Estradiol Acetate

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Cat Number

API4245414

CAS Number

4245-41-4

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Product Detail Description Scientific Support Customer Q&A

CAS Number

4245-41-4

Synonyms

β-Estradiol 3-acetate;Estra-1,3,5(10)-triene-3,17-diol (17β)-, 3-acetate

Molecular Formula

C20H26O3

Molecular Weight

314.4

Smiles

CC(=O)OC1=CC2=C(C=C1)[C@H]3CC[C@]4([C@H]([C@@H]3CC2)CC[C@@H]4O)C

Melting Point

136.5-137.5℃

Boiling Point

455.5℃

Relative Density

1.16

pKa

15.06

General Description

Estradiol Acetate is an esterified form of 17beta-estradiol, the most potent naturally occurring estrogen. Acetylation at the C-17 position modestly modulates the lipophilicity and pharmacokinetic profile of estradiol. As a prodrug of 17beta-estradiol, it is used in hormone replacement therapy (HRT) for menopausal symptoms and in the management of estrogen deficiency states.

Mechanism of Action

Estradiol Acetate is hydrolyzed by plasma and tissue esterases to 17beta-estradiol, which binds to intracellular estrogen receptors (ERalpha and ERbeta) in target tissues. The activated estrogen-receptor complex translocates to the nucleus, dimerizes, and modulates the transcription of estrogen-responsive genes involved in female reproductive development, bone homeostasis, cardiovascular protection, and cognitive function. Estrogen also exerts rapid non-genomic effects through membrane-associated ER signaling.

Application

Estradiol Acetate is indicated for the treatment of moderate to severe vasomotor symptoms (hot flashes, night sweats) associated with menopause, and for the treatment of hypoestrogenism due to hypogonadism, castration, or primary ovarian insufficiency.

Estradiol acetate (EA) is an oral prodrug that rapidly hydrolyzes to estradiol. Two 12-week randomized, double-blind, placebo-controlled trials evaluated EA 0.45 mg, 0.9 mg, and 1.8 mg in postmenopausal women with moderate-to-severe vasomotor symptoms. EA 1.8 mg significantly reduced symptom frequency versus placebo starting at week 2, EA 0.9 mg at week 3, and EA 0.45 mg at week 6. At week 12, mean frequency reductions from baseline were 61% (0.45 mg), 78% (0.9 mg), and 91% (1.8 mg), compared with 46% for placebo. Severity scores, vaginal pH, and maturation index improved significantly at all EA doses. Signs of vaginal atrophy improved with 0.9 mg and 1.8 mg. The responder rate (≥75% frequency reduction) at week 12 was 46.9% for EA 0.45 mg versus 26.9% for placebo. EA provides dose-dependent relief of menopausal vasomotor symptoms and vaginal atrophy.

Fig. 1 Oral estradiol acetate for menopause symptoms. (Speroff L.; et al. 2006)

References

Speroff L, et al. Efficacy of a new, oral estradiol acetate formulation for relief of menopause symptoms. Menopause, 2006, 13(3): 442-450.

What is the recommended storage condition for Estradiol Acetate?

It should be stored at controlled room temperature in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

Can we obtain batch-specific analytical data for Estradiol Acetate?

Batch-specific COA documents are standard with every shipment. Additional analytical reports, including HPLC chromatograms or spectral data, may be provided upon request.

What is the minimum order quantity (MOQ) for Estradiol Acetate?

Flexible MOQ options are available to support both early-stage research and large-scale manufacturing needs. Our team can tailor order quantities to match your specific requirements.

Is Estradiol Acetate compatible with standard pharmaceutical formulation processes?

Pharmaceutical-grade material suitable for standard formulation processes is available. Technical data sheets and compatibility information can be provided upon request.