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Treprostinil sodium

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Chemical Structure| 289480-64-4 同义名 : 曲前列素钠 ;UT-15 sodium;UT-15;Trevyent;Tyvaso;Orenitram;Remodulin
CAS号 : 289480-64-4
货号 : A867461
分子式 : C23H33NaO5
纯度 : 97%
分子量 : 412.495
MDL号 : -
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(60.61 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 15 mg/mL(36.36 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Prostaglandins such as prostacy-clin elicit their molecular, pharmacological and biochemical effects through binding and activation of specific receptor sites. The prostanoid receptors are identified as the IP, EP1, EP2, EP3, EP4, DP (now DP1), FP and TP receptor. The IP, EP2, EP4 and DP1 receptors are classically known to be Gs-coupled receptors linked to cyclic AMP (cAMP) generation. Treprostinil sodium is a highly potent DP1 and EP2 agonist with EC50 values of 0.6 ± 0.1 and 6.2 ± 1.2 nM, respectively. Treprostinil had high affinity for the DP1, EP2 and IP receptors with Ki values of 4.4, 3.6 and 32 nM, respectively, low affinity for EP1 and EP4 receptors and even lower affinity for EP3, FP and TP receptors[3]. 10 μM treprostinil inhibited ECFC (endothelial colony forming cells) proliferation in media containing either high or low serum concentrations. Treprostinil significantly stimulated ECFC+MSC (mesenchymal stem cells) induced vessel formation with a significant increase of microvessel density[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL
参考文献

[1]Whittle BJ, Silverstein AM, et al. Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist. Biochem Pharmacol. 2012 Jul 1;84(1):68-75.

[2]Ferrantino M, White RJ. Inhaled treprostinil sodium for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2011 Nov;12(16):2583-93.

[3]Whittle BJ, Silverstein AM, Mottola DM, Clapp LH. Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist. Biochem Pharmacol. 2012;84(1):68‐75

[4]Smadja DM, Levy M, Huang L, et al. Treprostinil indirectly regulates endothelial colony forming cell angiogenic properties by increasing VEGF-A produced by mesenchymal stem cells. Thromb Haemost. 2015;114(4):735‐747