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PPT

 
Catalog No.
B6735
ERα激动剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,733.00
现货
10mg
¥ 3,033.00
现货
25mg
¥ 5,091.00
现货

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A

背景

PPT, abbreviated from propyl pyrazole triol, is a potent, selective agonist of estrogen receptor α (ERα), with a reported 410-fold selectivity for ERα over ERβ. ERα is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen and involved in normal developmental, physiological, and reproductive processes in vertebrates. Compared with ERβ, ERα is encoded by a distinct gene, and differs in its relative and absolute tissue distribution. Since PPT exhibits subtype-selective property for estrogen receptors, it may serve as a useful tool for exploring how estrogens work through different ER subtypes.

References:

1. Sotoca AM, van den Berg H, Vervoort J, et al. Influence of cellular ERα/ERβ ratio on the ERα-agonist induced proliferation of human T47D breast cancer cells. Toxicological Sciences, 2008, 105(2): 303-311.

2. Stauffer SR, Coletta CJ, Tedesco R, et al. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. Journal of Medicinal Chemistry, 2000, 43(26): 4934-4947.

3. Harris HA, Katzenellenbogen JA, Katzenellenbogen BS. Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in vivo through the use of an ERα-selective ligand. Endocrinology, 2002, 143(11): 4172-4177.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt386.45
Cas No.263717-53-9
FormulaC24H22N2O3
Solubility≥95.4 mg/mL in DMSO,≥48.9 mg/mL in EtOH,insoluble in H2O
Chemical Name4-(1,5-bis(4-hydroxyphenyl)-4-propyl-1H-pyrazol-3(2H)-ylidene)cyclohexa-2,5-dienone
SDFDownload SDF
Canonical SMILESOC1=CC=C(C=C1)C(N(C(C=C2)=CC=C2O)N/3)=C(CCC)C3=C(C=C4)/C=CC4=O
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试验操作

Cell experiment:[3]

Cell lines

Saos-2 cells expressing either human ERα or ERβ

Reaction Conditions

1 μM PPT for 24 h incubation

Applications

PPT did not up-regulate metallothionein-II mRNA which is regulated only by ERβ, and only up-regulated IGFBP-4 mRNA (regulated by both ERα and ERβ) in Saos-2 cells expressing ERα.

Animal experiment:[3]

Animal models

Sexually immature Sprague Dawley rats

Dosage form

5 ~ 1000 μg/rat

Once daily by subcutaneous injection for 3 days

Applications

In a short-term (4 d) uterotrophic assay, PPT was found to be as efficacious as 17α-ethinyl-17β-estradiol in stimulating uterine weight gain and up-regulating complement 3 gene expression.

Note

The technical data provided above is for reference only.

References:

1. Sotoca AM, van den Berg H, Vervoort J, et al. Influence of cellular ERα/ERβ ratio on the ERα-agonist induced proliferation of human T47D breast cancer cells. Toxicological Sciences, 2008, 105(2): 303-311.

2. Stauffer SR, Coletta CJ, Tedesco R, et al. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. Journal of Medicinal Chemistry, 2000, 43(26): 4934-4947.

3. Harris HA, Katzenellenbogen JA, Katzenellenbogen BS. Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in vivo through the use of an ERα-selective ligand. Endocrinology, 2002, 143(11): 4172-4177.

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