Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.

Progesterone Receptor^[1]

Norethindrone acetate could be a cost-effective alternative with relatively mild side effects in the treatment of symptomatic endometriosis. Subjects treated with norethindrone acetate obtain dysmenorrhea and noncyclic pelvic pain relief^[1]. Norethindrone acetate alone is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis. Post-Norethindrone acetate bleeding scores are improved regardless of prior hormonal regimen, and post-Norethindrone acetate pain scores improved in all patients except for those previously prescribed GnRH-agonist plus add-back^[2]. Norethindrone acetate shows low acute toxicity in experimental animals and is consistent with the lack of toxicity seen in humans. Administration of norethindrone acetate alone to rodents at several multiples of the human dose results in no treatment related mortality, hematological changes, behavioral changes, or organ pathology^[3]. Norethindrone acetate administration leads to significant and proportional reductions of the concentrations of triglycerides, cholesterol and phospholipids of plasma lipoproteins of density<1.006 of rats fed a high carbohydrate diet. Norethindrone acetate (0.1 mM) also significantly inhibits the incorporation of both palmitate and glycerol into triglycerides of isolated hepatocytes from fed rats^[4].

298.42

Solid

C₂₀H₂₆O₂

68-22-4

炔诺酮；去甲基脱氢羟孕酮

Room temperature in continental US; may vary elsewhere.

DMSO : 110 mg/mL(368.61 mM;Need ultrasonic)

H₂O : 2.7 mg/mL(9.05 mM;Need ultrasonic)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: 2.75 mg/mL (9.22 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.75 mg/mL (9.22 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.75 mg/mL (9.22 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (9.22 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.75 mg/mL (9.22 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (9.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。