Clomiphene
Based on 5 publication(s) in Google Scholar
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.
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- CAS No.: 911-45-5
- 화학식: C26H28ClNO
- 분자량:405.96
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Clomiphene
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
37.86 μM
Compound: 76
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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
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[PMID: 29847930] |
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.
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Cell Line:PC3 human prostate cancer cells
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Concentration:50 μM
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Incubation Time:2 min; 5 min; 10 min; 15 min; 20 min; 30 min
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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.
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.
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Animal Model:ICR (female, 8-12 weeks, 25-34 g, ovarian stimulation with PMSG and hCG)[1]
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Dosage:25, 50, 100 mg/kg
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Administration:i.p.; 3 doses over 4 hours
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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.
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Animal Model:Wistar (female, 190-210 g, Letrozole-induced PCOS)[2]
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Dosage:1 mg/kg
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Administration:p.o.; daily; 15 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 911-45-5
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분자량 405.96
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화학식 C26H28ClNO
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SMILES
Cl/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCN(CC)CC)/C3=CC=CC=C3
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Synonyms
Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Biochem Biophys Res Commun
Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]2020 Feb 19;522(4):862-868. PMID: 31806372 -
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순도&문서
References
[1]. London SN, et al. Clomiphene citrate-induced perturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes in vivo and in vitro. Fertil Steril. 2000;73(3):620-626. [Content Brief]
[2]. Akintoye OO, et al. Synergistic action of carvedilol and clomiphene in mitigating the behavioral phenotypes of letrozole-model of PCOS rats by modulating the NRF2/NFKB pathway. Life Sci. 2023;324:121737. [Content Brief]
[3]. Legro R S, et al. Clomiphene, metformin, or both for infertility in the polycystic ovary syndrome[J]. New England Journal of Medicine, 2007, 356(6): 551-566. [Content Brief]
[4]. Jiann BP, et al. Effect of clomiphene on Ca(2+) movement in human prostate cancer cells. Life Sci. 2002;70(26):3167-3178. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Clomiphene Related Classifications
HY-A0287 Related Classifications
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- Clomiphene
- 911-45-5
- Clomifene
- (Z/E)-Enclomiphene
- (Z/E)-Enclomifene
- Estrogen Receptor/ERR
- endoplasmic reticulum
- polycystic ovary syndrome
- PC3 human prostate cancer cells
- PCOS models
- hypothalamic estrogen receptors
- letrozole-induced PCOS rats
- mouse oocytes
- prostate cancer cells
- estrogen receptor
- musk shrews
- Inhibitor
- inhibitor
- inhibit