2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. (R)-Moxestrol

(R)-Moxestrol ((R)-R 2858; RU 16117) is an orally active weak partial agonist-antagonist of estrogen receptor (ER). (R)-Moxestrol binds to ER to form a rapidly dissociating complex, reduces the levels of estrogen and prolactin receptors, exerts weak estrogenic effects at low doses, and exhibits anti-estrogenic effects at high doses or when competing with E2 (HY-B0141). (R)-Moxestrol can be used in research related to breast cancer and postmenopausal estrogen deficiency (menopausal symptoms, severe osteoporosis).

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(R)-Moxestrol

(R)-Moxestrol Chemical Structure

CAS No. : 61665-15-4

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(R)-Moxestrol Related Antibodies

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Description

(R)-Moxestrol ((R)-R 2858; RU 16117) is an orally active weak partial agonist-antagonist of estrogen receptor (ER). (R)-Moxestrol binds to ER to form a rapidly dissociating complex, reduces the levels of estrogen and prolactin receptors, exerts weak estrogenic effects at low doses, and exhibits anti-estrogenic effects at high doses or when competing with E2 (HY-B0141). (R)-Moxestrol can be used in research related to breast cancer and postmenopausal estrogen deficiency (menopausal symptoms, severe osteoporosis)[3].

In Vitro

RU 16117 forms cytoplasmic estrogen receptor (ER) complexes in the uteri of immature mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(R)-Moxestrol Related Antibodies
In Vivo

