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PPT (Synonyms: PPT)

Catalog No.GC14370

PPT (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of PPT for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

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PPT Chemical Structure

Cas No.: 263717-53-9

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1mg
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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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Background

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).

Chemical Properties

Cas No. 263717-53-9 SDF
Synonyms PPT
Chemical Name 4-(1,5-bis(4-hydroxyphenyl)-4-propyl-1H-pyrazol-3(2H)-ylidene)cyclohexa-2,5-dienone
Canonical SMILES OC1=CC=C(C=C1)C(N(C(C=C2)=CC=C2O)N/3)=C(CCC)C3=C(C=C4)/C=CC4=O
Formula C24H22N2O3 M.Wt 386.45
Solubility ≤10mg/ml in ethanol;20mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5877 mL 12.9383 mL 25.8766 mL
5 mM 0.5175 mL 2.5877 mL 5.1753 mL
10 mM 0.2588 mL 1.2938 mL 2.5877 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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