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Tanaproget

产品编号 T16985 CAS 304853-42-7

别名: NSP-989

Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins (IC50: 0.1 nM),

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Tanaproget, CAS 304853-42-7

规格	价格/CNY	货期
2 mg	￥ 513	5日内发货
5 mg	￥ 997	5日内发货
10 mg	￥ 1,660	5日内发货
1 mL * 10 mM (in DMSO)	￥ 855	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins (IC50: 0.1 nM),
体外活性	In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mammalian two-hybrid assay to measure PR agonist-induced interaction between steroid receptor co-activator-1 and PR, TNPR showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1].
体内活性	TNPR effectively down-regulated MMP expression in vitro and induced a significant reduction of lesions in mice with disease established by tissues from endometriosis patients. The maximum concentration (C(max)) of tanaproget occurred approximately 2 to 3 h after administration. The elimination half-life (t(1/2)) ranged from 12 to 30 h, and the oral clearance was approximately 70 L/h. The pharmacokinetics of tanaproget was not noticeably altered with a high-fat meal [2][3].

别名	NSP-989
分子量	297.38
分子式	C16H15N3OS
CAS No.	304853-42-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (168.14 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3627 mL	16.8135 mL	33.627 mL	84.0675 mL
	5 mM	0.6725 mL	3.3627 mL	6.7254 mL	16.8135 mL
	10 mM	0.3363 mL	1.6814 mL	3.3627 mL	8.4068 mL
	20 mM	0.1681 mL	0.8407 mL	1.6814 mL	4.2034 mL
	50 mM	0.0673 mL	0.3363 mL	0.6725 mL	1.6814 mL
	100 mM	0.0336 mL	0.1681 mL	0.3363 mL	0.8407 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Bruner-Tran KL, et al. Down-regulation of endometrial matrix metalloproteinase-3 and -7 expression in vitro and therapeutic regression of experimental endometriosis in vivo by a novel nonsteroidal progesterone receptor agonist, tanaproget. J Clin Endocrinol Metab. 2006 Apr;91(4):1554-60. 2. Zhang Z, et al. Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget. J Biol Chem. 2005 Aug 5;280(31):28468-75. 3. Bapst JL, et al. Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women. Contraception. 2006 Nov;74(5):414-8.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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