对于治疗有症状的子宫内膜异位症，醋酸炔诺酮可能是一种价格合理且副作用可控的替代品。接受醋酸炔诺酮治疗的受试者痛经和非周期性盆腔不适得到缓解[1]。对于控制子宫内膜异位症各个阶段的疼痛和出血，单独使用醋酸炔诺酮是一种耐受性良好且有效的治疗方法。无论之前的激素治疗方案如何，醋酸炔诺酮药物都可以改善出血评分，并且还可以改善所有患者的疼痛评分，除了那些之前接受过 GnRH 激动剂 + 加回治疗的患者之外 [2]。在实验动物中，醋酸炔诺酮显示出很少的急性毒性，这与在人类中不存在毒性的情况一致。当给啮齿动物施用多个人类剂量的醋酸炔诺酮时，没有观察到与治疗相关的死亡率、血液学改变、行为改变或器官疾病[3]。当喂食高碳水化合物饮食的大鼠给予醋酸炔诺酮时，它们的血浆脂蛋白密度（<1.006）以及胆固醇、甘油三酯和血浆脂蛋白的磷脂浓度显着且成比例地降低。当给予醋酸炔诺酮（0.1 mM）时，观察到给予离体大鼠肝细胞的甘油三酯中棕榈酸酯和甘油的摄取显着减少[4]。

[1]. Effect of norethindrone acetate in the treatment of symptomatic endometriosis. Int J Fertil Womens Med. 1998 Jan-Feb;43(1):24-7.

[2]. Use of norethindrone acetate alone for postoperative suppression of endometriosis symptoms. J Pediatr Adolesc Gynecol. 2012 Apr;25(2):105-8.

[3]. Pharmacology and toxicology of ethinyl estradiol and norethindrone acetate in experimental animals. Regul Toxicol Pharmacol. 2001 Aug;34(1):53-61.

[4]. Norethindrone acetate inhibition of triglyceride synthesis and release by rat hepatocytes. Atherosclerosis. 1983 Jan;46(1):41-8.

Norethisterone Acetate (Norethindrone Acetate) can cause developmental toxicity according to state or federal government labeling requirements.
Norethisterone acetate is a 3-oxo Delta(4)-steroid that is norethisterone in which the hydroxy group has been converted to its acetate ester. It has a role as a synthetic oral contraceptive and a progestin. It is a 3-oxo-Delta(4) steroid, a terminal acetylenic compound and an acetate ester. It is functionally related to a norethisterone.
Norethindrone Acetate is the orally bioavailable acetate salt of norethindrone, a synthetic progestin with some anabolic, estrogenic, and androgenic activities. As do all progestins, norethindrone binds to and activates nuclear progesterone receptors (PRs) in target tissues such as the pituitary and reproductive system; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes, followed by various transcriptional events and histone acetylation. Physiological effects include the inhibition of luteinizing hormone (LH) release, an increase in the endometrial luteal-phase, and alterations in endocervical mucus secretion.
Acetate ester of norethindrone that is used as a long-term contraceptive (CONTRACEPTIVE AGENTS).
See also: Norethindrone (has active moiety); Estradiol; Norethindrone Acetate (component of); Leuprolide acetate; norethindrone acetate (component of) ... View More ...

C22H28O3

340.46

340.203

51-98-9

Norethindrone acetate-d8

5832

White to off-white solid powder

1.1±0.1 g/cm3

454.7±45.0 °C at 760 mmHg

197.1±28.8 °C

0.0±1.1 mmHg at 25°C

1.556

3.99

43.37

0

3

3

25

695

6

CC(=O)O[C@]1(CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=CC(=O)CC[C@H]34)C)C#C

IMONTRJLAWHYGT-ZCPXKWAGSA-N

InChI=1S/C22H28O3/c1-4-22(25-14(2)23)12-10-20-19-7-5-15-13-16(24)6-8-17(15)18(19)9-11-21(20,22)3/h1,13,17-20H,5-12H2,2-3H3/t17-,18+,19+,20-,21-,22-/m0/s1

[(8R,9S,10R,13S,14S,17R)-17-ethynyl-13-methyl-3-oxo-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] acetate

NSC-22844 NSC22844NSC 22844ENTA Norethindrone acetate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (~293.72 mM)
H2O : ~0.67 mg/mL (~1.97 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (7.34 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (7.34 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (7.34 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。