically used in combination with ethinylestradiol and in combination with estradiol in menopausal hormone replacement therapy [3].
References:
[1] Thomas L. Lemke; David A. Williams (2008). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 1316–. ISBN 978-0-7817-6879-5.
[2] Kuhnz W, Beier S. Comparative progestational and androgenic activity of norgestimate and levonorgestrel in the rat. Contraception. 1994 Mar;49(3):275-89.
[3] https://en. wikipedia.org/wiki/Norgestimate
Cas No. | 35189-28-7 | SDF | |
别名 | 诺孕酯 | ||
化学名 | (17α)-17-(acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oxime | ||
Canonical SMILES | CC[C@@]12[C@](CC[C@@]2(OC(C)=O)C#C)([H])[C@]3([H])CCC4=C/C(CC[C@]4([H])[C@@]3([H])CC1)=N/O | ||
分子式 | C23H31NO3 | 分子量 | 369.5 |
溶解度 | ≤2mg/ml in ethanol;14mg/ml in DMSO;16mg/ml in dimethyl formamide | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7064 mL | 13.5318 mL | 27.0636 mL |
5 mM | 0.5413 mL | 2.7064 mL | 5.4127 mL |
10 mM | 0.2706 mL | 1.3532 mL | 2.7064 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet