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PPT
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PPT图片
CAS NO:263717-53-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍

PPT (PPT) 是一种选择性雌激素受体α (ERα) 激动剂。 PPT对ER&#945的相对结合亲和力; (ERα: 49%) 比雌激素受体β (ERβ: 0.12%) 高约 410 倍。

Cas No.263717-53-9
别名PPT
化学名4-(1,5-bis(4-hydroxyphenyl)-4-propyl-1H-pyrazol-3(2H)-ylidene)cyclohexa-2,5-dienone
Canonical SMILESOC1=CC=C(C=C1)C(N(C(C=C2)=CC=C2O)N/3)=C(CCC)C3=C(C=C4)/C=CC4=O
分子式C24H22N2O3
分子量386.45
溶解度≤10mg/ml in ethanol;20mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

Estrogen receptor α (ERα) and ERβ are ligand-activated transcription factors that mediate the actions of estrogen. Activation of ERα, but not ERβ, is required for the cardioprotective effects of estradiol. Propylpyrazole triol (PPT) is an ERα selective agonist with a 410-fold relative binding affinity for ERα (49%) versus ERβ (0.12%) and therefore activates gene transcription only through ERα.[1],[2] In an in vivo rabbit model of ischemia-reperfusion injury, treatment with estradiol and PPT, but not diarylpropinitrile (a selective agonist of ERβ) significantly decreased the infarct size compared with vehicle.[3]

Reference:
[1]. Stauffer, S.R., Coletta, C.J., Tedesco, R., et al. Pyrazole ligands: Structure-affinity/activity relationships and estrogen receptor-α-selective agonists. Journal of Medicinal Chemistry 43, 4934-4947 (2000).
[2]. Meyers, M.J., Sun, J., Carlson, K.E., et al. Estrogen receptors-β potency-selective ligands: Structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogus. Journal of Medicinal Chemistry 44, 4230-4251 (2001).
[3]. Booth, E.A., Obeid, N.R., and Lucchesi, B.R. Activation of estrogen receptor-α protects the in vivo rabbit heart from ischemia-reperfusion injury. American Journal of Physiology 289, H2039-H2047 (2005).