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Lasofoxifene tartrate

Catalog No: 24054
CAS Number: 190791-29-8
Purity: 98% Min.

 Lasofoxifene, also known as CP 336156, is a non-steroidal selective estrogen receptor modulator (SERM) for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy. Lasofoxifene selectively binds to both ERα and ERβ with high affinity. Its IC50 for ERα (1.5 nM) is similar to that of estradiol (4.8 nM) and is at least 10-fold higher than those of tamoxifen and raloxifene.Lasofoxifene is a desmethyl dihydro analog of nafoxidine.

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Chemical Information

NameLasofoxifene tartrate
Iupac Chemical Name(5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
Synonyms Lasofoxifene tartrate; Fablyn; CP-336156; CP 336156; CP336156;
Molecular FormulaC32H37NO8
Molecular Weight563.64
SmileOC1=CC=C2C(CC[C@]([C@]2([H])C3=CC=C(OCCN4CCCC4)C=C3)([H])C5=CC=CC=C5)=C1.O[C@@](C(O)=O)([H])[C@@](O)([H])C(O)=O
InChiKeyINEHJXCWEVNEDZ-LUDNRVPPSA-N
InChiInChI=1S/C28H31NO2.C4H6O6/c30-24-11-15-27-23(20-24)10-14-26(21-6-2-1-3-7-21)28(27)22-8-12-25(13-9-22)31-19-18-29-16-4-5-17-29;5-1(3(7)8)2(6)4(9)10/h1-3,6-9,11-13,15,20,26,28,30H,4-5,10,14,16-19H2;1-2,5-6H,(H,7,8)(H,9,10)/t26-,28+;1-,2-/m10/s1
CAS Number190791-29-8
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Ordering Information

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FormulationOff-white solid
Purity98% Min.
StorageDry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
SolubilitySoluble in DMSO
HandlingRefer to MSDS
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
HS Code2934200090
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Targets
Mechanism
Cell study
Animal study
Clinical study

1: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Sep;30(7):543-88. PubMed PMID: 18985183.

2: Prakash C, Johnson KA, Schroeder CM, Potchoiba MJ. Metabolism, distribution, and excretion of a next generation selective estrogen receptor modulator, lasofoxifene, in rats and monkeys. Drug Metab Dispos. 2008 Sep;36(9):1753-69. doi: 10.1124/dmd.108.021808. Epub 2008 May 30. PubMed PMID: 18515329.

3: Space JS, Opio AM, Nickerson B, Jiang H, Dumont M, Berry M. Validation of a dissolution method with HPLC analysis for lasofoxifene tartrate low dose tablets. J Pharm Biomed Anal. 2007 Sep 3;44(5):1064-71. Epub 2007 May 3. PubMed PMID: 17560750.

4: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Sep;28(7):451-95. Review. PubMed PMID: 17003851.

5: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Jul-Aug;28(6):379-412. PubMed PMID: 16894408.

6: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Jan-Feb;28(1):31-63. PubMed PMID: 16541195.

7: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Sep;27(7):505-22. PubMed PMID: 16258596.

8: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Jul-Aug;27(6):411-61. PubMed PMID: 16179960.

9: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Jan-Feb;27(1):49-77. PubMed PMID: 15834459.

10: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. PubMed PMID: 12949633.

11: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2002 Nov;24(9):615-43. PubMed PMID: 12616707.

12: Ke HZ, Paralkar VM, Grasser WA, Crawford DT, Qi H, Simmons HA, Pirie CM, Chidsey-Frink KL, Owen TA, Smock SL, Chen HK, Jee WS, Cameron KO, Rosati RL, Brown TA, Dasilva-Jardine P, Thompson DD. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models. Endocrinology. 1998 Apr;139(4):2068-76. PubMed PMID: 9528995.

Chemical Structure

24054 - Lasofoxifene tartrate | CAS 190791-29-8

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