Norgestimate (Synonyms: Dexnorgestrel acetime) |
| カタログ番号GC12290 |
合成プロゲステロン類似体であるノルゲスチメートは、高度に選択的なプロゲステロン活性と最小限のアンドロゲン性を有する経口活性プロゲスチンです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 35189-28-7
Sample solution is provided at 25 µL, 10mM.
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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 | |
| 同義語 | Dexnorgestrel acetime | ||
| Chemical Name | (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 | ||
| Formula | C23H31NO3 | M.Wt | 369.5 |
| 溶解度 | ≤2mg/ml in ethanol;14mg/ml in DMSO;16mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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