标签归档：dienogest

Dienogest-d4(Synonyms: STS 557-d4)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dienogest-d4 (Synonyms: STS 557-d4)

Dienogest-d4 是 Dienogest 氘代物。Dienogest(STS-557)是孕酮受体激动剂，有口服的子宫内膜活性，可作用于子宫内膜异位。

Dienogest-d4(Synonyms: STS 557-d4)

Dienogest-d4 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
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生物活性

Dienogest-d4 is deuterium labeled Dienogest.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

315.44

Formula

C20H21D4NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Oettel M, et al. Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations. Zentralbl Gynakol. 1997;119(12):597-606.

    [3]. Meena R, et al. Extended intervention time and evaluation of sperm suppression by dienogest plus testosterone undecanoate in male rat. Contraception. 2012 Jan;85(1):113-21.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Dienogest-d5(Synonyms: STS 557-d5)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dienogest-d5 (Synonyms: STS 557-d5)

Dienogest-d5 是 Dienogest 氘代物。Dienogest(STS-557)是孕酮受体激动剂，有口服的子宫内膜活性，可作用于子宫内膜异位。

Dienogest-d5(Synonyms: STS 557-d5)

Dienogest-d5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Dienogest-d5 is deuterium labeled Dienogest.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

316.45

Formula

C20H20D5NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Oettel M, et al. Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations. Zentralbl Gynakol. 1997;119(12):597-606.

    [3]. Meena R, et al. Extended intervention time and evaluation of sperm suppression by dienogest plus testosterone undecanoate in male rat. Contraception. 2012 Jan;85(1):113-21.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Dienogest-d6(Synonyms: STS 557-d6)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dienogest-d6 (Synonyms: STS 557-d6)

Dienogest-d6 是 Dienogest 氘代物。Dienogest(STS-557)是孕酮受体激动剂，有口服的子宫内膜活性，可作用于子宫内膜异位。

Dienogest-d6(Synonyms: STS 557-d6)

Dienogest-d6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Dienogest-d6 is deuterium labeled Dienogest.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

317.45

Formula

C20H19D6NO2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Oettel M, et al. Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations. Zentralbl Gynakol. 1997;119(12):597-606.

    [3]. Meena R, et al. Extended intervention time and evaluation of sperm suppression by dienogest plus testosterone undecanoate in male rat. Contraception. 2012 Jan;85(1):113-21.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Dienogest(Synonyms: 地诺孕素; STS 557)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dienogest (Synonyms: 地诺孕素; STS 557) 纯度: 99.83%

Dienogest(STS-557)是孕酮受体激动剂，有口服的子宫内膜活性，可作用于子宫内膜异位。

Dienogest(Synonyms: 地诺孕素; STS 557)

Dienogest Chemical Structure

CAS No. : 65928-58-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
10 mg ￥500 In-stock
50 mg ￥900 In-stock
100 mg ￥1500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis. Target: progesterone receptor agonist Dienogest is an orally active synthetic progesterone (or progestin). It is available for use as an oral contraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone [1]. Complete sperm suppression was observed in rats sacrificed either 60 or 90 days after dienogest (DNG)+ testosterone undecanoate (TU) administration, for two injections at 45-day interval. The neutral α-glucosidase activity in these treated rats remained in the normal range. Germ cell loss due to apoptosis was frequently observed both after 60 or 90 days of combination treatment. Significant decline in serum gonadotropin and testosterone, both serum and intratesticular levels, were observed in the treated rats. Following stoppage of treatment (given at 45-day interval) after two (0 and 45 days) or three injections (0, 45 and 90 days), complete restoration of spermatogenesis was observed by 120 and 165 days, respectively [2]. Clinical indications: Adenomyosis; Endometriosis FDA Approved Date: 1995 Toxicity: weight gain; increased blood pressure; breast tenderness and nausea

Clinical Trial

分子量

311.42

Formula

C20H25NO2
CAS 号

65928-58-7
中文名称

地诺孕素；双烯孕腈
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (80.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2111 mL 16.0555 mL 32.1110 mL
5 mM 0.6422 mL 3.2111 mL 6.4222 mL
10 mM 0.3211 mL 1.6055 mL 3.2111 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

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: ≥ 2.5 mg/mL (8.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.03 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 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-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.03 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.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.03 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Oettel M, et al. Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations. Zentralbl Gynakol. 1997;119(12):597-606.

    [2]. Meena R, et al. Extended intervention time and evaluation of sperm suppression by dienogest plus testosterone undecanoate in male rat. Contraception. 2012 Jan;85(1):113-21.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务