Arzoxifene hydrochloride

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

MedKoo CAT#: 200310

CAS#: 182133-27-3 (HCl)

Description: Arzoxifene, also known as LY353381, is a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist. In comparison to other selective estrogen receptor modulators (SERMs), arzoxifene exhibits greater bioavailability and higher anti-estrogenic potency in the breast than raloxifene; it exhibits reduced estrogenicity in the uterus compared with either tamoxifen or raloxifene. This agent may have beneficial effects on bone and the cardiovascular system.

Chemical Structure

Arzoxifene hydrochloride
CAS# 182133-27-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 200310
Name: Arzoxifene hydrochloride
CAS#: 182133-27-3 (HCl)
Chemical Formula: C28H30ClNO4S
Exact Mass:
Molecular Weight: 512.06
Elemental Analysis: C, 65.68; H, 5.91; Cl, 6.92; N, 2.74; O, 12.50; S, 6.26

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Synonym: LY353381; LY-353381; LY 353381; SERM3; Arzoxifene hydrochloride.

IUPAC/Chemical Name: 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol , hydrochloride


InChi Code: InChI=1S/C28H29NO4S.ClH/c1-31-22-8-5-20(6-9-22)28-27(25-14-7-21(30)19-26(25)34-28)33-24-12-10-23(11-13-24)32-18-17-29-15-3-2-4-16-29;/h5-14,19,30H,2-4,15-18H2,1H3;1H


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 512.06 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: Arantes HP, Kulak CA, Fernandes CE, Zerbini C, Bandeira F, Barbosa IC, Brenol JC, Russo LA, Borba VC, Chiang AY, Bilezikian JP, Lazaretti-Castro M. Correlation between 25-hydroxyvitamin D levels and latitude in Brazilian postmenopausal women: from the Arzoxifene Generations Trial. Osteoporos Int. 2013 Oct;24(10):2707-12. doi: 10.1007/s00198-013-2366-x. Epub 2013 Apr 30. Erratum in: Osteoporos Int. 2013 Nov;24(11):2899-900. PubMed PMID: 23632825.

2: Powles TJ, Diem SJ, Fabian CJ, Neven P, Wickerham DL, Cox DA, Muram D, Agnusdei D, Dowsett SA, Amewou-Atisso M, Cummings SR. Breast cancer incidence in postmenopausal women with osteoporosis or low bone mass using arzoxifene. Breast Cancer Res Treat. 2012 Jul;134(1):299-306. doi: 10.1007/s10549-012-2041-5. Epub 2012 Apr 8. PubMed PMID: 22484799.

3: Goldstein SR, Bhattoa HP, Neven P, Cox DA, Dowsett SA, Alam J, Sipos A, Muram D. Gynecologic effects of arzoxifene in postmenopausal women with osteoporosis or low bone mass. Menopause. 2012 Jan;19(1):41-7. doi: 10.1097/gme.0b013e318223bbf4. PubMed PMID: 21993078.

4: Kendler DL, Palacios S, Cox DA, Stock J, Alam J, Dowsett SA, Zanchetta J. Arzoxifene versus raloxifene: effect on bone and safety parameters in postmenopausal women with osteoporosis. Osteoporos Int. 2012 Mar;23(3):1091-101. doi: 10.1007/s00198-011-1587-0. Epub 2011 Mar 4. PubMed PMID: 21374068.

5: Cummings SR, McClung M, Reginster JY, Cox D, Mitlak B, Stock J, Amewou-Atisso M, Powles T, Miller P, Zanchetta J, Christiansen C. Arzoxifene for prevention of fractures and invasive breast cancer in postmenopausal women. J Bone Miner Res. 2011 Feb;26(2):397-404. doi: 10.1002/jbmr.191. Epub 2010 Jul 23. PubMed PMID: 20658564.

6: Downs RW Jr, Moffett AM, Ghosh A, Cox DA, Dowsett SA, Harper K. Effects of arzoxifene on bone, lipid markers, and safety parameters in postmenopausal women with low bone mass. Osteoporos Int. 2010 Jul;21(7):1215-26. doi: 10.1007/s00198-009-1060-5. Epub 2009 Oct 2. PubMed PMID: 19798460.

7: Zwart W, Rondaij M, Jalink K, Sharp ZD, Mancini MA, Neefjes J, Michalides R. Resistance to antiestrogen arzoxifene is mediated by overexpression of cyclin D1. Mol Endocrinol. 2009 Sep;23(9):1335-45. doi: 10.1210/me.2008-0268. Epub 2009 May 28. PubMed PMID: 19477949; PubMed Central PMCID: PMC2737554.

8: Bolognese M, Krege JH, Utian WH, Feldman R, Broy S, Meats DL, Alam J, Lakshmanan M, Omizo M. Effects of arzoxifene on bone mineral density and endometrium in postmenopausal women with normal or low bone mass. J Clin Endocrinol Metab. 2009 Jul;94(7):2284-9. doi: 10.1210/jc.2008-2143. Epub 2009 Apr 7. PubMed PMID: 19351734.

9: Jackson LR, Cheung KL, Buzdar AU, Robertson JF. Arzoxifene: the evidence for its development in the management of breast cancer. Core Evid. 2008 Jul 31;2(4):251-8. PubMed PMID: 21221190; PubMed Central PMCID: PMC3012444.

10: Deshmane V, Krishnamurthy S, Melemed AS, Peterson P, Buzdar AU. Phase III double-blind trial of arzoxifene compared with tamoxifen for locally advanced or metastatic breast cancer. J Clin Oncol. 2007 Nov 1;25(31):4967-73. PubMed PMID: 17971595.

Additional Information

Related CAS#
CAS#182133-25-1 (Arzoxifene free base)
CAS#182133-27-3 (Arzoxifene hydrochloride)