Estropipate

Estrogen receptor agonist and OATP1B1 inhibitor CAS# 7280-37-7

Estropipate

Catalog No. BCC7719----Order now to get a substantial discount!

Product Name & Size Price Stock
Estropipate: 5mg $12 In Stock
Estropipate: 10mg Please Inquire In Stock
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Chemical structure

Estropipate

3D structure

Chemical Properties of Estropipate

Cas No. 7280-37-7 SDF Download SDF
PubChem ID 5284555 Appearance Powder
Formula C22H32N2O5S M.Wt 436.56
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 36 mg/mL (82.46 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name [(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate;piperazine
SMILES CC12CCC3C(C1CCC2=O)CCC4=C3C=CC(=C4)OS(=O)(=O)O.C1CNCCN1
Standard InChIKey HZEQBCVBILBTEP-ZFINNJDLSA-N
Standard InChI InChI=1S/C18H22O5S.C4H10N2/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19;1-2-6-4-3-5-1/h3,5,10,14-16H,2,4,6-9H2,1H3,(H,20,21,22);5-6H,1-4H2/t14-,15-,16+,18+;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Estropipate

DescriptionEstrogen receptor agonist. Also inhibits organic anion transporting polypeptide 1B1 (OATP1B1) (IC50= 70 nM).

Estropipate Dilution Calculator

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Estropipate Molarity Calculator

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Preparing Stock Solutions of Estropipate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2906 mL 11.4532 mL 22.9064 mL 45.8127 mL 57.2659 mL
5 mM 0.4581 mL 2.2906 mL 4.5813 mL 9.1625 mL 11.4532 mL
10 mM 0.2291 mL 1.1453 mL 2.2906 mL 4.5813 mL 5.7266 mL
50 mM 0.0458 mL 0.2291 mL 0.4581 mL 0.9163 mL 1.1453 mL
100 mM 0.0229 mL 0.1145 mL 0.2291 mL 0.4581 mL 0.5727 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Estropipate

Effects of estropipate treatment on plasma lipids and lipoprotein lipid composition in postmenopausal women.[Pubmed:1991799]

J Clin Endocrinol Metab. 1991 Feb;72(2):283-6.

It is generally believed that the cardioprotective benefit of long term treatment of postmenopausal women with estrogen results in part from its capacity to increase high density lipoprotein (HDL) and lower low density lipoprotein (LDL) concentrations. The extent to which the various estrogens employed in replacement treatment affect the composition of lipoproteins, however, is not known. For this reason, we have examined the impact of one such preparation, the synthetic estrone Estropipate (1.25 mg/day), on lipoprotein levels and composition in six postmenopausal women. After 6 months of treatment, whole plasma triglyceride (pretreatment, 135 +/- 63; posttreatment, 143 +/- 56 mg/dL), cholesterol (pretreatment, 232 +/- 14; posttreatment, 216 +/- 29 mg/dL), and HDL-C (pretreatment, 57.8 +/- 14.8; posttreatment, 55.6 +/- 13.2) were unchanged. However, plasma free (unesterified) cholesterol (FC) fell (pretreatment, 73.4 +/- 6.2; posttreatment, 53.7 +/- 9.3 mg/dL; P less than 0.05) and lecithin (L) rose significantly (pretreatment, 2.12 +/- 0.29; posttreatment, 2.47 +/- 0.34 mumol/mL; P less than 0.01). The consequence of these changes was a significant decline in the plasma FC/L ratio (pretreatment, 0.91 +/- 0.17; posttreatment, 0.68 +/- 0.12; P less than 0.01) to levels observed in healthy menstruating women. The calculated lipoprotein particle size was unchanged in very low density lipoproteins and increased significantly (P less than 0.05) in LDL after Estropipate therapy. Since qualitatively altered lipoproteins enriched in FC and an increased FC/L ratio in plasma are both associated with increased coronary risk, the improvement noted in these parameters after Estropipate therapy indicates that its use may be beneficial despite the lack of change in whole plasma lipids.

Estrogen regulation of the cytochrome P450 3A subfamily in humans.[Pubmed:15282264]

J Pharmacol Exp Ther. 2004 Nov;311(2):728-35.

This study examines the possible role of estrogen in regulating the expression of the human CYP3A subfamily: CYP3A4, CYP3A5, CYP3A7, and CYP3A43. To accomplish this goal, mRNA was quantified from human livers and endometrial samples, and total CYP3A protein levels were evaluated by Western immunoblot analysis of the liver samples. The human endometrial samples were from premenopausal and postmenopausal women. The premenopausal endometrium was either in the proliferative or secretory phase, whereas for the postmenopausal endometrium samples, the women had been treated with either a placebo or Estropipate, an estrogen substitute. After analyses, CYP3A4 mRNA was shown to have lower hepatic expression in females than in males. In the endometrium, CYP3A4 and CYP3A43 are down-regulated by estrogen, whereas CYP3A5 is expressed at higher levels during the secretory phase. CYP3A7 was not detected in the endometrium. In addition, the CYP3A subfamily showed increased mRNA expression in the liver as age increased. The expression levels of total CYP3A protein and total CYP3A mRNA showed good correlation. Despite apparent regulation of CYP3A4 mRNA expression by estrogen, the effects of estrogen may be overshadowed by additional regulators of gene expression.

Description

Estropipate is a form of estrogen, used to treat symptoms of menopause, also used to prevent osteoporosis.

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