Fig. 1 · Structure

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Evista (Raloxifene HCl)

Cat. No. A10375 CAS 82640-04-8
Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.

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Publications for Evista (Raloxifene HCl)

1 publication citing this product

  1. Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371

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Biological Activity

Target & Activity

Target Activity Value
ER 5.7 nM

In Vivo Studies

In ovariectomized rats treated orally for five weeks, raloxifene hydrochloride partly preserved distal femoral bone mineral density and reduced serum cholesterol. Uterine wet weight increased modestly, although the measured uterine histology scores did not differ significantly from ovariectomized controls. Serum triglycerides were unchanged. These findings describe the tested rat model and do not establish clinical benefit or absence of uterine effects. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Five-week raloxifene hydrochloride response in ovariectomized rats

Animal study · Female Sprague–Dawley rats, 10–11 weeks old at acquisition; dosing started after ovariectomy recovery; repeated five-week dose-response design. [1]

Raloxifene partly preserved femoral BMD and lowered serum cholesterol. Uterine wet weight increased modestly without significant changes in measured histology scores; tissue selectivity does not imply no uterine response.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Distal femoral metaphysis BMD relative to intact controlsBMD relative to intact 88–90% at 0.1–10 mg/kg/day[1]
Serum cholesterol decrease relative to OVX controlsReported percentage decrease 37% at 0.1 mg/kg/day; 67% at 10 mg/kg/day[1]
Uterine wet weight after five weeksMean ± SEM OVX: 127 ± 5 mg; raloxifene 0.1 mg/kg/day: 196 ± 5 mg; raloxifene 10 mg/kg/day: 186 ± 4 mg[1]
Uterine epithelial height, myometrial thickness, stromal expansion, eosinophilia and composite estrogenicity scoresStatistical comparison No statistically significant raloxifene effect versus OVX controls on reported histology scores[1]
Serum triglyceridesStatistical comparison No significant change with raloxifene or ethynyl estradiol versus OVX controls[1]

Conditions shared by the study groups

Route
Oral gavage
Frequency
Daily
Treatment course
5 weeks
Vehicle
1.5% carboxymethylcellulose
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Raloxifene hydrochloride dose-response groups
0.01–10 mg/kg/day; endpoint-specific dose sets in Figures 2/4 and Table II.
OVX vehicle; intact controls; 17α-ethynyl estradiol 0.1 mg/kg/day comparator.Partial BMD protection and cholesterol reduction; modest uterine wet-weight increase without significant changes in reported histology scores. Triglycerides unchanged.[1]
Raloxifene hydrochloride dose-response groups
Model: Female ovariectomized Sprague–Dawley rats
Reported limits: Endpoint-specific sample sizes differ; animal-level overlap is not established.
Methods and source locations

Compound reported in the paper: Raloxifene hydrochloride; Compound label in the paper: LY139481 HCl

Preclinical evidence for the reported Lilly HCl material; no Adooq sourcing/lot validation.

Methods p.64; Results pp.64–66; Figures 2 and 4 with captions p.65; Tables I–II and footnotes p.66

Distal femoral metaphysis BMD relative to intact controls: Single-photon absorptiometry; Figure 2 mean ± SEM combines six experiments: intact n=28, OVX n=29, raloxifene n=30 per dose, estrogen n=12. Significantly above OVX but below intact controls, P < 0.05. — Results: Bone p.64; Figure 2/caption p.65; Methods p.64

Serum cholesterol decrease relative to OVX controls: Colorimetric assay; Figure 4 mean ± SEM: intact and OVX n=6 each, raloxifene n=12 per group, estrogen n=6; P < 0.05 versus OVX. — Results: Serum lipids and Figure 4/caption p.65; Serum assays p.64

Uterine wet weight after five weeks: Table II; n=6–12 per group, exact group-specific n not given. These raloxifene groups differ from OVX at P < 0.05 by Scheffé range test. — Table II/footnotes p.66; Results: Uterus p.65; Methods p.64

Uterine epithelial height, myometrial thickness, stromal expansion, eosinophilia and composite estrogenicity scores: Blinded semiquantitative histology. Table II reports relative scores, not absolute cell-height units; mean ± SEM for n=6–12 per group. Ethynyl estradiol increased these scores. — Uterine histology/Statistics p.64; Results pp.65–66; Table II p.66

Serum triglycerides: Enzymatic serum assay; Table I reports mean ± SEM for 6–12 rats per group. — Serum assays p.64; Serum lipids p.65; Table I p.66

Raloxifene hydrochloride dose-response groups · Methods p.64; Results pp.64–66; Figures 2 and 4 with captions p.65; Tables I–II and footnotes p.66

Specifications

Manufacturer Adooq Bioscience
Actions Modulator
CAS Number 82640-04-8
Formula C28H28ClNO4S
Molecular Weight 510
SMILES
C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 90 mg/mL (176.45 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
1% methylcellulose

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Black LJ, Sato M, Rowley ER, et al. Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. The Journal of clinical investigation (1994). PMID: 8282823 DOI: 10.1172/jci116985 Source material

Publications

1 publication citing this product

  1. Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371

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