Propyl pyrazole triol

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Chemical Structure| 263717-53-9 同义名 : PPT
CAS号 : 263717-53-9
货号 : A293266
分子式 : C24H22N2O3
纯度 : 99%+
分子量 : 386.44
MDL号 : MFCD03453628
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%). The EC50 of Propyl pyrazole triol for the ERα-dependent response is 140 pM in ERα-U2OS(human osteosarcoma)-Luc cells. In the T47D-ERbeta cell line, PPT was unable to suppress cell proliferation at all ratios of ERalpha/ERbeta expression, reflecting its ability to activate only ERalpha and not ERbeta[1]. Moreover, repeated administration of the selective oestrogen receptors (ER)α agonist propyl-pyrazole triol (PPT) results in anxiolytic-like behaviours on the elevated plus maze (EPM) in primiparous (but not nulliparous) female rats. Acute PPT administration significantly modified EPM (elevated plus maze) behaviour as a function of reproductive experience, with nulliparous females tending toward increased anxiety-like behaviours and primiparous females tending toward decreased anxiety-like behaviours[2]. The increased MPO (myeloperoxidase) levels were inhibited with PPT in male pancreas and female lung and with 17β-estradiol in female pancreas[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.88mL

5.18mL

2.59mL

参考文献

[1]Stauffer SR, Coletta CJ, Tedesco R, Nishiguchi G, Carlson K, Sun J, Katzenellenbogen BS, Katzenellenbogen JA. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. J Med Chem. 2000 Dec 28;43(26):4934-47

[2]Byrnes EM, Casey K, Carini LM, Bridges RS. Reproductive experience alters neural and behavioural responses to acute oestrogen receptor α activation. J Neuroendocrinol. 2013 Dec;25(12):1280-1289

[3]Guleken Z, Ozbeyli D, Acikel-Elmas M, Oktay S, Alev B, Sirvanci S, Velioglu Ogunc A, Kasimay Cakir O. The effect of estrogen receptor agonists on pancreaticobiliary duct ligation induced experimental acute pancreatitis. J Physiol Pharmacol. 2017 Dec;68(6):847-858