Norgestimate metabolite Norelgestromin (17-Deacetyl norgestimate)
(Synonyms: 甲基孕酮,17-Deacetyl norgestimate; 17-Deacylnorgestimate) 目录号 : GC33532
An active metabolite of norgestimate
Cas No.:53016-31-2
Sample solution is provided at 25 µL, 10mM.
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Norelgestromin is an active metabolite of the progestin norgestimate .1 Norelgestromin is formed from norgestimate via deacetylation in human liver microsomes. It is an agonist of the progesterone receptor and estrogen receptor α (ERα; EC50s = 11.1 and 43.4 nM, respectively) and an antagonist of the glucocorticoid and mineralocorticoid receptors (IC50s = 255 nM and 83.7 nM, respectively).2 Norelgestromin selectively binds to progestin receptors (IC50 = 4.61 nM for rabbit uterine receptors) over androgen receptors (IC50 = 222 nM for rat prostatic receptors) in radioligand binding assays.3 However, norelgestromin (1 nM) activates the androgen receptor in a transactivation assay in MDA-MB-231 breast cancer cells expressing the human receptor.4 Formulations containing norelgestromin in combination with ethynyl estradiol have been used as contraceptives and in the treatment of acne vulgaris in women.
1.Madden, S., and Back, D.J.Metabolism of norgestimate by human gastrointestinal mucosa and liver microsomes in vitroJ. Steroid Biochem. Mol. Biol.38(4)497-503(1991) 2.Paris, F., Balaguer, P., Rimbault, F., et al.Molecular action of norgestimate: New developmentsGynecol. Endocrinol.31(6)487-490(2015) 3.Phillips, A., Demarest, K., Hahn, D.W., et al.Progestational and androgenic receptor binding affinities and in vivo activities of norgestimate and other progestinsContraception41(4)399-410(1990) 4.Prifti, S., Lelle, I., Strowitzki, T., et al.Induction of androgen receptor activity by norgestimate and norelgestromin in MDA-MB 231 breast cancer cellsGynecol. Endocrinol.19(1)18-21(2004)
| Cas No. | 53016-31-2 | SDF | |
| 别名 | 甲基孕酮,17-Deacetyl norgestimate; 17-Deacylnorgestimate | ||
| Canonical SMILES | O/N=C1CC[C@@]2([H])C(CC[C@]3([H])[C@]2([H])CC[C@@]4(CC)[C@@]3([H])CC[C@]4(C#C)O)=C\1 | ||
| 分子式 | C21H29NO2 | 分子量 | 327.46 |
| 溶解度 | DMSO : 20 mg/mL (61.08 mM; Need ultrasonic) | 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 | 3.0538 mL | 15.269 mL | 30.5381 mL |
| 5 mM | 0.6108 mL | 3.0538 mL | 6.1076 mL |
| 10 mM | 0.3054 mL | 1.5269 mL | 3.0538 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet