Norgestrel|6533-00-2|(炔诺孕酮)-陌孚医药/Medlife

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Norgestrel (Synonyms: 炔诺孕酮)

目录号: PC18045 纯度: ≥98%

CAS No. :6533-00-2

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中文名称

Norgestrel

中文别名

炔诺孕酮;18-甲基炔诺酮;DL-甲基炔诺酮;高诺酮;药典标准品;左炔孕酮;甲基炔诺酮,18-甲炔诺酮;甲基炔诺酮;炔诺酮;炔诺酮-D6;炔诺孕酮 USP标准品;炔诺孕酮标准品(JP)

英文名称

Norgestrel

英文别名

Norgestrel;Norgestrel [USAN:INN:BAN:JAN];(+-)-13-Ethyl-17-hydroxy-18,19-dinor-17alpha-pregn-4-en-20-yn-3-one;dl-13-beta-Ethyl-17-alpha-ethynyl-17-beta-hydroxygon-4-en-3-one;dl-13-beta-Ethyl-17-alpha-ethynyl-19-nortestosterone;18,19-Dinor-17-alpha-pregn-4-en-20-yn-3-one, 13-ethyl-17-hydroxy-, (+-)-;18,19-Dinorpregn-4-en-20-yn-3-one, 13-ethyl-17-hydroxy-,(17alpha)-(+-)-;Norgestrel (DL-);Levonorgestrel;(±)-Norgestrel;fh122-a;monovar;Neogest;NORPLANT;Ovrette;sh850;wy3707;(17α)-(±)-13-Ethyl-17-hydroxy-18,19-dinorpregn-4-en-20-yn-3-one;DL-13b-Ethyl-17a-ethynyl-17b-hydroxygon-4-en-3-one

Cas No.

6533-00-2

分子式

C₂₁H₂₈O₂

分子量

312.45

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Norgestrel is a synthetic analog of progesterone, a compound commonly found in oral contraceptive pill, and a powerful neuroprotective antioxidant, preventing light-induced ROS in photoreceptor cells, and cell death.

性状

Solid

体外研究(In Vitro)

Norgestrel (20 μM; 24 hours; 661W cells) treatment significantly increases cellular viability after serum deprivation and so it is demonstrated that Norgestrel is neuroprotective to stressed 661W cells.
Norgestrel (20 μM; 24 hours; 661W cells) treatment decreases apoptotic induced cleavage of PARP and caspase-3.
Norgestrel (20 μM; 6 hours; 661W cells) treatment bFGF is results in a significant upregulation of bFGF mRNA in photoreceptor cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	661W cells
Concentration:	20 μM
Incubation Time:	24 hours
Result:	Significantly increased cellular viability after serum deprivation.

Western Blot Analysis

Cell Line:	661W cells
Concentration:	20 μM
Incubation Time:	24 hours
Result:	Decreased apoptotic induced cleavage of PARP and caspase-3.

RT-PCR

Cell Line:	661W cells
Concentration:	20 μM
Incubation Time:	6 hours
Result:	A significant upregulation of bFGF mRNA over 1 hour.

体内研究(In Vivo)

Norgestrel (100 mg/kg; intraperitoneal injection; for 6, 24 or 48 hours; Balb/c mice) treatment can prevent light-induced ROS in photoreceptor cells, and subsequent cell death. Norgestrel acts via post-translational modulation of the major antioxidant transcription factor Nrf2; bringing about its phosphorylation, subsequent nuclear translocation, and increases levels of its effector protein superoxide dismutase 2 (SOD₂).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Balb/c mice are born into and maintained in dim cyclic light
Dosage:	100 mg/kg;
Administration:	Intraperitoneal injection; for 6, 24 or 48 hours
Result:	Increased expression and activation of Nrf2 via phosphorylation on serine 40, increased expression of its target antioxidant superoxide dismutase 2 (SOD₂), and reduced mitochondrial oxidative stress.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Wyse Jackson AC, et al. The synthetic progesterone Norgestrel is neuroprotective in stressed photoreceptor-like cellsand retinal explants, mediating its effects via basic fibroblast growth factor, protein kinase A and glycogen synthase kinase 3β signallin [Information]

[2]. Byrne AM, et al. The synthetic progestin norgestrel modulates Nrf2 signaling and acts as an antioxidant in a model of retinal degeneration. Redox Biol. 2016 Dec;10:128-139. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (320.05 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2005 mL	16.0026 mL	32.0051 mL
5 mM	0.6401 mL	3.2005 mL	6.4010 mL
10 mM	0.3201 mL	1.6003 mL	3.2005 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.00 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.00 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.00 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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