| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Arzoxifene (also known as LY353381) is a novel, potent, synthetic aromatic derivative, and selective estrogen receptor antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. 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.
| ln Vitro |
Azoxifene blocks the growth of cells just as well as tamoxifen, an anti-estrogen. Northern analysis revealed that the expression of progesterone receptor B mRNA and pS2 was statistically significantly inhibited by arzoxifene. The expression of antitrypsin mRNA was shown to be significantly agonistic. As opposed to tamoxifen and estradiol, azoxifen does not increase the expression of cathepsin D mRNA and protein [1].
|
|---|---|
| ln Vivo |
In rats treated with ovariectomy, azoxifene avoided increases in body weight and blood cholesterol levels and, in a dose-dependent manner, brought them down below sham levels; its maximal efficacy was comparable to that of raloxifene or estrogen. Azoxifene (LY353381.HCl) has an ED50 of roughly 0.01 mg/kg and a maximum efficacy of 0.1–1 mg/kg/day in preventing bone loss caused by ovariectomy. Estrogen-induced increases in uterine weight are countered by arzoxifene (LY353381.HCl), which has an ED50 of 0.03 mg/kg/day and returns the weight to vehicle dose control levels [2].
|
| References | |
| Additional Infomation |
Arzoxifene Hydrochloride is the hydrochloride salt of arzoxifene, 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.
|
| Molecular Formula |
C28H29NO4S.HCL
|
|---|---|
| Molecular Weight |
512.0601
|
| Exact Mass |
511.158
|
| CAS # |
182133-27-3
|
| Related CAS # |
Arzoxifene;182133-25-1
|
| PubChem CID |
179338
|
| Appearance |
Off-white to light yellow solid powder
|
| Boiling Point |
656.4ºC at 760mmHg
|
| Flash Point |
350.8ºC
|
| Vapour Pressure |
7.85E-18mmHg at 25°C
|
| LogP |
7.679
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
35
|
| Complexity |
601
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NHSNLUIMAQQXGR-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol , hydrochloride
|
| Synonyms |
LY353381 HCl; LY353381; LY-353381; LY 353381; SERM3; Arzoxifene HCl; Arzoxifene hydrochloride.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~48.82 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9529 mL | 9.7645 mL | 19.5290 mL | |
| 5 mM | 0.3906 mL | 1.9529 mL | 3.9058 mL | |
| 10 mM | 0.1953 mL | 0.9764 mL | 1.9529 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA