PHTPP


Catalog No. Size PriceQuantity
M13386-2 2mg solid $100
M13386-10 10mg solid $300

Description

PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα.

Product information

CAS Number: 805239-56-9

Molecular Weight: 423.31

Formula: C20H11F6N3O

Chemical Name: 4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol

Smiles: OC1C=CC(=CC=1)C1=C2N=C(C=C(N2N=C1C1C=CC=CC=1)C(F)(F)F)C(F)(F)F

InChiKey: AEZPAUSGTAHLOQ-UHFFFAOYSA-N

InChi: InChI=1S/C20H11F6N3O/c21-19(22,23)14-10-15(20(24,25)26)29-18(27-14)16(11-6-8-13(30)9-7-11)17(28-29)12-4-2-1-3-5-12/h1-10,30H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 25 mg/mL (59.06 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PHTPP is a selective ERβ antagonist. PHTPP reduces FSH-mediated cAMP production by 80% (p<0.01) while it has no effect on basal cAMP. PHTPP (10-6 M) inhibits E2-stimulated ERβ activity, but does not suppress E2-stimulated ERα activity. A high dose of PHTPP (10-6 M) slightly increases class 1 Igf1 mRNA expression, and facilitates the DPN-induced increase in class 1 Igf1 mRNA expression.

References:

  1. Dennis R Compton, et al. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93.
  2. Ogo Y, et al. IGF-1 gene expression is differentially regulated by estrogen receptors α and β in mouse endometrial stromal cells and ovarian granulosa cells. J Reprod Dev. 2014;60(3):216-23. Epub 2014 Mar 25.

Products are for research use only. Not for human use.

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