Raloxifene hydrochloride
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 100761

CAS#: 82640-04-8 (HCl)

Description: Raloxifene is a selective estrogen receptor modulator with effects on bone and breast cancer and cardiovascular disease risk. It is used for breast cancer and osteoporosis research.

Chemical Structure

img
Raloxifene hydrochloride
CAS# 82640-04-8 (HCl)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 100761
Name: Raloxifene hydrochloride
CAS#: 82640-04-8 (HCl)
Chemical Formula: C28H28ClNO4S
Exact Mass: 0.00
Molecular Weight: 510.050
Elemental Analysis: C, 65.94; H, 5.53; Cl, 6.95; N, 2.75; O, 12.55; S, 6.29

Price and Availability

Size Price Availability Quantity
200mg USD 150
500mg USD 350
1g USD 650
2g USD 950
5g USD 1450
Bulk inquiry

Related CAS #: 84449-90-1 (free base)   82640-04-8 (HCl)   84449-90-1 (HCl)    

Synonym: LY-139481; LY139481; LY 139481; Raloxifene hydrochloride; US brand names: Evista; Keoxifene. Abbreviation: RALOX .

IUPAC/Chemical Name: (6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl)(4-(2-(piperidin-1-yl)ethoxy)phenyl)methanone hydrochloride

InChi Key: BKXVVCILCIUCLG-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H27NO4S.ClH/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29;/h4-13,18,30-31H,1-3,14-17H2;1H

SMILES Code: O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C31)C4=CC=C(OCCN5CCCCC5)C=C4.[H]Cl

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: EVISTA (raloxifene hydrochloride) is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM) that belongs to the benzothiophene class of compounds.Raloxifene HCl is an off-white to pale-yellow solid that is very slightly soluble in water. EVISTA is supplied in a tablet dosage form for oral administration. Each EVISTA tablet contains 60 mg of raloxifene HCl, which is the molar equivalent of 55.71 mg of free base. Inactive ingredients include anhydrous lactose, carnauba wax, crospovidone, FD&C Blue No. 2 aluminum lake, hypromellose, lactose monohydrate, magnesium stearate, modified pharmaceutical glaze, polyethylene glycol, polysorbate 80, povidone, propylene glycol, and titanium dioxide.     Mechanism of Action Decreases in estrogen levels after oophorectomy or menopause lead to increases in bone resorption and accelerated bone loss. Bone is initially lost rapidly because the compensatory increase in bone formation is inadequate to offset resorptive losses. In addition to loss of estrogen, this imbalance between resorption and formation may be due to age-related impairment of osteoblasts or their precursors. In some women, these changes will eventually lead to decreased bone mass, osteoporosis, and increased risk for fractures, particularly of the spine, hip, and wrist. Vertebral fractures are the most common type of osteoporotic fracture in postmenopausal women. The biological actions of raloxifene are largely mediated through binding to estrogen receptors. This binding results in activation of certain estrogenic pathways and blockade of others. Thus, raloxifene is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM). Raloxifene decreases resorption of bone and reduces biochemical markers of bone turnover to the premenopausal range. These effects on bone are manifested as reductions in the serum and urine levels of bone turnover markers, decreases in bone resorption based on radiocalcium kinetics studies, increases in bone mineral density (BMD), and decreases in incidence of fractures.  

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Raloxifene HCl is a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
In vitro activity: The combined treatment of raloxifene and gefitinib decreased the ability of neovascularization as assessed by tube formation of endothelial cells. These results suggested the potential of the combination of raloxifene and gefitinib for the prevention of triple-negative breast cancer growth and the appearance of metastatic events. Reference: Med Oncol. 2022 Dec 9;40(1):45. https://pubmed.ncbi.nlm.nih.gov/36494506/
In vivo activity: This study showed that raloxifene decreased depression, fearfulness, and anxiety after focal cranial blast traumatic brain injury in mice, using standard assays of these behavioral end-points. These results indicate that raloxifene could be used to treat deficits after mild traumatic brain injury. Reference: Neurotrauma Rep. 2022 Nov 24;3(1):534-544. https://pubmed.ncbi.nlm.nih.gov/36479361/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 102.0 199.98

Preparing Stock Solutions

The following data is based on the product molecular weight 510.05 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: 1. Narendra G, Raju B, Verma H, Kumar M, Jain SK, Tung GK, Thakur S, Kaur R, Kaur S, Sapra B, Singh PK, Silakari O. Raloxifene and bazedoxifene as selective ALDH1A1 inhibitors to ameliorate cyclophosphamide resistance: A drug repurposing approach. Int J Biol Macromol. 2023 Jul 1;242(Pt 1):124749. doi: 10.1016/j.ijbiomac.2023.124749. Epub 2023 May 7. PMID: 37160174. 2. Taurin S, Rosengren RJ. Raloxifene potentiates the effect of gefitinib in triple-negative breast cancer cell lines. Med Oncol. 2022 Dec 9;40(1):45. doi: 10.1007/s12032-022-01909-3. PMID: 36494506. 3. Hering NA, Günzler E, Arndt M, Zibell M, Lauscher JC, Kreis ME, Beyer K, Seeliger H, Pozios I. Targeting Interleukin-6/Glycoprotein-130 Signaling by Raloxifene or SC144 Enhances Paclitaxel Efficacy in Pancreatic Cancer. Cancers (Basel). 2023 Jan 11;15(2):456. doi: 10.3390/cancers15020456. PMID: 36672405; PMCID: PMC9856922. 4. Honig MG, Del Mar NA, Moore BM, Reiner A. Raloxifene Mitigates Emotional Deficits after Mild Traumatic Brain Injury in Mice. Neurotrauma Rep. 2022 Nov 24;3(1):534-544. doi: 10.1089/neur.2022.0052. PMID: 36479361; PMCID: PMC9718433.
In vitro protocol: 1. Narendra G, Raju B, Verma H, Kumar M, Jain SK, Tung GK, Thakur S, Kaur R, Kaur S, Sapra B, Singh PK, Silakari O. Raloxifene and bazedoxifene as selective ALDH1A1 inhibitors to ameliorate cyclophosphamide resistance: A drug repurposing approach. Int J Biol Macromol. 2023 Jul 1;242(Pt 1):124749. doi: 10.1016/j.ijbiomac.2023.124749. Epub 2023 May 7. PMID: 37160174. 2. Taurin S, Rosengren RJ. Raloxifene potentiates the effect of gefitinib in triple-negative breast cancer cell lines. Med Oncol. 2022 Dec 9;40(1):45. doi: 10.1007/s12032-022-01909-3. PMID: 36494506.
In vivo protocol: 1. Hering NA, Günzler E, Arndt M, Zibell M, Lauscher JC, Kreis ME, Beyer K, Seeliger H, Pozios I. Targeting Interleukin-6/Glycoprotein-130 Signaling by Raloxifene or SC144 Enhances Paclitaxel Efficacy in Pancreatic Cancer. Cancers (Basel). 2023 Jan 11;15(2):456. doi: 10.3390/cancers15020456. PMID: 36672405; PMCID: PMC9856922. 2. Honig MG, Del Mar NA, Moore BM, Reiner A. Raloxifene Mitigates Emotional Deficits after Mild Traumatic Brain Injury in Mice. Neurotrauma Rep. 2022 Nov 24;3(1):534-544. doi: 10.1089/neur.2022.0052. PMID: 36479361; PMCID: PMC9718433.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x