Raloxifene HCl
Modify Date: 2024-01-02 17:34:54
Raloxifene HCl structure
|
Common Name | Raloxifene HCl | ||
|---|---|---|---|---|
| CAS Number | 82640-04-8 | Molecular Weight | 510.044 | |
| Density | 1.285g/cm3 | Boiling Point | 728.2ºC at 760 mmHg | |
| Molecular Formula | C28H28ClNO4S | Melting Point | 143-147ºC | |
| MSDS | Chinese USA | Flash Point | 394.2ºC | |
Use of Raloxifene HClRaloxifene hydrochloride(LY156758 hydrochloride) is a second generation selective estrogen receptor antagonist.Target: Estrogen receptorApproved: September 14, 2007Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays [1]. Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM [2]. Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats. [3]. Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue [4]. Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats [5]. |
| Name | raloxifene hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | Raloxifene hydrochloride(LY156758 hydrochloride) is a second generation selective estrogen receptor antagonist.Target: Estrogen receptorApproved: September 14, 2007Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays [1]. Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM [2]. Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats. [3]. Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue [4]. Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats [5]. |
|---|---|
| Related Catalog | |
| References |
| Density | 1.285g/cm3 |
|---|---|
| Boiling Point | 728.2ºC at 760 mmHg |
| Melting Point | 143-147ºC |
| Molecular Formula | C28H28ClNO4S |
| Molecular Weight | 510.044 |
| Flash Point | 394.2ºC |
| Exact Mass | 509.142761 |
| PSA | 98.24000 |
| LogP | 6.81510 |
| Index of Refraction | 1.654 |
| Storage condition | -20°C Freezer |
| Water Solubility | DMSO: 28 mg/mL, soluble |
| Precursor 10 | |
|---|---|
| DownStream 1 | |
![[4-(6-acetyloxy-1-benzothiophen-2-yl)phenyl] acetate Structure](https://image.chemsrc.com/caspic/336/84449-63-8.png)
CAS#:84449-63-8
CAS#:84449-80-9
CAS#:84541-36-6
CAS#:63675-74-1![[6-[(methylsulfonyl)oxy]-2-[4-[(methylsulfonyl)oxy]phenyl]benzo[b]thien-3-yl][4-[2-(1-pyrrolidinyl)ethoxy]phenyl]methanone hydrochloride Structure](https://image.chemsrc.com/caspic/336/84449-85-4.png)
CAS#:84449-85-4
CAS#:84449-90-1
CAS#:15570-12-4
CAS#:166975-76-4![4-Methoxy-alpha-[(3-methoxyphenyl)thio]acetophenone Structure](https://image.chemsrc.com/caspic/109/63675-73-0.png)
CAS#:63675-73-0
CAS#:2632-13-5|
Oxidative metabolic pathway of lenvatinib mediated by aldehyde oxidase.
Drug Metab. Dispos. 42(8) , 1326-33, (2014) Lenvatinib is a multityrosine kinase inhibitor that inhibits vascular endothelial growth factor receptors, and is being developed as an anticancer drug. P450s are involved in one of the elimination pa... |
|
|
Selective estrogen-receptor modulators suppress microglial activation and neuronal cell death via an estrogen receptor-dependent pathway.
J. Steroid Biochem. Mol. Biol. 145 , 85-93, (2015) Growing evidence shows that steroid hormones, especially 17β-estradiol (E2), protect neuronal cells by attenuating excess activation of microglia. However, the use of E2 in the clinic is controversial... |
|
|
Bioluminescent cell-based NAD(P)/NAD(P)H assays for rapid dinucleotide measurement and inhibitor screening.
Assay Drug Dev. Technol. 12(9-10) , 514-26, (2014) Abstract The central role of nicotinamide adenine dinucleotides in cellular energy metabolism and signaling makes them important nodes that link the metabolic state of cells with energy homeostasis an... |
| [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone hydrochloride |
| [6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(piperidin-1-yl)ethoxy]phenyl}methanone hydrochloride (1:1) |
| Raloxifene HCl |
| [6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanonhydrochlorid |
| 1-[2-(4-{[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]carbonyl}phenoxy)ethyl]piperidinium chloride |
| [6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(1-piperidinyl)ethoxy]phenyl}methanone hydrochloride (1:1) |
| Methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-, hydrochloride (1:1) |
| methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-, hydrochloride |
| 6-Hydroxy-2-(p-hydroxyphenyl)benzo(b)thien-3-yl-p-(2-piperidinoethoxy)phenyl ketone hydrochloride |
| MFCD01938233 |
| Raloxifene hydrochloride |
| Raloxifene (hydrochloride) |