6α-Fluorotestosterone
6α-Fluorotestosterone is a non-aromatizable aromatase inhibitor, with IC50 values of 115 nM and 580 nM against human and rat aromatase, respectively. 6α-Fluorotestosterone binds to the substrate site of human aromatase P450arom with a Ki of 150 nM, but is not aromatized into estrogen. In vivo, 6α-Fluorotestosterone maintains sexual behavior in castrated male rats (with an effect comparable to that of testosterone), induces defeminization of sexual development, and inhibits nuclear translocation of hypothalamic estrogen receptors; its pro-mating effect is blocked by the aromatase inhibitors ATD and Fadrozole (HY-14247A). Combined with Progesterone (HY-N0437), 6α-Fluorotestosterone induces lordosis behavior in ovariectomized female rats. 6α-Fluorotestosterone can be used in studies related to anovulatory infertility and sexual behavior regulation.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1597-68-8
- 分子式: C19H27FO2
- 分子量:306.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[2]|
P450arom 150 nM (Ki) |
体外実験
6α-Fluorotestosterone (1 μM; 15 min) is not aromatized by human placental microsomes, with less than 1% of the aromatization rate of testosterone[2].
6α-Fluorotestosterone (1 μM; up to 9 min) is not aromatized by human placental microsomes, purified reconstituted human placental P450_arom, or rat ovarian microsomes[2].
6α-Fluorotestosterone (0.01-10 μM; 8 min) potently inhibits testosterone aromatization in human placental microsomes (IC50 = 115 nM) and rat ovarian microsomes (IC50 = 580 nM)[2].
6α-Fluorotestosterone (250-500 nM; 6 min) competitively inhibits purified reconstituted human placental P450_arom with a Ki of 150 nM, exhibiting similar binding affinity to the natural substrate testosterone[2].
6α-Fluorotestosterone (5 μM) binds to the substrate site of aromatase in human placental microsomes, inducing the same low to high spin state shift of the heme iron as testosterone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Co-administration of 6α-Fluorotestosterone (500 μg; intravenous injection; single dose) with [3H]-estradiol does not directly compete for binding sites in the hypothalamic-preoptic area nuclei of castrated adult male rats[3].
Combination of 6α-Fluorotestosterone (600 μg; injection site not fixed; 3 times per week; for 3 consecutive weeks) with Progesterone (HY-N0437) induces lordosis behavior in ovariectomized female rats, while co-administration of 1 mg CI-628 (HY-100266) with each injection of this androgen inhibits this activity[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (male; castrated)[1]
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Dosage:25 μg/day (weeks 1-5); 50 μg/day (week 6); 100 μg/day (week 7); 200 μg/day (4 days post week 7); 400 μg/day (weeks 8-9)
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Administration:s.c.; daily starting the day after castration
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Result:Restored mating behavior with increased doses; showed 87.5% mount rate (7 of 8 males) in weeks 8-9.
Exhibited a mount rate of 1.0 mounts per min, mount latency of 13.9 min, mount efficiency of 71%, post-ejaculatory interval (PEI) of 6.9 min, and body weight gain of 49 g over weeks 1-5.
Reached a final seminal vesicle weight of 41 mg/100g body weight.
Showed reduced mount rate (0.4 mounts per min), increased mount latency (22.9 min), and increased PEI (9.9 min) over weeks 1-5 when co-administered with Fadrozole (HY-14247A).
Showed no difference from controls on mating metrics over weeks 1-5 when co-administered with ATD.
Showed 0% mount rate (0 of 16 males) in weeks 8-9 when co-administered with ATD or Fadrozole.
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Animal Model:Sprague-Dawley (male, castrated at 90 days of age)[3]
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Dosage:500 μg
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Administration:i.v.; single injection
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Result:Did not decrease cell nuclear binding of [3H] estradiol in the hypothalamus-preoptic area.
Left cortical nuclear radioactivity levels unchanged relative to controls.
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Animal Model:Sprague-Dawley (female, 70-80 days old, ovariectomized)[4]
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Dosage:600 μg
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Administration:The injection sites
were varied; three times weekly; 3 weeks -
Result:Induced lordosis behavior in ovariectomized female rats when given with progesterone, with an average lordosis quotient of 30.
Had its behavioral activity inhibited by concurrent administration of CI-628, reducing the average lordosis quotient to 12.
Did not differentially affect relative uterine weight compared to testosterone, and CI-628 did not alter uterine weight despite suppressing body weight.
化学情報
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CAS 番号 1597-68-8
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分子量 306.42
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分子式 C19H27FO2
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SMILES
C[C@@]12[C@@]3([C@]([C@]4([C@](C)(CC3)[C@@H](O)CC4)[H])(C[C@H](F)C1=CC(=O)CC2)[H])[H]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
6α-Fluorotestosterone 関連分類
HY-187614 関連分類
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