WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406649

CAS#: 444643-64-5

Description: CHF-4227 is a novel potent and selective estrogen receptor modulator. CHF 4227 binds with high affinity to the human estrogen receptor-alpha and -beta (dissociation constant K(i) = 0.017 and 0.099 nM, respectively). CHF 4227 compares favorably in efficacy and potency with raloxifene in preventing bone loss and in antagonizing EE2 stimulation of the uterus. This profile along with the minimal uterine stimulation suggests a therapeutic advantage to CHF 4227 over EE2 or raloxifene for the treatment of postmenopausal women. CHF 4227 is a well-tolerated SERM when administered once daily for 28 days. It is potentially active on bone resorption and serum lipids, without affecting the endometrium and without worsening hot flushes. CHF 4227 is a promising agent for the treatment of several conditions in postmenopausal women.

Chemical Structure

CAS# 444643-64-5

Theoretical Analysis

MedKoo Cat#: 406649
Name: CHF-4227
CAS#: 444643-64-5
Chemical Formula: C30H33NO4
Exact Mass: 471.24096
Molecular Weight: 471.59
Elemental Analysis: C, 76.41; H, 7.05; N, 2.97; O, 13.57

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Related CAS #: 444643-63-4   444643-64-5  

Synonym: CHF4227; CHF 4227; CHF-4227.

IUPAC/Chemical Name: 3-(4-methoxyphenyl)-4-(4-(2-(piperidin-1-yl)ethoxy)benzyl)-2H-chromen-7-ol


InChi Code: InChI=1S/C30H33NO4/c1-33-25-12-7-23(8-13-25)29-21-35-30-20-24(32)9-14-27(30)28(29)19-22-5-10-26(11-6-22)34-18-17-31-15-3-2-4-16-31/h5-14,20,32H,2-4,15-19,21H2,1H3


Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 471.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Civelli M, Preti AP, Cenacchi V, Rondelli I, Guastalla D, Tarral A, Dostert P, Guillevic Y, Homery MC. Single and multiple ascending dose studies of a novel tissue-selective oestrogen receptor modulator, CHF 4227, in healthy postmenopausal women. Br J Clin Pharmacol. 2007 Sep;64(3):304-16. Epub 2007 Mar 16. PubMed PMID: 17367495; PubMed Central PMCID: PMC2000661.

2: Armamento-Villareal R, Sheikh S, Nawaz A, Napoli N, Mueller C, Halstead LR, Brodt MD, Silva MJ, Galbiati E, Caruso PL, Civelli M, Civitelli R. A new selective estrogen receptor modulator, CHF 4227.01, preserves bone mass and microarchitecture in ovariectomized rats. J Bone Miner Res. 2005 Dec;20(12):2178-88. Epub 2005 Aug 1. PubMed PMID: 16294271.

3: Galbiati E, Caruso PL, Amari G, Armani E, Ghirardi S, Delcanale M, Civelli M. Pharmacological actions of a novel, potent, tissue-selective benzopyran estrogen. J Pharmacol Exp Ther. 2002 Oct;303(1):196-203. PubMed PMID: 12235251.


10.0mg / Not available

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