2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Clomiphene

Clomiphene  (Synonyms: Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene)

Cat. No.: HY-A0287
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Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) is an orally active ovulation-inducing agent. Clomiphene binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene ameliorates memory impairment in PCOS models. Clomiphene mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer.

For research use only. We do not sell to patients.

Clomiphene

Clomiphene Chemical Structure

CAS No. : 911-45-5

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Based on 5 publication(s) in Google Scholar

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Clomiphene Related Antibodies

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Description

Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) is an orally active ovulation-inducing agent. Clomiphene binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene ameliorates memory impairment in PCOS models. Clomiphene mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
HT-1080 IC50
37.86 μM
Compound: 76
Inhibition of IDH1 R132H mutant in human HT-1080 cells assessed as suppression of 2-HG production incubated for 48 hrs by LC-MS analysis
Inhibition of IDH1 R132H mutant in human HT-1080 cells assessed as suppression of 2-HG production incubated for 48 hrs by LC-MS analysis
[PMID: 29847930]
In Vitro

Clomiphene (citrate) (1.0-5.0 μg/mL; 18 h) significantly increases hyperploidy and diploidy in cultured mouse germinal vesicle-stage oocytes, while reducing the proportion of metaphase I oocytes, indicating accelerated oocyte maturation[1].
Clomiphene (citrate) (10-50 μM) increases cytosolic free calcium levels in PC3 human prostate cancer cells with an EC50 of approximately 30 μM[4].
Clomiphene (citrate) (50 μM; 2-30 min) induces time-dependent mild cytotoxicity in PC3 human prostate cancer cells, reducing viability by 10-50% over 2-15 minutes of incubation with no further decrease after 15 minutes[4].

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

Clomiphene Related Antibodies

Cell Viability Assay[4]

Cell Line: PC3 human prostate cancer cells
Concentration: 50 μM
Incubation Time: 2 min; 5 min; 10 min; 15 min; 20 min; 30 min
Result: Reduced cell viability in a time-dependent manner: 2 minutes of incubation reduced viability by 10%, 15 minutes of incubation reduced viability by 50%, and extending incubation to 30 minutes did not further reduce viability.
In Vivo

Clomiphene (citrate) (25-100 mg/kg; i.p.; 3 doses over 4 hours) induces a significant 1.5% hyperploidy rate in mouse oocytes in vivo at the highest dose, while lower doses increase premature centromere separation and single unpaired chromatids, and all tested doses reduce ovulated oocyte counts[1].
Clomiphene (citrate) (1 mg/kg; p.o.; daily; 15 days) improves spatial and non-spatial memory impairment, restores reproductive hormone levels, increases serum antioxidant enzyme concentrations, and downregulates prefrontal cortex AchE gene expression in Letrozole (HY-14248)-induced PCOS rats, but does not reduce anxiety-like behavior[2].
Clomiphene decreases serum gonadotropin levels and reduces testosterone secretion in rats[4].

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

Animal Model: ICR (female, 8-12 weeks, 25-34 g, ovarian stimulation with PMSG and hCG)[1]
Dosage: 25, 50, 100 mg/kg
Administration: i.p.; 3 doses over 4 hours
Result: Increased hyperploidy to 1.5% (4 of 265 analyzed oocytes) and reduced average number of ovulated oocytes per mouse to 20.5 at 100 mg/kg.
Increased premature centromere separation to 5.0% (15 of 300 analyzed oocytes) and reduced average ovulated oocytes per mouse to 35.0 at 25 mg/kg.
Increased premature centromere separation to 3.6% (12 of 329 analyzed oocytes), increased single unpaired chromatids to 1.8% (6 of 329 analyzed oocytes), and reduced average ovulated oocytes per mouse to 37.7 at 50 mg/kg.
Animal Model: Wistar (female, 190-210 g, Letrozole-induced PCOS)[2]
Dosage: 1 mg/kg
Administration: p.o.; daily; 15 days
Result: Significantly increased spontaneous alternation performance count and percentage in the Y maze compared to PCOS-only rats.
Increased serum superoxide dismutase (SOD) and catalase concentrations compared to PCOS-only rats.
Showed weak non-significant reduction in serum interleukin-1β (IL-1B) levels compared to PCOS-only rats.
Reversed upregulated acetylcholine esterase (AchE) gene expression in the prefrontal cortex compared to PCOS-only rats.
Reduced follicle-stimulating hormone (FSH) to 0.31 mIU/mL, reduced luteinizing hormone (LH) to 3.14 mIU/mL, increased estradiol to 27.68 ng/mL, and reduced testosterone to 0.28 ng/mL compared to PCOS-only rats.
Did not reduce anxiety-like behavior, as anxiety index values remained statistically high compared to control rats.
Clinical Trial
Molecular Weight

405.96

Formula

C26H28ClNO
CAS No.
SMILES

Cl/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCN(CC)CC)/C3=CC=CC=C3
Shipping

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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Clomiphene Related Classifications

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Help & FAQs
  • 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:

Clomiphene911-45-5Clomifene (Z/E)-Enclomiphene (Z/E)-EnclomifeneEstrogen Receptor/ERRendoplasmic reticulumpolycystic ovary syndromePC3 human prostate cancer cellsPCOS modelshypothalamic estrogen receptorsletrozole-induced PCOS ratsmouse oocytesprostate cancer cellsestrogen receptormusk shrewsInhibitorinhibitorinhibit

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