Lasofoxifene tartrate
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Hodoodo CAT#: H563056

CAS#: 190791-29-8 (tartrate)

Description: 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.

Chemical Structure

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Lasofoxifene tartrate
CAS# 190791-29-8 (tartrate)
Instruction

Theoretical Analysis

Hodoodo Cat#: H563056
Name: Lasofoxifene tartrate
CAS#: 190791-29-8 (tartrate)
Chemical Formula: C32H37NO8
Exact Mass: 563.25
Molecular Weight: 563.647
Elemental Analysis: Chemical Formula: C32H37NO8 Exact Mass: 563.2519 Molecular Weight: 563.6470 Elemental Analysis: C, 68.19; H, 6.62; N, 2.49; O, 22.71

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
50mg USD 750 2 Weeks
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Related CAS #: 180916-16-9 (free base)   190791-29-8 (tartrate)  

Synonym: Lasofoxifene tartrate; Fablyn; CP-336156; CP 336156; CP336156;

IUPAC/Chemical Name: (5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol

InChi Key: INEHJXCWEVNEDZ-LUDNRVPPSA-N

InChi Code: InChI=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

SMILES Code: OC1=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

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

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 563.65 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.