(R)-Moxestrol (2-24 μg; i.p.; daily administration; for 4 consecutive weeks) inhibits DMBA (HY-W011845)-induced breast cancer growth in female rats in a dose-dependent manner[1][3].
(R)-Moxestrol (0.1-50 μg; subcutaneous injection) potently inhibits multiple indicators of the estrous cycle in rats[2][3].
(R)-Moxestrol (1-100 μg; subcutaneous injection; single injection, administered consecutively for 3 days; sustained release for 72 hours) exerts weak estrogenic effects in immature female Swiss mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (female, 50-55 days old, DMBA-induced mammary carcinoma)[1]
Dosage: 2 μg; 8 μg; 24 μg
Administration: i.p.; daily; 4 weeks
Result: Exhibited little effect on tumor number or total tumor area, caused a slight increase in average tumor size due to 11 new tumors developing, and showed no significant reduction in [3H]E2, [3H]R5020, or 125I-labeled ovine PRL receptor levels in tumor tissue at 2 μg daily.
Inhibited tumor number by 45% compared to controls, had minimal effect on total tumor area, caused a slight increase in average tumor size due to 4 new tumors developing, showed no significant reduction in [3H]E2, [3H]R5020, or 125I-labeled ovine PRL receptor levels in tumor tissue, and increased plasma PRL levels relative to controls at 8 μg daily.
Reduced tumor number by 65% compared to controls, caused marked reduction in total tumor area and average tumor size (only 3 new tumors developed), reduced [3H]E2 binding in tumor tissue from 2.3 pmoles/g (controls) to 0.3 pmoles/g, significantly reduced 125I-labeled ovine PRL specific binding in tumor tissue, resulted in low progesterone receptor levels in 4 of 6 tumors accompanying reduced estrogen and prolactin receptor levels, and increased plasma PRL levels relative to controls at 24 μg daily.
Animal Model: Sprague-Dawley (female, 200-225 g, with 2-3 prior 4-day estrous cycles)[2]
Dosage: 0.1-50 μg (various regimens)
Administration: s.c.; twice daily; 2-4 days; s.c.; single dose; s.c.; twice on single day
Result: Caused a 1-day delay in vaginal cornification with 0.5 μg twice-daily 4-day treatment.
Caused a 4.5 day delay in vaginal cornification with 5.0 μg twice-daily 4-day treatment.
Caused a 14.8 day delay in vaginal cornification with 50 μg twice-daily 4-day treatment.
Caused a 1.6 day delay in vaginal cornification with 0.5 μg twice-daily 2-day (estrus + diestrus 1) treatment.
Caused a 1.1 day delay in vaginal cornification with 1.5 μg twice-daily 2-day (estrus + diestrus 1) treatment.
Caused a 4.9 day delay in vaginal cornification with 4.5 μg twice-daily 2-day (estrus + diestrus 1) treatment.
Caused a 5.8 day delay in vaginal cornification with 13.5 μg twice-daily 2-day (estrus + diestrus 1) treatment.
Reduced uterine weight to 522 mg (0.5 μg), 358 mg (1.5 μg), 372 mg (4.5 μg), 327 mg (13.5 μg) at 1600 h on expected proestrus (control: 756 mg) with twice-daily 2-day (estrus + diestrus 1) treatment.
Reduced uterine weight to 489 mg (0.5 μg), 362 mg (1.5 μg), 282 mg (4.5 μg), 294 mg (13.5 μg) at 1000 h on expected estrus (control: 453 mg) with twice-daily 2-day (estrus + diestrus 1) treatment.
Completely inhibited ovulation (0/10 rats ovulating) with all doses ≥0.5 μg twice-daily 2-day (estrus + diestrus 1) treatment (control: 10/10).
Reduced plasma LH to 407 ng/mL (control: 888 ng/mL) with 0.5 μg twice-daily estrus-only treatment.
Reduced plasma LH to 103 ng/mL, plasma PRL to 23 ng/mL (control: 203 ng/mL), and uterine weight to 426 mg (control: 590 mg) with 2.5 μg twice-daily estrus-only treatment.
Completely inhibited the preovulatory LH and FSH peaks with 5 μg single dose injected at 2000 h proestrus, 0800 h estrus, or 2000 h estrus.
Depressed the plasma LH response to LHRH by 60% with 0.5 μg twice-daily 2-day (estrus + diestrus 1) treatment.
Almost completely inhibited the plasma LH response to LHRH with doses ≥ 1.5 μg twice-daily 2-day (estrus + diestrus 1) treatment.
Showed much less effectiveness at inhibiting the plasma LH response to LHRH with 4.5 μg and 13.5 μg twice-daily diestrus 1-only treatment compared to treatment over estrus + diestrus 1.
Animal Model: Swiss mice (immature 18-day old female)[3]
Dosage: 1 μg; 10 μg; 100 μg (single s.c.); 1 μg; 3 μg; 10 μg (daily s.c. x3); 30 μg (total s.c. over 3 days); 3 μg; 10 μg (continuous silastic implant over 72 hours)
Administration: s.c. (single injection); s.c. (daily for 3 consecutive days); silastic implant (continuous release over 72 hours)
Result: Increased uterine wet weight to a similar extent as 1 μg estradiol or moxestrol at 6 hours, but returned to control levels by 48 hours with a single 10 μg s.c. dose.
Maintained uterine weight increase for 48 hours with a single 100 μg s.c. dose.
Produced maximum uterine weight increase within 24 hours with three daily 1-3 μg s.c. doses, with no further effect from subsequent injections.
Required a daily 10 μg s.c. dose to match the effect of 0.1 μg estradiol.
Increased uterine weight 8-10-fold over 72 hours with silastic implants releasing 3 μg or 10 μg.
Depleted cytosolic ER by 1 hour, increased nuclear ER, and allowed cytosolic ER replenishment to control or above levels by 24 hours with a single 1 μg s.c. dose.
Kept cytosolic ER levels low for at least 24 hours with a single 100 μg s.c. dose.
Induced a 24-hour PR increase similar to estradiol, but PR levels returned to control by 48 hours with a single 1 μg s.c. dose.
Maintained PR at 3-4 times control at 48 hours, dropping to twice control by day 3 and control by day 5 with a single 100 μg s.c. dose.
Inhibited the estradiol-induced uterine weight increase by 30%, and antagonized estradiol-induced ER replenishment and PR induction with a total 30 μg s.c. dose over 3 days; lower doses were ineffective.
Molecular Weight

326.43

Formula

C21H26O3
CAS No.
SMILES

CO[C@H]1[C@@]2([H])[C@](CCC3=CC(O)=CC=C32)([H])[C@@]4([H])[C@](C1)([C@@](O)(CC4)C#C)C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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(R)-Moxestrol Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(R)-Moxestrol61665-15-4(R)-R 2858 RU 16117RU16117RU 16117RU-16117Estrogen Receptor/ERRovulationestrogen receptorSwiss miceuterine cytosolic ERprolactin receptor7,12-dimethylbenz[a]anthracene-induced mammary carcinomapostmenopausal estrogen deficiencySprague-Dawley ratsprogesterone receptorgonadotropin secretionInhibitorinhibitorinhibit

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